- Vibrational spectra and computational study of 3-amino-2-phenyl quinazolin-4(3H)-one
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FT-Raman and FT-IR spectra of 3-amino-2-phenyl quinazolin-4(3H)-one were recorded and analyzed. The vibrational wavenumbers of the title compound have been computed using the Hartree-Fock/6-31G* and B3LYP/6-31G* basis sets and compared with the experiment
- Panicker, C. Yohannan,Varghese, Hema Tresa,Ambujakshan,Mathew, Samuel,Ganguli, Subarna,Nanda, Ashis Kumar,Van Alsenoy, Christian,Mary, Y. Sheena
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- A novel hydrazide-based selective and sensitive optical chemosensor for the detection of Ni2+ ions: Applications in live cell imaging, molecular logic gates and smart phone-based analysis
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A novel flexible "N", "O"-rich hydrazide-based Schiff base chemoreceptor, 2-(benzamido)-N′-((pyridin-2-yl)methylene)benzohydrazide (L), was designed, synthesised and characterised via1H-NMR, IR spectroscopy, ESI-MS spectrometry and single-cryst
- Manna, Amit Kumar,Chowdhury, Shubhamoy,Patra, Goutam K.
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Read Online
- Synthesis, characterization and antibacterial activities of Zn(II) and Cd(II) complexes of a 3-amino-2-phenylquinazolin-4(3H )- -one Schiff base
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Zn(II) and Cd(II) complexes of a Schiff base derived from 3-amino-2-phenylquinazolin-4(3H)-one and 2-(2-formylphenoxy) acetic acid were prepared and characterized by elemental and different spectroscopic (IR, UV-Vis and NMR) analyses. The elemental analys
- Brahman, Dhiraj,Sinha, Biswajit
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Read Online
- Asymmetric Synthesis of N-N Axially Chiral Compounds by Phase-Transfer-Catalyzed Alkylations
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N-N axially chiral skeletons are significant structural motifs in natural products, pharmaceuticals, and functional materials. Herein we disclose a method for the asymmetric synthesis of N-N axially chiral compounds by phase-transfer catalysis. A wide range of N-N axially chiral quinazolinone derivatives were prepared in high yields with excellent stereoselectivities. Furthermore, the synthetic utility of the protocol was proved by large-scale reaction and transformation of the product. Density functional theory calculations provide insight into the mechanism.
- Pan, Ming,Shao, Ying-Bo,Zhao, Qun,Li, Xin
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p. 374 - 378
(2022/01/04)
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- Design, synthesis, pharmacological evaluation, in silico modeling, prediction of toxicity and metabolism studies of novel 1-(substituted)-2-methyl- 3-(4-oxo-2-phenyl quinazolin-3(4H)-yl)isothioureas
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Background: Although exhaustive efforts to prevent and treat tuberculosis (TB) have been made, the problem still continues due to multi-drug-resistant (MDR) and extensively drugresistant TB (XDR-TB). It clearly highlights the urgent need to develop novel
- Sulthana,Alagarsamy,Chitra
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p. 352 - 368
(2021/03/08)
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- Design, molecular docking, in vitro, and in vivo studies of new quinazolin-4(3H)-ones as VEGFR-2 inhibitors with potential activity against hepatocellular carcinoma
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A series of new VEGFR-2 inhibitors were designed, synthesized and evaluated for their anti-proliferative activities against hepatocellular carcinoma (HepG-2 cell line). Compound 29b (IC50 = 4.33 ± 0.2 μg/ml) was found to be the most potent derivative as it has showed to be more active than doxorubicin (IC50 = 4.50 ± 0.2 μg/ml) and 78% of sorafenib activity (IC50 = 3.40 ± 0.25 μg/ml). The inhibitory profiles against VEGFR-2 were also assessed for the most promising candidates (16b, 20c, 22b, 24a, 24b, 28c, 28e, 29a, 29b and 29c). Compounds 29b, 29c and 29a exhibited potent inhibitory activities towards VEGFR-2 at IC50 values of 3.1 ± 0.04, 3.4 ± 0.05 and 3.7 ± 0.06 μM, respectively, comparing sorafenib (IC50 = 2.4 ± 0.05 μM). Furthermorer, compound 29b induced apoptosis and arrested the cell cycle growth at G2/M phase. Additionally, in vivo antitumor experiments revealed that compounds 29b and 29c have significant tumor growth inhibition. The test of immuno-histochemical expression of activated caspase-3 revealed that there is a time-dependent increase in cleaved caspase-3 protein expression upon exposure of HepG-2 cells to compound 29b. Moreover, the fibroblastic proliferative index test revealed that compound 29b could attenuate liver fibrosis. Docking studies also supported the results concluded from the biological screening via prediction of the possible binding interactions of the target compounds with VEGFR-2 active sites using the crystal structure of VEGFR-2 downloaded from the Protein Data Bank, (PDB ID: 2OH4) using Discovery Studio 2.5 software. Further structural optimization of the most active candidates may serve as a useful strategy for getting new lead compounds in search for powerful and selective antineoplastic agents.
- Eissa, Ibrahim.H.,Ibrahim, Mohammed K.,Metwaly, Ahmed M.,Belal, Amany,Mehany, Ahmed B.M.,Abdelhady, Alsayed A.,Elhendawy, Mostafa A.,Radwan, Mohamed M.,ElSohly, Mahmoud A.,Mahdy, Hazem A.
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- Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines
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New acetamide (IV a-e) and 1,3-thiazolidinone derivatives (VII a-e) were designed, synthesized and assessed for their cytotoxic activity against MCF-7 and A549 cell lines along with their lead compounds (erlotinib and gefitinib). The newly designed compou
- Aziz, Marian W.,Kamal, Aliaa M.,Mohamed, Khaled O.,Elgendy, Adel A.
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- Design, synthesis, molecular modeling, in vivo studies and anticancer evaluation of quinazolin-4(3H)-one derivatives as potential VEGFR-2 inhibitors and apoptosis inducers
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Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer. Accordingly, new quinazoline-based derivatives having the structural features of VEGFR-2 inhibitors were designed and synthesized. Anti-proliferative activities were evaluated against three human cancer cell lines (HepG-2, MCF-7 and HCT-116) using MTT assay method. Doxorubicin and sorafenib were used as positive controls. Compounds 26b, 29a, 29b and 30 showed excellent anti-cancer activities against all cell lines. Moreover, compound 31 was the most active with IC 50 values of 3.97 ± 0.2, 4.83 ± 0.2 and 4.58 ± 0.3 μM, respectively. The most active cytotoxic agents were further evaluated in vitro for their VEGFR-2 inhibitory activities, compound 31 showed a high activity against VEGFR-2 with an IC50 value of 2.5 ± 0.04 μM, almost equal to that of sorafenib (IC50 = 2.4 ± 0.05 μM). Further studies revealed the ability of this promising quinazoline derivative 31 to induce apoptosis and arrest cell cycle growth at G2/M phase. In vivo antitumor activities of the synthesized compounds revealed that compounds 30 and 31 possessed significant tumor growth inhibition effect. Molecular docking studies were also performed and finally we can say that VEGFR-2 inhibition confers the reported cytotoxic activities.
- Belal, Amany,Eissa, Ibrahim H.,El-Gamal, Kamal M. A.,El-Sharkawy, Abdou,Elhendawy, Mostafa A.,Elsohly, Mahmoud A.,Ibrahim, Mohammed K.,Mahdy, Hazem A.,Mehany, Ahmed B. M.,Metwaly, Ahmed M.,Radwan, Mohamed M.
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- Quinazolinone-schiff's base hybrids as phosphodiesterase 4b inhibitors with dual activity against COPD and lung cancer
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A series of thirty compounds of quinazolinone-Schiff's base hybrids were rationally designed, synthesized, and evaluated for their in vitro Phosphodiesterase 4B inhibition, anti-lung and anti-colon cancer activities. Compounds 9, 16, 23, 29, 30, 31, 32 an
- Mansour, Mostafa A.,El-Saadi, Mohamed T.,Amin, Noha H.,Canzoneri, Joshua C.,Keeton, Adam B.,Piazza, Gary A.,Abdel-Rahman, Hamdy M.
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p. 4851 - 4866
(2020/12/25)
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- Synthesis, anticorrosion, antibacterial, and antifungal activity of new amphiphilic compounds possessing quinazolin-4(3H)-one scaffold
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For the first time, quinazolin-4(3H)-one-based cationic surfactants were prepared and fully characterized by IR and NMR spectroscopic techniques and elemental analysis. Some of their physicochemical properties, such as density, critical micelle concentrat
- ?ztürk, S.,Okay, S.,Y?ld?r?m, A.
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p. 2205 - 2214
(2020/12/09)
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- Quinazolin-4(3H)-ones and 5,6-dihydropyrimidin-4(3H)-ones from β-aminoamides and orthoesters
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Quinazolin-4(3H)-ones have been prepared in one step from 2-aminobenzamides and orthoesters in the presence of acetic acid. Simple 2-aminobenzamides were easily converted to the heterocycles by refluxing in absolute ethanol with 1.5 equivalents of the orthoester and 2 equivalents of acetic acid for 12–24 h. Ring-substituted and hindered 2-aminobenzamides as well as cases incorporating an additional basic nitrogen required pressure tube conditions with 3 equivalents each of the orthoester and acetic acid in ethanol at 110?C for 12–72 h. The reaction was tolerant towards functionality on the benzamide and a range of structures was accessible. Workup involved removal of the solvent under vacuum and either recrystallization from ethanol or trituration with ether-pentane. Several 5,6-dihydropyrimidin-4(3H)-ones were also prepared from 3-amino-2,2-dimethylpropionamide. All products were characterized by melting point, FT-IR, 1H-NMR, 13C-NMR, and HRMS.
- Gavin, Joshua T.,Annor-Gyamfi, Joel K.,Bunce, Richard A.
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- Design, synthesis and pharmacological evaluation of 2-phenyl quinazolin-4-one derivatives as anticolorectal cancer and anti-inflammatory agent
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Quinazoline derivatives are heterocyclic compounds that acts as important structural lead for the discovery of effective therapeutic agents. The anti-inflammatory activity along with cytotoxicity helps to reduce the inflammation and pain associated with carcinoma. Derivatives of quinazoline-4-one were preliminary screened and in silico molecular modelling studies using Autodock were performed. In the docking study, ligands were docked against anticancer and anti-inflammatory targets. In silico analysis revealed that the compounds with aromatic substitution at 3rd and halogen substitution at 6th or 7th positions possess lesser side effects and have more potent antitumor activity. Based upon these results 12 compounds were selected, synthesized, characterized and screened for their in vitro, anti-inflammatory, antioxidant and anticancer activities. From the in vitro studies, compounds QA4, QA7 and QB1 showed good anticancer, anti-inflammatory and antioxidant activity when compared to the standard.
- Bosco, Deena,Balakrishnan, Ashitha,Mishra, Rohan,Aneesh
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p. 2677 - 2685
(2018/11/20)
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- Quinazolinone platinum metal complexes: In silico design, synthesis and evaluation of anticancer activity
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Dihydrofolate reductase (DHFR) has been explored as a target for the development of agents for wide variety of human diseases, including cancer, autoimmune and infectious diseases. Several metal complexes are being used in management of cancer. The square planar Pt(II) complex, cis PtCl2(NH3)2 turned out to be even more effective at forcing filamentous growth. Cisplatin is an inorganic heavy metal complex that has activity similar to cell-cycle-phase-nonspecific alkylating agents such as cyclophosphamide and some other Ni and Cu metal complexes. It produces intrastrand DNA cross-link and form DNA adducts, thus inhibiting the synthesis of DNA, RNA and proteins preferentially. in silico Screening of platinum metal complexes was performed by Vlife MDS 4.3 software. In this procedure, selection of molecule, selection of PDB, optimization of PDB and docking of molecules was carried out. Synthesis of metal complexes was done by multi component reaction method. Platinum metal complexes of quinazolinone Schiff bases prioritized by in silico studies were characterized by IR, TLC, NMR, XRD, FESEM and some physico-chemical parameters. Prioritized molecules were further evaluated by in vitro anticancer cell line assay on ten cell lines with adriamycin as standard. The results showed that the platinum metal complexes of qunazolinone Schiff bases can be potential anticancer agents through DHFR inhibitory mechanism.
- Sawant, Sanjay D.,Sahu, Megha,Nerkar, Amit G.
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p. 2164 - 2170
(2018/09/10)
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- Anti-convulsant potential of quinazolinones
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A series of novel quinazoline derivatives were synthesized, virtually screened through different filters and evaluated for their anticonvulsant activity against electrically and chemically induced seizures, compared with that of the standard drugs methaqualone and sodium valproate. Compound 48, 3-(2-aminophenyl)-7-chloro-2-phenylquinazolin-4(3H)-one, was found to be the most potent compound of the series accompanied by relatively low neurotoxicity and low toxicity in the median lethal dose test as compared with the reference drugs. The obtained results showed that compounds 12, 48, 49 and 50 could be useful templates for future design, optimization, and investigation to construct more active analogs.
- Patel, Harun M.,Noolvi, Malleshappa N.,Shirkhedkar, Atul A.,Kulkarni, Abhijeet D.,Pardeshi, Chandrakantsing V.,Surana, Sanjay J.
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p. 44435 - 44455
(2016/06/09)
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- Synthesis, Antimicrobial and Anticancer Evaluation of 2-Azetidinones Clubbed with Quinazolinone
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A novel series of 2-azetidinones clubbed with quinazolinone was synthesized using anthranilic acid. All the synthesized compounds were evaluated for their antimicrobial activity against two Gram positive bacterial strains (Bacillus subtilis and Staphyloco
- Deep, Aakash,Kumar, Pradeep,Narasimhan, Balasubrmanian,Meng, Lim Siong,Ramasamy, Kalavathy,Mishra, Rakesh Kumar,Mani, Vasudevan
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- Design and synthesis of quinazolinyl acetamides for their analgesic and anti-inflammatory activities
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A variety of novel 2-(substituted)-N-(4-oxo-2-phenylquinazolin-3(3H)-yl)acetamides were synthesized by the reaction of 2-chloro-N-(4-oxo-2-phenylquinazolin-3(3H)-yl)acetamide with various amines. The starting material, 2-chloro-N-(4-oxo-2-phenylquinazolin
- Alagarsamy, Veerachamy,Solomon, Viswas Raja,Sulthana, Mohaideen Thasthagir,Vijay, Meduri Satyasai,Narendhar, Bandi
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p. 597 - 604
(2016/02/12)
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- Design and synthesis of quinazolinone tagged acridones as cytotoxic agents and their effects on EGFR tyrosine kinase
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In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR.
- Babu, Yarlagadda Rajesh,Bhagavanraju, Mantripragada,Reddy, Gade Deepak,Peters, Godefridus J.,Prasad, Velivela V. S. Rajendra
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p. 624 - 634
(2014/11/08)
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- Synthesis and characterization of quinazoline derivatives: Search for hybrid molecule as diuretic and antihypertensive agents
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To explore the pharmacological and structure-activity relationship of a series of N-substituted-(4-oxo-2-substituted-phenylquinazolin-3-(4H)-yl), substituted benzene sulfonamide derivatives (1-25) were synthesized from substituted anthranilic acids derive
- Rahman, Mujeeb Ur,Rathore, Ankita,Siddiqui, Anees A.,Parveen, Gazala,Yar, M. Shahar
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p. 733 - 743
(2014/12/11)
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- Novel quinazolin-4(3H)-one/Schiff base hybrids as antiproliferative and phosphodiesterase 4 inhibitors: Design, synthesis, and docking studies
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A novel series of quinazolin-4(3H)-one/Schiff base hybrids was rationally designed and synthesized. The prepared compounds were evaluated for in vitro activity to inhibit phosphodiesterase 4 (PDE4), where several of them showed good-to-moderate activity c
- Abdel-Rahman, Hamdy M.,Abdel-Aziz, Mohamed,Canzoneri, Joshua C.,Gary, Bernard D.,Piazza, Gary A.
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p. 650 - 657
(2014/11/07)
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- Dihydrofolate reductase inhibitors: Synthesis, characterization and biological evaluation of some novel 2,3-disubstituted quinazolinones
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A series of some novel dihydrofolate reductase inhibitors (DHFR) of 2,3-disubstituted quinazolinone derivatives were synthesized by condensing benzoxazone derivatives with compounds containing primary amino group. The chemical structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analysis. The enzyme inhibitory activities were studied by using GLIDE 4.5 module. In vitro cytotoxic activity of the synthesized compounds was evaluated by MTT assay method. Compounds 3g and 5a exhibited good hydrogen bond interactions with the amino acid residue of DHFR and also showed significant cytotoxic activity.
- Hemalatha,Kumar, M. Suresh,Girija
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- Synthesis, characterization and antibacterial activities of Zn(II) and Cd(II) complexes of a quinazoline-4(3H)-one Schiff base
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Zn(II) and Cd(II) complexes of a Schiff base derived from quinazoline-4(3H) one and 2-formylphenoxy acetic acid were prepared and characterized by elemental and different spectroscopic (IR, UV-Visible and NMR) analyses. The elemental analysis indicated th
- Brahman, Dhiraj,Sinha, Biswajit
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- Design and synthesis of some new quinazolin-4-(3H)-ones as anticonvulsant and antidepressant agents
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A series of 3-[(4-substituted-benzylidene)-amino]-2-phenyl-3H-quinazolin-4- ones (5a-k) were synthesized by reacting 3-amino-2-phenyl-1H-quinazolin-4-one with p-hydroxybenzaldehyde, and then further with various alkyl/benzyl halides or substituted phenacy
- Amir, Mohd,Ali, Israr,Hassan, Mohd Zaheen
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- Synthesis and biological evaluation of some new quinazolin-4(3H)-ones derivatives as anticonvulsants
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Epilepsy is the most common neurological disorder known, affecting around 1 % of the world's population, characterized by recurrent seizure attack. A new series of 2-phenyl-3-(3-(substituted-benzylideneamino)-quinazolin-4(3H)-one derivatives (6a-h) was sy
- Gupta, Deepak,Kumar, Rajiv,Roy, Ram Kumar,Sharma, Adish,Ali, Israr,Shamsuzzaman, Md.
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p. 3282 - 3288
(2013/07/27)
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- Synthesis of novel 2-phenyl-3-[2-(substituted amino) ethylamino] quinazolin-4(3H)-ones as a new class of H1-antihistaminic agents
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A series of novel 2-phenyl-3-[2-(substituted amino) ethylamino] quinazolin-4(3H)-ones was synthesized by the nucleophilic substitution of 3-(2-bromo ethylamino)-2-phenyl quinazolin-4(3H)-one with various amines. The starting material, 3-(2-bromo ethylamin
- Alagarsamy,Shyam Sundar,Gobinath,Nivedhitha,Parthiban,Shankar,Sulthana,Raja Solomon
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p. 2486 - 2492
(2013/07/26)
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- Novel quinazolin-3(H)-4-one derivatives by microwave synthesis
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The substituted quinazolinones are reported to possesses anticonvulsant activity as they are cyclic amides and exhibit potent AMPAR non-competitive antagonism. The intermediate compound, 2-phenyl-4H-3,1-benzoxazin-4-one was synthesized from anthranilic ac
- Mathew, Mincy,Chand, M. Suresh,Jayasekhar
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p. 3103 - 3105
(2012/07/28)
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- Synthesis and evaluation of quinazoline derivative as antimicrobial and surface active agent
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Anthranilic acid reacted with benzoyl chloride to produce 2-substituted 3,1-benzoxazin-4-one which was used as starting material to synthesize 3-{[bis(4-fluorophenyl)methylidene]amino}-2-phenylquinazolin-4(3H)-one. The products were subjected to reaction
- Saini, Sangita,Kaur, Harmeet,Garg, Arun,Singh,Mishra
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p. 1425 - 1428
(2012/09/07)
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- Synthesis, spectroscopic characterization, antineoplastic, in vitro-cytotoxic, and antibacterial activities of mononuclear ruthenium(II) complexes
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The synthesis, antineoplastic, cytotoxic, and antibacterial activities of Ru(II) complexes derived from quinazoline and thiosemicarbazone ligands are reported. These complexes have been prepared and characterized by UV-Vis, IR, 1H-NMR, FAB-mass
- Thota, Sreekanth,Imran, Mohammad,Udugula, Manasa,Karki, Subhas Somalingappa,Kanjarla, Narasimha,Yerra, Rajeshwar,Balzarini, Jan,De Clercq, Erik
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p. 823 - 839
(2012/09/22)
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- Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one
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Thirty new 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one were designed and synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The anticonvulsant activity of the titled compounds was assessed using the 6 Hz psychomotor seizure test. The most active compound of the series was 3-({(E)-[3-(4-chloro-3-methylphenoxy)phenyl]methylidene}amino) -2-phenylquinazolin-4(3H)-one PhQZ 7, which showed 100% protection (4/4, 0.5 h) and 75% protection (3/4, 0.25 h) at a dose of 100 mg/kg in mice. A computational study was carried out for calculation of pharmacophore pattern and prediction of pharmacokinetic properties. Titled compounds have also exhibited good binding properties with epilepsy molecular targets such as glutamate, GABA (A) delta and GABA (A) alpha-1 receptors, in Lamarckian genetic algorithm based flexible docking studies.
- Kumar, Praveen,Shrivastava, Birendra,Pandeya, Surendra N.,Stables, James P.
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p. 1006 - 1018
(2011/04/24)
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- Design, facile synthesis and biological evaluation of quinazoline containing pyrazolothiazolyl, triazinone and their ethoxyphthalimide derivatives
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A series of 3-(4-substituted benzylidene)-4-N-ethoxyphthalimido-6-phenyl-3, 4-dihydro-2H-[1,2,4]triazino[2,3-c]quinazolin-2-one 6a-d and 3-[3-(4-substituted benzylidene-5-phenyl-2-N-ethoxyphthalimido-3,3a-dihydro-2H-pyrazolo[3,4-d][1,3] thiazol-6(5H)-yl)]
- Dangi, Raja Ram,Hussain, Nasir,Joshi, Ajit,Pemawat, Gangotri,Talesara, Ganpat Lal
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p. 1165 - 1172
(2011/10/12)
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- Synthesis and antiviral activity of 2-aryl-3-(substituted-benzalamino)- 4(3H)-quinazolinones
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A series of new heterocyclic compounds 2-aryl-3-(substituted-benzalamino)- 4(3H)-quinazolinone have been synthesized by the treatment of 3-amino-2-aryl-4(3H)-quinazolinone with a substituted benzaldehyde in ethanol. All the synthesized compounds were char
- Pandey, Shradha,Singh, Pravin K.,Siddiqui,Singh, Jagdamba
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p. 835 - 839
(2012/04/04)
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- Synthesis of quinozoline and its imino sugars by using NaY zeolite catalyst under microwave condition
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3-Amino-2-phenylquinazolin-4-(3H)-one (2) has been synthesized by the treatment of hydrazine hydrate with 2-phenyl- 4H-3,1-benzoxazin-4-one (1) using NaY zeolite as a solid support under microwave irradiation. Compound (2) on reaction with various aldoses affords the corresponding imino sugars (3a-h). In this work, NaY zeolite has been found to act both as solid support as well as catalyst.
- Rawala, Manish Kumar,Tiwaria, Urvashi,Parashara, Bharat,Ametab, Rakshit,Punjabi, Pinki B
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experimental part
p. 734 - 737
(2011/07/30)
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- In vitro bacteriostatic and DNA interaction studies of drug-based mixed-ligand complexes of cobalt(II)
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The dinuclear cobalt(II) complexes with ciprofloxacin and bidentate ligands were synthesized and characterized using infrared spectra, electronic spectra, magnetic measurements, elemental analyses, thermal investigation, and mass spectroscopy. Here in we
- Patel, Mohan,Chhasatia, Mehul,Bhatt, Bhupesh
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experimental part
p. 220 - 230
(2012/03/10)
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- Synthesis of some N-(4-oxo-2-sustitutedphenylquinazolin-3-(4H)-yl)-2-[(5- aryl-1,3.4-oxadiazol-2-yl) sulfanyl] acetamides as antitubercular agents
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A series of some N-(4-oxo-2-substituted phenylquinazolin-3-(4H)-yl)-2-[(5- aryl-1,3,4-oxadiazol-2-yl) sulfanyl] acetamides 5 were synthesized and characterized on the basis of IR, NMR and mass spectral data. The title compounds were subjected to in-vitro
- Rao, Gopal Krishna,Rajasekaran,Sanjay Pai
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body text
p. 293 - 294
(2011/12/15)
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- Conversion of solar energy to chemical energy
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The rate of evolution of hydrogen from water by photochemical process using solar energy has been investigated employing fourteen metal complexes as catalysts, ten electron relays, three electron donors and two co-catalysts in different permutation and combinations. The effect of varying reaction conditions like temperature, concentration and pH have also been investigated for the optimum production of hydrogen by the photochemical cleavage of water molecules.
- Ranganayakulu,Murthy
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p. 309 - 316
(2011/08/09)
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- Quinazolinones with amide linkage: Synthesis and antimicrobial activity
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Treatment of anthranilic acid in pyridine with benzoyl chloride gives 2-phenyl-3,1-benzoxazine-4-one (I). 3-Amino-2-phenylquinazol-4-one (II) was synthesized by reaction of 2-phenyl-3,1-benzoxazine-4-one I with hydrazine hydrate (80%) in ethanol. Aseries of amides were synthesized by treatment of various substituted acid chlorides with 3amino-2-phenylquinazol-4-one using pyridine as solvent. All the synthesized compounds were characterized by elemental analysis and spectral data. They were screened for antibacterial activity against E. coli and S. aureus and for antifungal activity against A. niger by cup plate method at 1 μg/ml cone in DMF. All the synthesized compounds showed good to moderate antimicrobial activity.
- Prajapati,Modi, Vishal
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p. 269 - 272
(2011/12/15)
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- Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases
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A combinatorial series of novel quinazolin-4(3H)-ones were synthesised and their structures were established based on spectroscopic data (IR, NMR, EI-MS, and FAB-MS). The compounds were tested for inhibition of the zinc metalloproteinase thermolysin (TLN) utilizing a chemical array-based approach. Some of the compounds were found to inhibit TLN, with IC50 values ranging from 0.0115 μM (compound 3) to 122,637 μM (compound 29). Compound 3 [3-phenyl-2-(trifluoromethyl) quinazolin-4(3H)-one] (IC50 = 0.0115 μM) and compound 35 [3-(isopropylideneamino)-2,2-dimethyl-2,3-dihydroquinazolin-4 (1H)-one] (IC50 = 0.2477 μM) were found to be the most potent inhibitors.
- Khan, Mahmud Tareq Hassan,Khan, Rasool,Wuxiuer, Yimingjiang,Arfan, Mohammad,Ahmed, Manzoor,Sylte, Ingebrigt
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experimental part
p. 4317 - 4327
(2010/09/12)
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- Antibacterial and DNA interaction studies of zinc(II) complexes with quinolone family member, ciprofloxacin
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DNA binding and cleavage characteristics of Zn(II) complexes have been investigated. The DNA interaction property of the complexes has been investigated using absorption spectra, viscosity measurements, as well as gel electrophoresis studies. Intrinsic bi
- Patel, Mohan,Chhasatia, Mehul,Parmar, Pradhuman
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experimental part
p. 439 - 446
(2010/04/02)
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- Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones
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A new series of 3-(benzylideneamino)-2-phenylquinazoline-4(3H)-ones were prepared through Schiff base formation of 3-amino-2-phenyl quinazoline-4(3)H-one with various substituted carbonyl compounds. Their chemical structures were elucidated by spectral st
- Kumar, Krishnan Suresh,Ganguly, Swastika,Veerasamy, Ravichandran,De Clercq, Erik
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body text
p. 5474 - 5479
(2010/12/20)
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- Synthesis of phthalimido or succinimido[2-aryl-4-oxo-3-{2-phenyl-4(3H)- quinazolinon-3-yl}-1,3-thiazolidin-5-yl]ethanoate
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Treatment of benzoxazine 1 with hydrazine hydrate in ethanol furnished 3-amino-2-phenylquinazolin-4-(3H)-one 2, which upon condensation with aldehydes 3a-d yielded the corresponding 3-arylideneamino derivatives 4a-d. Cyclization of these derivatives using
- Sharma, Shweta,Sharma, Chirag,Thadhaney, Bhawana,Talesara
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experimental part
p. 397 - 401
(2010/05/19)
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- Heterocyclization of some chalcones to isoxazoles, pyrazoles and pyrimidine nuclei under microwave irradiation and their biological profile
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Rapid and efficient methods for the preparation of a set of isoxazole, pyrazole and pyrimidine derivatives of imidazolinone and quinazolinone by the reaction of 5-substituted arylidene-{2-(imidazolyl/quinazolyI)imino} thiazolidinone (chalcones) with hydro
- Vyas, Ritu,Swarnkar, Neelam,Sancheti, Abhilasha,Verdia, Jitendra,Punjabi
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experimental part
p. 1217 - 1226
(2010/02/28)
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- Synthesis and antiviral bioactivities of 2-aryl- or 2-methyl-3- (substituted- benzalamino)-4(3H)-quinazolinone derivatives
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A simple and general method has been developed for the synthesis of various 4(3H)-quinazolinone derivatives by the treatment of the appropriate 3-amino-2-aryl-4(3H)-quinazolinone with a substituted benzaldehyde in ethanol. The structures of the compounds were characterized by elemental analysis, IR, 1H-NMR and 13C-NMR spectra. The title 2-aryl- or 2-methyl-3-(substituted-benzalamino)-4(3H)-quinazolinone compounds III-1-III-31 were found to possess moderate to good antiviral activity. Semi-quantitative PCR and Real Time PCR assays were used to ascertain the target of action of compound III-31 against TMV. The studies suggest that III-31 possesses antiviral activity due to induction of up-regulation of PR-1a and PR-5, thereby inhibiting virus proliferation and movement by enhancement of the activity of some defensive enzyme.
- Gao, Xingwen,Cai, Xuejian,Yan, Kai,Song, Baoan,Gao, Lili,Chen, Zhuo
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p. 2621 - 2642
(2008/03/18)
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- Synthesis and antimicrobial activities of some novel substituted 2-imidazolyl-N-(4-oxo-quinazolin-3(4H)-yl)-acetamides
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Several substituted-quinazolin-3(4H)-ones 8-11ad were synthesized by condensation of 2-chloro-N-(4-oxosubstituted-quinazolin-3(4H)-yl)-acetamides with various substituted imidazoles through one pot reaction. Elemental analysis, IR, 1H-NMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antitubercular, antibacterial and antifungal activities. Some of the tested compounds showed good antitubercular activity. None of the synthesized compounds showed significant antibacterial and antifungal activity.
- Raghavendra, Nulgulmnalli Manjunathiah,Thampi, Parameshwaran,Gurubasavarajaswamy, Purvarga Mattada,Sriram, Dharmarajan
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p. 1615 - 1619
(2008/09/19)
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- Synthesis and biological properties of 4-(3H)-quinazolone derivatives
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A new quinazolone series has been designed, and synthesized by the anthranilic acid and different acid derivatives. Their structures have been elucidated on the basis of elemental analyses and spectral studies (IR, 1H NMR, FT-IR and FAB-MS). A
- Tiwari, Anjani K.,Singh, Vinay Kumar,Bajpai, Aruna,Shukla, Gauri,Singh, Sweta,Mishra, Anil K.
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p. 1234 - 1238
(2008/03/17)
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- Synthesis, antitubercular and anticancer activities of substituted furyl-quinazolin-3(4H)-ones
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Some novel substituted-3-{[(1E)-(substituted-2-furyl)-methylene]amino} quinazolin-4(3H)-one (5, 6, 7) a-f were synthesized by a multi-step process. These synthesized compounds are characterized by various spectroscopic techniques and evaluated for their antitubercular and anticancer activities. Biological activity indicated that some of the title compounds are potent antitubercular and anticancer agents.
- Raghavendra, Nulgulmnalli M.,Thampi, Parameshwaran,Gurubasavarajaswamy, Purvarga M.,Sriram, Dharmarajan
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p. 635 - 641
(2008/12/21)
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- Quinazolin-4-one derivatives
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A medicament having an inhibitory activity against hematopoietic prostaglandin D2 synthase, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein X represents a group represented by the formula —N═C(R5)— or the formula —NH—CH(R5)—, R1, R2, R3, and R4 represent a hydrogen atom, a halogen atom, a C1 to C6 alkyl group, or a hydroxy group, R5 represents a C1 to C6 alkyl group or a C6 to C10 aryl group, and R represents an amino group.
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Page/Page column 25
(2010/11/24)
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- Synthesis and pharmacological investigation of some novel 2,3-disubstituted quinazolin-4(3H)-ones as analgesic and antiinflammatory agents
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A series of novel 2-substituted quinazolin-4(3H)-ones have been synthesized by condensing the aromatic primary amine of 2-substituted quinazolines with different aldehydes and ketones. The synthesized compounds were confirmed by their spectral data (IR, N
- Alagarsamy,Meena,Vijayakumar,Ramseshu,Revathi
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p. 233 - 236
(2007/10/03)
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- Synthesis of some new benzoxazine derivatives of biological interest
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The synthesis of a number of biologically important imino-quinazolones has been achieved by the condensation of 3-amino-2-aryl-4-quinazolone and aromatic aldehydes.
- Verma, Manjusha,Singh, Sundaram,Singh
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p. 499 - 502
(2007/10/03)
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- Synthesis and pharmacological investigation of some novel 2-phenyl-3-(substituted methyl amino) quinazolin-4(3h)-ones as h1-receptor blockers
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A series of 2-phenyl-3 -(substituted methyl amino) quinazolin-4(3H)-ones were synthesized from 3-amino-2-phenyl quina-zolin-4(3H)-one. Their structures were confirmed by spectral data (IR, NMR, and MS) and the purity was ascertained by microanalysis. When
- Alagarsamy,Venkatesaperumal,Vijayakumar,Angayarkanni,Pounammal,Senthilganesh,Kandeeban
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p. 306 - 307
(2007/10/03)
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- Synthesis, analgesic, anti-inflammatory and antibacterial activities of some novel 2-phenyl-3-substituted quinazolin-4(3H) ones.
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A series of novel 2-phenyl-3-substituted quinazolin-4(3H)-ones have been synthesized by treating methyl-N-(2-phenyl quinazolin-3-yl-4(3H)-one) dithiocarbamate with different amines, the starting material dithiocarbamate was synthesized from anthranilic ac
- Alagarsamy, Veerachamy,Salomon, Viswas Raja,Vanikavitha, Gnanavel,Paluchamy, Veeran,Chandran, Muniyandi Ravi,Sujin, Augustin Arnald,Thangathiruppathy, Arunachalam,Amuthalakshmi, Sivaperuman,Revathi, Rajappan
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p. 1432 - 1435
(2007/10/03)
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- Kinetics of hydrolysis of 2-methyl/ phenyl-3-(2′-hydroxybenzalamino)quinazolin-4(3H)-one
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Kinetics of hydrolysis of 2-methyl-3-(2′-hydroxybenzalamino)quinazolin-4(3H)-one (MHBQ) and 2-phenyl-3-(2′-hydroxybenzalamino)quinazolin-4(3H)-one (PHBQ) have been studied. Rate coefficients have been measured for the alkaline hydrolysis of MHBQ and PHBQ in 70% (v/v) dioxane-water at various temperatures. The enthalpies and entropies of activation have been evaluated. The hydrolysis of MHBQ and PHBQ follows first order kinetics in both the substrate and the base. The relative rates of hydrolysis and activation parameters have been used to suggest the mechanism of the reactions.
- Laxma Reddy,Upender,Adinarayana Reddy
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p. 712 - 715
(2007/10/03)
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