- Quinazoline clubbed 1,3,5-triazine derivatives as VEGFR2 kinase inhibitors: design, synthesis, docking, in vitro cytotoxicity and in ovo antiangiogenic activity
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Abstract: A series of quinazoline clubbed 1,3,5-triazine derivatives (QCT) were synthesized and evaluated for their in vitro anticancer activity against HeLa (human cervical cancer), MCF-7 (human breast cancer cell), HL-60 (human promyelocytic leukemia cell), HepG2 (human Hepatocellular carcinoma cell), and one normal cell line HFF (human foreskin fibroblasts). In vitro assay result encouraged to further move towards in ovo anticancer evaluation using chick embryo. The series of QCT derivatives showed higher anticancer and antiangiogenic activity against HeLa and MCF-7 cell lines. In the series, synthetic molecule 8d, 8l, and 8m displayed significant activity. Further, these results substantiated by docking study on VGFR2. SAR study concluded that the potency of drugs depends on the nature of aliphatic substitution and the heterocyclic ring system. Graphical Abstract: [Figure not available: see fulltext.]
- Pathak, Prateek,Shukla, Parjanya Kumar,Kumar, Vikas,Kumar, Ankit,Verma, Amita
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- Synthesis, antiviral and cytotoxic activity of 6-bromo-2,3-disubstituted-4(3H)-quinazolinones.
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In the present study, a series of 6-bromo-2,3-disubstitued-4(3H)-quinazolinones was synthesized by condensation of 6-bromo-2-substituted-benzoxazin-4-one with trimethoprim, pyrimethamine and lamotrigine. The chemical structures of the synthesized compound
- Dinakaran, Murugesan,Selvam, Periyaswamy,DeClercq, Erik,Sridhar, Seshaiah Krishnan
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- Quinazoline based 1,3,5-triazine derivatives as cancer inhibitors by impeding the phosphorylated RET tyrosine kinase pathway: Design, synthesis, docking, and QSAR study
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The present research focused on designing a quinazoline skeleton, framed via 1,3,5-triazine derivatives (QBT) through field mapping and alignment studies. The QBT derivatives were synthesized via time- and cost-effective protocol. The 3D-QSAR study, computational physicochemical properties, and ADME calculation of the derivatives were performed to establish the affinity towards the biological system. Molecular docking in the adenosine triphosphate binding site of the RET tyrosine kinase domain (PDB ID: 7IVU) was studied to elucidate vital structural residues necessary for bioactivity. The derivatives were evaluated for anticancer potency against TPC-1 cells (thyroid cancer), MCF-7 cells (breast cancer), and one normal cell line (human foreskin fibroblasts) via 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay followed by an in ovo CAM assay. The entire series of derivatives (8a–o) showed mild to significant anticancer potency against the selected cancer cell lines.
- Pathak, Prateek,Naumovich, Vladislav,Grishina, Maria,Shukla, Parjanya Kumar,Verma, Amita,Potemkin, Vladimir
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- Atroposelective Desymmetrization of Resorcinol-Bearing Quinazolinones via Cu-Catalyzed C–O Bond Formation
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Enantioselective Cu-catalyzed C–O cross coupling reactions yielding atropisomeric resorcinol-bearing quinazolinones have been developed. Utilizing a new guanidinylated dimeric peptidic ligand, a set of products were generated in good yields with excellent
- Galls, Alexandra,Miller, Scott J.,Rozema, Soren D.,Yoon, Hyung
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supporting information
p. 762 - 766
(2022/01/28)
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- Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
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Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstrated cell viabilities of 65.9 and 42.7% respectively. The IC50 values of 15d were ~20?μg/ml. Assessment of apoptotic activity revealed that 15d decreased the cell viability by down regulating Bcl2 and BclxL. Moreover, compounds, 8j, 8d/15a/15e, 5b, and 8f displayed lowered IC50 values than oleanolic acid against proinflammatory isoforms of hGV, hG-X, NmPLA2, and AmPLA2. In addition, 8d, 8h, 8j, 15a, 15b, 15e, and 15f showed better anti-α-amylase than quercetin, whereas 8g, 8h, and 8i showed higher anti-α-glucosidase activity than allopurinol. Thus, these compounds can be considered as potential antidiabetic agents. Finally, none of the compounds showed higher antiproteases or xanthine oxidase activities than the used reference drugs.
- El-Sayed, Nahed N. E.,Almaneai, Norah M.,Ben Bacha, Abir,Al-Obeed, Omar,Ahmad, Rehan,Abdulla, Maha,Alafeefy, Ahmed M.
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p. 672 - 683
(2019/04/02)
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- Synthesis and evaluation of new quinazolin-4(3H)-one derivatives as potent antibacterial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis
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Staphylococcus aureus and Mycobacterium tuberculosis are major causative agents responsible for serious nosocomial and community-acquired infections impacting healthcare systems globally. Over several decades, these pathogens have developed resistance to multiple antibiotics significantly affecting morbidity and mortality. Thus, these recalcitrant pathogens are amongst the most formidable microbial pathogens for which international healthcare agencies have mandated active identification and development of new antibacterial agents for chemotherapeutic intervention. In our present work, a series of new quinazolin-4(3H)-one derivatives were designed, synthesized and evaluated for their antibacterial activity against ESKAP pathogens and pathogenic mycobacteria. The experiments revealed that 4'c, 4'e, 4'f and 4'h displayed selective and potent inhibitory activity against Staphylococcus aureus with MIC values ranging from 0.03-0.25 μg/mL. Furthermore, compounds 4'c and 4'e were found to be benign to Vero cells (CC50 = >5 μg/mL) and displayed promising selectivity index (SI) > 167 and > 83.4 respectively. Additionally, 4'c and 4'e demonstrated equipotent MIC against multiple drug-resistant strains of S. aureus including VRSA, concentration dependent bactericidal activity against S. aureus and synergized with FDA approved drugs. Moreover, compound 4′c exhibited more potent activity in reducing the biofilm and exhibited a PAE of ~2 h at 10X MIC which is comparable to levofloxacin and vancomycin. In vivo efficacy of 4'c in murine neutropenic thigh infection model revealed that 4'c caused a similar reduction in cfu as vancomycin. Gratifyingly, compounds 4d, 4e, 9a, 9b, 14a, 4'e and 4'f also exhibited anti-mycobacterial activity with MIC values in the range of 2-16 μg/mL. In addition, the compounds were found to be less toxic to Vero cells (CC50 = 12.5->100 μg/mL), thus displaying a favourable selectivity index. The interesting results obtained here suggest the potential utilization of these new quinazolin-4(3H)-one derivatives as promising antibacterial agents for treating MDR-Staphylococcal and mycobacterial infections.
- Gatadi, Srikanth,Gour, Jitendra,Shukla, Manjulika,Kaul, Grace,Dasgupta, Arunava,Madhavi,Chopra, Sidharth,Nanduri, Srinivas
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p. 287 - 308
(2019/05/15)
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- Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases
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Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20–30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as novel potent inhibitors of the FLT3-ITD and FLT3-D835Y kinases. Their prominent effects were confirmed by biochemical and cellular proliferation assays followed by mice xenograft studies. Our modelling experiments and the chemical structures of the compounds predict the possibility of covalent inhibition. The most effective compounds triggered apoptosis in FLT3-ITD AML cells but had either weak or no effect in FLT3-independent leukemic and non-leukemic cell lines. Our results strongly suggest that our compounds may become therapeutics in relapsing and refractory AML disease harboring various ITD and tyrosine kinase domain mutations, by their ability to overcome drug resistance.
- Baska, Ferenc,Sipos, Anna,?rfi, Zoltán,Nemes, Zoltán,Dobos, Judit,Szántai-Kis, Csaba,Szabó, Eszter,Szénási, Gábor,Dézsi, László,Hamar, Péter,Cserepes, Mihály T.,Tóvári, József,Garamv?lgyi, Rita,Krekó, Marcell,?rfi, László
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supporting information
(2019/10/16)
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- Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials
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We recently reported on the discovery of a novel antibacterial (2) with a 4(3H)-quinazolinone core. This discovery was made by in silico screening of 1.2 million compounds for binding to a penicillin-binding protein and the subsequent demonstration of antibacterial activity against Staphylococcus aureus. The first structure-activity relationship for this antibacterial scaffold is explored in this report with evaluation of 77 variants of the structural class. Eleven promising compounds were further evaluated for in vitro toxicity, pharmacokinetics, and efficacy in a mouse peritonitis model of infection, which led to the discovery of compound 27. This new quinazolinone has potent activity against methicillin-resistant (MRSA) strains, low clearance, oral bioavailability and shows efficacy in a mouse neutropenic thigh infection model.
- Bouley, Renee,Ding, Derong,Peng, Zhihong,Bastian, Maria,Lastochkin, Elena,Song, Wei,Suckow, Mark A.,Schroeder, Valerie A.,Wolter, William R.,Mobashery, Shahriar,Chang, Mayland
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p. 5011 - 5021
(2016/06/13)
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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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- Reactivity of 2-methyl-4H-3,1-benzoxazin-4-ones and 2-methyl-4H-pyrido[2,3- d][1,3]oxazin-4-one under microwave irradiation conditions
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The reactivity of variably substituted 2-methyl-4H-3,1-benzoxazin-4-ones and 2-methyl-4H-pyrido[2,3-d][1,3]oxazin-4-one towards carbon and oxygen nucleophiles under microwave irradiation conditions was investigated. Optimization of the reaction conditions of oxazinones with carbon nucleophiles led to the synthesis of a series of 4-hydroxy-quinolin-2-ones and 4-hydroxy-1,8-naphthyridin-2-ones in high yields, whereas reaction with a variety of alcohols proceeded smoothly to the formation of the corresponding N-acetyl-anthranilates and nicotinates.
- Prousis, Kyriakos C.,Tzani, Andromachi,Avlonitis, Nicolaos,Calogeropoulou, Theodora,Detsi, Anastasia
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p. 1313 - 1321
(2014/01/06)
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- Quinazolin-4-one derivatives: A novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate receptor antagonists
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We describe a new class of subunit-selective antagonists of N-methyl d-aspartate (NMDA)-selective ionotropic glutamate receptors that contain the (E)-3-phenyl-2-styrylquinazolin-4(3H)-one backbone. The inhibition of recombinant NMDA receptor function induced by these quinazolin-4-one derivatives is noncompetitive and voltage-independent, suggesting that this family of compounds does not exert action on the agonist binding site of the receptor or block the channel pore. The compounds described here resemble CP-465,022 ((S)-3-(2-chlorophenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl] -6-fluoro-3H-quinazolin-4-one), a noncompetitive antagonist of AMPA-selective glutamate receptors. However, modification of ring substituents resulted in analogues with greater than 100-fold selectivity for recombinant NMDA receptors over AMPA and kainate receptors. Furthermore, within this series of compounds, analogues were identified with 50-fold selectivity for recombinant NR2C/D-containing receptors over NR2A/B containing receptors. These compounds represent a new class of noncompetitive subunit-selective NMDA receptor antagonists.
- Mosley, Cara A.,Acker, Timothy M.,Hansen, Kasper B.,Mullasseril, Praseeda,Andersen, Karen T.,Le, Phuong,Vellano, Kimberly M.,Br?uner-Osborne, Hans,Liotta, Dennis C.,Traynelis, Stephen F.
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supporting information; experimental part
p. 5476 - 5490
(2010/11/16)
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- Synthesis and evaluation of novel 2-substituted-quinazolin-4(3H)-ones as potent analgesic and anti-inflammatory agents
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A novel series of 2-substituted-quinazolin-4(3H)-ones were synthesized by reacting 3,5-disubstituted-anthranilic acid with acetic anhydride/benzoyl chloride, which were further reacted with different primary amines to obtain 2,6,8-substituted-quinazolin-4(3H)-ones 6a-f, 7, 8. All the synthesized compounds were characterized and screened for analgesic and anti-inflammatory activities. Compounds 6,8-dibromo-2-phenyl-3-(4′-carboxyl phenyl)quinazolin-4(3H)-one 7 and 6,8-dibromo-2-phenyl-3-(2′- phenylethanoic acid)quinazolin-4(3H)-one 8 displayed good analgesic and anti-inflammatory activity in comparison to the reference standards acetyl salicylic acid and indomethacin, respectively.
- Rather, Bilal Ahmad,Raj, Tilak,Reddy, Aravind,Ishar, Mohan Paul S.,Sivakumar, Samitha,Paneerselvam, Perumal
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experimental part
p. 108 - 113
(2010/07/04)
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- BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
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The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.
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Page/Page column 136-137
(2009/12/27)
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- New vistas in quinoline synthesis
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The gold-catalyzed Friedlander reaction was applied to the condensation of 2-aminoarylketones with β-keto-esters, β-diketones, β-keto-amides, and β-keto-sulfones to afford a diverse range of 2,3,4-trisubstituted quinolines in 3-82% yield. The seven-membered rings 1,3-cycloheptadione and azepane-2,4-dione reacted smoothly in 75% yield. An alternative procedure for the synthesis of 3-(methanesulfonyl)quinolines was developed and provided an entry into late stage manipulation of the 4-position of these quinolines. The requisite 2-aminoarylketones for the Friedlander reaction were prepared in one pot by modified Sugasawa reaction using gallium(III) chloride and boron(III) chloride in 12-54% yield.
- Atechian, Sarkis,Nock, Nadine,Norcross, Roger D.,Ratni, Hassen,Thomas, Andrew W.,Verron, Julien,Masciadri, Raffaello
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p. 2811 - 2823
(2007/10/03)
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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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- 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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- 3-Methanesulfonylquinolines as GABAB enhancers
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The present invention relates to compounds of formula I wherein R1, R2 and R3 are as defined in the specification, which are active at the GABAB receptor and which can be used for the treatment of CNS disorders.
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Page/Page column 9
(2010/11/25)
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- NOVEL FUSED TRIAZOLONES AND THE USES THEREOF
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This invention relates to novel compounds having the structural diagram (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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- SUBSTITUTED HETEROARYLS AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES
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Disclosed are compounds and pharmaceutically acceptable salts of formula (I), which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
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- Synthesis and anti-inflammatory, analgesic, ulcerogenic and cyclooxygenase activities of novel quinazolinyl-Δ2-pyrazolines
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Synthesis of 2-(ω -chloroacetonyl)-3-substituted-phenyl-6-halo/6,8-dihaloquinazolin-4(3H)-ones 6-10, 2-(ω -hydrazinoacetonyl)-3-substituted-phenyl-6-halo/6,8-dihaloquinazolin-4(3H)ones 11-15 and 1′ -[3H-3-substituted-phenyl-4-oxo-6-halo/6,8-dihaloquinazolin-2-acetonyl] -3′-aryl-5′-(2-substituted-indol-3-yl)-Δ 2-pyrazolines 16-30 have been described. All the compounds have been tested in vivo for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity.
- Kumar, Ashok,Sharma, Shalabh,Bajaj, Kiran,Bansal, Deepti,Sharma, Shipra,Saxena, Archana K. K.,Lata,Gupta,Srivastava
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p. 1979 - 1984
(2007/10/03)
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- Thiazolidinyl-triazinoquinazolines as potent anti-inflammatory agents
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Some new 5-(5′-substituted-aryl-2′-oxo-4′ -thiazolidin-1′-yl)amino-4-phenyl-2-methyl-10-bromo-[1,2,4] triazino[2,3c]quinazolines have been synthesized by [1,5]cyclocondensation of thiolactic acid with 5-arylidene hydrazino-4-phenyl-2methyl-10-bromo-[1,2,4] triazino [2,3-c] quinazolines. All the compounds of the series have been screened for their anti-inflammatory activity. The most potent compound of the series 5-(5′-p-dimethylaminophenyl-2′-oxo-4′-thiazolidin-1 ′yl)amino-4-phenyl-2-methyl-10-bromo-[1,2,4] triazino[2,3-c]quinazolines has shown 48.93% activity at a dose of 50 mg/kg p.o. The structures of the products have been delineated by chemical reactions, elemental analysis and spectral studies.
- Bansal, Ekta,Ram, Tilak,Sharma, Shalabh,Tyagi, Mirdula,Rani, Archana Preeti,Bajaj, Kiran,Tyagi, Ritu,Goel, Bhawna,Srivastava,Guru,Kumar, Ashok
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p. 307 - 312
(2007/10/03)
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- Atropisomeric quinazolin-4-one derivatives are potent noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists
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Piriqualone (1) was found to be an antagonist of AMPA receptors. Structure-activity optimization was conducted on each of the three rings in 1 to afford a series of potent and selective antagonists. The sterically crowded environment surrounding the N-3 aryl group provided sufficient thermal stability for atropisomers to be isolated. Separation of these atropisomers resulted in the identification of (+)-38 (CP-465,022), a compound that binds to the AMPA receptor with high affinity (IC50 = 36 nM) and displays potent anticonvulsant activity.
- Welch,Ewing,Huang,Menniti,Pagnozzi,Kelly,Seymour,Guanowsky,Guhan,Guinn,Critchett,Lazzaro,Ganong,DeVries,Staigers,Chenard
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p. 177 - 181
(2007/10/03)
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- Quinazolineacetic Acids and Related Analogues as Aldose Reductase Inhibitors
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A variety of 2,4-dioxoquinazolineacetic acids (10, 11) were synthesized as hybrids of the known aldose reductase inhibitors alrestatine (8), ICI-105,552 (9), and ICI-128,436 (2) and evaluated for their ability to inhibit partially purified bovine lens aldose reductase (in vitro) and their effectiveness to decrease galactitol accumulation in the 4-day galactosemic rat model (in vivo).In support to SAR studies, related analogues pyrimidinediones (12), dihydroquinazolones (13), and indazolidinones (14, 15) were synthesized and tested in the in vitro and in vivo assays.All prepared compounds (10-15) have shown a high level of in vitro activity (IC50 ca. 10-6 to 4 10-8 M).However, only the 2,4-quinazolinedione analogues 10 and 11, with similar N-aralkyl substitution found in 2 and 9, have exhibited good oral potency.The remaining compounds were either inactive or had only a marginal in vivo activity.The structure-activity data support the presence of a secondary hydrophobic pocket in the vicinity of the primary lipophilic region of the enzyme.
- Malamas, Michael S.,Millen, Jane
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p. 1492 - 1503
(2007/10/02)
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- The Synthesis of Benzofuroquinolines. VIII. Some Halobenzofuroquinoline Derivatives
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Three 2-halo-6(5H)-benzofuroquinolinones 1 (X = F, Cl, Br) were synthesized in two procedures, photocyclization of N-benzyl-N-(p-halophenyl)-2-benzofurancarboxamides 3 (X = F, Cl, Br) and condensation of 2-amino-2'-hydroxybenzophenones 7 (X = F, Cl
- Yamaguchi, Seiji,Yokoi, Takashi,Yamada, Minoru,Arai, Hitomi,Uchiuzo, Yasuto,Kawase, Yoshiyuki
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p. 1003 - 1005
(2007/10/02)
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- Synthesis of Quinazolinylpyrimidinediones and Their Anti-inflammatory Activity
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Hexahydro-1--3-aryl-2-thioxopyrimidine-4,6-diones (IV) have been prepared and converted into hexahydro-1--3-aryl-5-benzyliden-2-thioxopyrimidine-4,6-diones (V) and hexahydro-1-2-alkyl-4(
- Kumar, Atul,Singh, S.,Saxena, A. K.,Shanker, K.
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p. 443 - 447
(2007/10/02)
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- Synthesis and Pharmacological Activity of Some New 4(3H)-Quinazolone Derivatives
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New derivatives of 2-methyl-4(3H)-quinazolone have been prepared and their structures assigned on the basis of IR, PMR and mass spectra.Some of them show CNS depressant activity.
- Ossman, Abdel Rahman El Nasser,Safwat, H. M.,Aziza, Mohsen A.
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p. 333 - 335
(2007/10/02)
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- Synthesis of Some 6-Bromo-3-- and 2-Styryl-3--4(3H)-quinazolinones
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Some substituted 6-bromo-3--4(3H)-quinazolinones have been synthesized under the conditions of the Mannich reaction.In addition, a few unsubstituted and substituted 2-styryl-4(3H)-quinazolinones, 6-bromo-2-styryl-4(3H)-quinazolinones, and 6-bromo-2-styryl-3--4(3H)-quinazolinones have also been synthesized by condensing the corresponding 2-methyl derivative with an appropriate aromatic aldehyde.Representative compounds have been screened for their central neural system and antiviral activity.
- Varma, Rajendra S.,Bahadur, Surendra,Agnihotri, Anil K.
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p. 103 - 104
(2007/10/02)
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