- Synthesis, characterization, in vitro cholinesterase and hRBCs hemolysis assay and computational evaluation of novel 2,3,4,5-tetrahydrobenzothiazepine appended α-aminophosphonates
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A series of novel 2,3,4,5-tetrahydrobenzothiazepine appended α-aminophosphonate derivatives were synthesized by subjecting 2,3-dihydrobenzothiazepine to Pudovik reaction using diethyl phosphite. Tested derivatives exhibited better AChE inhibition (0.86–12
- Shaikh, Sarfaraz,Dhavan, Pratik,Uparkar, Jasmin,Singh, Pinky,Vaidya,Jadhav,Ramana
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- Discovery of Novel Approach for Regioselective Synthesis of Thioxotriaza-Spiro Derivatives via Oxalic Acid
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A vital approach for the synthesis of a range of novel thioxotriaza-spiro derivatives is described. These new heterocyclic systems are obtained via oxalic acid catalyzed reaction of α,β-unsaturated ketones in the presence of 5,6-diamino-2-mercaptopyrimidi
- Gopinatha, Vindya K.,Mantelingu, Kempegowda,Raghavan, Sathees C.,Rangappa, Kanchugarakoppal S.,Swarup, Hassan A.
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supporting information
p. 2004 - 2009
(2019/10/28)
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- Naphtho[2,3-: B] furan-4,9-dione synthesis via palladium-catalyzed reverse hydrogenolysis
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A reverse hydrogenolysis process has been developed for two-site coupling of 2-hydroxy-1,4-naphthoquinones with olefins to produce naphtha[2,3-b]furan-4,9-diones and hydrogen (H2). The reaction is catalyzed by commercially available Pd/C without oxidants and hydrogen acceptors, thereby providing an intrinsically waste-free approach for the synthesis of functionalized and potentially biologically relevant naphtha[2,3-b]furan-4,9-diones.
- Li, Jimei,Zhang, Jie,Li, Mingfei,Zhang, Chenyang,Yuan, Yongkun,Liu, Renhua
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supporting information
p. 2348 - 2351
(2019/02/27)
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- An improved synthesis of pyrido[2,3-: D] pyrimidin-4(1 H)-ones and their antimicrobial activity
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The screening of a small library of diverse chemical structures resulted in the identification of 2-thioxodihydropyrido[2,3-d]pyrimidine 10a as having broad spectrum antibacterial activity (MIC 0.49-3.9 μg mL-1), and reasonable antifungal activity (MIC 31.25 μg mL-1). An expeditious synthesis of 10a was optimized by varying solvents, catalysts and the use of microwave irradiation with the best conditions using DMF as a solvent, I2 (10 mol%) and a 30 minutes reaction time compared to 15 h for classic conventional heating. The pharmacokinetic properties and calculation of drug likeness of 10a suggested good traditional drug-like properties and led to the synthesis of a small library with seven compounds 10a and 10d-i showing broad antimicrobial activity (MIC = 0.49-7.81 μg mL-1) and selectivity indices of more than 5.6 against the normal colon cell line (CCD-33Co). The antifungal activity of compounds 10d-i was moderate to strong with MIC values of 1.95-15.63 μg mL-1.
- Fares, Mohamed,Abd El Hadi, Soha R.,Eladwy, Radwa A.,Shoun, Aly A.,Abdel-Aziz, Marwa M.,Eldehna, Wagdy M.,Abdel-Aziz, Hatem A.,Keller, Paul A.
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supporting information
p. 3389 - 3395
(2018/05/23)
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- Synthesis of stable benzimidazole derivatives bearing pyrazole as anticancer and EGFR receptor inhibitors
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A new series of benzimidazole linked pyrazole derivatives were synthesized by cyclocondensation reaction through one-pot multicomponent reaction in absolute ethanol. All the synthesized compounds were tested for their in vitro anticancer activities on fiv
- Akhtar, Md. Jawaid,Khan, Ahsan Ahmed,Ali, Zulphikar,Dewangan, Rikeshwer Prasad,Rafi, Md.,Hassan, Md. Quamrul,Akhtar, Md. Sayeed,Siddiqui, Anees Ahmad,Partap, Sangh,Pasha, Santosh,Yar, M. Shahar
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p. 158 - 169
(2018/03/24)
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- Synthesis and cytotoxic activities of some pyrazoline derivatives bearing phenyl pyridazine core as new apoptosis inducers
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The cyclization of chalcones 3a-3u with 3-hydrazinyl-6-phenylpyridazine 7 under basic condition led to the formation of new pyrazoline derivatives 8a-8u. All final compounds were characterized by spectral and elemental analyses. They were screened for their antiproliferative activities against A549 (lung), HepG-2 (liver), CaCo-2 (intestinal) and MCF-7 (breast) cancer cell lines. Some of the synthesized compounds exhibited promising antiproliferative activities especially compound 8k with IC50values of 8.33, 1.67 and 10?μM against HepG-2, MCF-7 and CaCo-2 cancer cell lines, respectively. Moreover, their antiproliferative activity was due to apoptosis rather than necrosis induction except compound 8h which exhibited equal apoptotic and necrotic properties. Compound 8k showed 5 fold increase in caspase-3 activity indicating that the apoptosis proceeds via caspase-3 activation.
- George, Riham F.,Fouad, Marwa A.,Gomaa, Iman E.O.
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- Novel benzothiazole based sulfonylureas/sulfonylthioureas: Design, synthesis and evaluation of their antidiabetic potential
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In the present study, twenty-eight benzothiazole based sulfonylureas/sulfonylthioureas were synthesized and were assessed for their antidiabetic effect in a normoglycemic rat model by the in vivo oral glucose tolerance test (OGTT). All the synthesized com
- Kharbanda, Chetna,Alam, Mohammad Sarwar,Hamid, Hinna,Javed, Kalim,Bano, Sameena,Ali, Yakub,Dhulap, Abhijeet,Alam, Parwez,Pasha
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p. 6777 - 6786
(2016/08/10)
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- Monoamine Oxidase Inhibitory Activity: Methyl- versus Chlorochalcone Derivatives
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Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series
- Mathew, Bijo,U?ar, Gülberk,Mathew, Githa Elizabeth,Mathew, Sincy,Kalatharakkal Purapurath, Praseedha,Moolayil, Fasil,Mohan, Smrithy,Varghese Gupta, Sheeba
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p. 2649 - 2655
(2016/12/23)
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- Monitoring the DNA by ruthenium complexes of heterocyclic N,S-donor ligands and evaluation of biological activities
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Neutral N,S-donor bidentate ligands have been synthesized and characterized by NMR and IR spectroscopic techniques. The ligands have been used to synthesized ruthenium(II) complexes ([Ru(L1–L6)PPh3)2Cl2/su
- Karia, Parag S.,Vekariya, Pankajkumar A.,Patidar, Anshul P.,Patel, Ravi R.,Patel, Mohan N.
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p. 1903 - 1914
(2016/10/21)
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- DNA interaction and cytotoxic activities of square planar platinum(II) complexes with N, S-donor ligands
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The platinum(II) complexes with N, S-donor ligands have been synthesized and characterized by physicochemical methods viz. elemental, electronic, FT-IR, 1H NMR and LC-MS spectra. The binding mode and potency of the complexes with HS DNA (Herrin
- Patel, Mohan N.,Patel, Chintan R.,Joshi, Hardik N.,Thakor, Khyati P.
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supporting information
p. 261 - 267
(2014/04/03)
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- Cytotoxic, antibacterial and nucleic acid interaction studies of square planar palladium(II) complexes
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A series of substituted N, O-donor bidentate ligands(Ln) and their square planar mononuclear palladium(II) complexes of the type [PdCl 2(Ln)] were synthesized and characterized by elemental analysis, conductivity measureme
- Patel, Mohan N.,Patidar, Anshul P.,Karia, Parag S.,Vekariya, Pankaj A.
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- Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents
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The present study aims at the synthesis of pyrazolines bearing benzothiazole and their evaluation as anti-inflammatory agents. The synthesized compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model. Two co
- Kharbanda, Chetna,Alam, Mohammad Sarwar,Hamid, Hinna,Javed, Kalim,Bano, Sameena,Dhulap, Abhijeet,Ali, Yakub,Nazreen, Syed,Haider, Saqlain
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p. 5804 - 5812
(2015/02/02)
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- Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors
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A series of pyrazolyl-thiazolinone derivatives (E1-E36) have been designed and synthesized and their biological activities were also evaluated as potential EGFR and HER-2 kinase inhibitors. Thirty-four of the 36 compounds were reported for the first time. Among them, compound 2-(5-(4-bromophenyl)-3-p-tolyl-4,5- dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-one (E28) displayed the most potent inhibitory activity (IC50 = 0.24 μM for EGFR and IC50 = 1.07 μM for HER-2). Antiproliferative assay results indicated that compound E28 owned high antiproliferative activity against MCF-7, B16-F10 and HCT-116 in vitro, with IC50 value of 0.30, 0.54, and 0.70 μM, respectively. Docking simulation was further performed to position compound E28 into the EGFR active site to determine the probable binding model. Based on the preliminary results, compound E28 with potent inhibitory activity in tumor growth would be a potential anticancer agent.
- Qiu, Ke-Ming,Wang, Hai-Hong,Wang, Li-Ming,Luo, Yin,Yang, Xian-Hui,Wang, Xiao-Ming,Zhu, Hai-Liang
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experimental part
p. 2010 - 2018
(2012/05/04)
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- Design, synthesis, and biological evaluation of chalcone oxime derivatives as potential immunosuppressive agents
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A series of deoxybenzoin oximes were recently reported as potent immunosuppressive agents by our group. In order to continue the original research for potential immunosuppressive agents with high efficacy and low toxicity, we synthesized a series of new c
- Luo, Yin,Song, Ran,Li, Yao,Zhang, Shuai,Liu, Zhi-Jun,Fu, Jie,Zhu, Hai-Liang
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supporting information; experimental part
p. 3039 - 3043
(2012/06/04)
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- Cytotoxic, DNA interaction, SOD mimic, and antimicrobial activities of square pyramidal copper(II) complexes
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The copper(II) complexes with NS donor ligand and ciprofloxacin were synthesized. The synthesized complexes were characterized by physicochemical parameters like elemental and thermal analysis, electronic, FT-IR, and LC-MS spectroscopy. The complexes were
- Patel, Mohan N.,Patel, Chintan R.,Joshi, Hardik N.
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scheme or table
p. 1224 - 1232
(2012/08/13)
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- Synthesis and evaluation of human monoamine oxidase inhibitory activities of some 3,5-diaryl-N-substituted-4,5-dihydro-1H-pyrazole-1-carbothioamide derivatives
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Sixteen 3-aryl-5-(4-fluorophenyl)-N-substituted-4,5-dihydro-1H-pyrazole-1- carbothioamide derivatives were synthesized and their structure were identified by UV, IR, 1H NMR, mass spectra, and microanalyses. The compounds were evaluated in vitro for their human monoamine oxidase (hMAO) inhibitory activities and their MAO-A and -B selectivity. All the compounds were found to potently inhibit MAO-A isoforms. 5-(4-Fluorophenyl)-3-(4-methoxyphenyl)-N- methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide (1.0 × 10-3 μM) was found to inhibit hMAO-A most selectively and potently. The binding mode of 5-(4-fluorophenyl)-3-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole- 1-carbothioamide to hMAO-A was also predicted using docking studies.
- Sentuerk, Kerem,Tan, Oya Unsal,Ciftci, Samiye Yabanoglu,Ucar, Guelberk,Palaska, Erhan
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p. 695 - 702
(2012/11/07)
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- Synthesis and selective inhibitory activity against human COX-1 of novel 1-(4-substituted-thiazol-2-yl)-3,5-di(hetero)aryl-pyrazoline derivatives
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Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2-pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1-thiocarbamoyl-2- pyrazolines with the ethyl ester of α-bromo-pyruvic acid. The synthesized compounds were confirmed by spectroscopic data and assayed to evaluate their in vitro ability to inhibit both isoforms of human cyclooxygenase (hCOX). Some derivatives (compounds 5, 6, 13, 16, and 17) displayed promising selectivity against hCOX-1 in the micromolar range and were shown to have a selectivity index similar or better than the reference drugs (indometacin, diclofenac). The introduction of a phenyl or a 4-F-phenyl ring on the C5 associated with a 4-substituted phenyl or a heteroaryl group on the C3 of (4-substituted-thiazol- 2-yl)pyrazoline derivatives improved the activity against hCOX-1. Thanks to these preliminary results it could be possible to extend our knowledge of the pharmacophoric requirements for the discovery of new pyrazoline-based hCOX-1 inhibitors. Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2- pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1- thiocarbamoyl-2-pyrazolines with the ethyl ester of α-bromo-pyruvic acid. Some derivatives displayed promising selectivity against human cyclooxygenase 1 (hCOX-1) in the micromolar range, with a selectivity index similar or better than the reference drugs, indometacin and diclofenac. Copyright
- Carradori, Simone,Secci, Daniela,Bolasco, Adriana,De Monte, Celeste,Yá?ez, Matilde
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p. 973 - 979
(2013/02/23)
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- Highly efficient one-pot synthesis, antimicrobial and docking studies of newer β-amino carbonyl derivatives catalyzed by silica sulfuric acid
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Mannich reaction was applied between 4-fluorobezaldehyde, selected acetophenone and several anilines, catalyzed by silica sulfuric acid for the synthesis of β-amino carbonyl derivatives. Reaction time and yield of the products depended on the nature of ac
- El-Bayouki,Basyouni,El-Sayed,Tohamy,El-Henawy
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p. 255 - 268
(2013/01/15)
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- Synthesis of some novel benzofuran-2-yl(4,5-dihyro-3,5-substituted diphenylpyrazol-1-yl) methanones and studies on the antiproliferative effects and reversal of multidrug resistance of human MDR1-gene transfected mouse lymphoma cells in vitro
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A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.
- Parekh, Shrey,Bhavsar, Dhairya,Savant, Mahesh,Thakrar, Shailesh,Bavishi, Abhay,Parmar, Manisha,Vala, Hardevsinh,Radadiya, Ashish,Pandya, Nilay,Serly, Juliana,Molnár, Joseph,Shah, Anamik
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scheme or table
p. 1942 - 1948
(2011/04/26)
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- Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors
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Fatty acid biosynthesis is essential for bacterial survival. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and -negative bacteria. Fifty-six 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 1-(5-(4-fluorophenyl)- 3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (12) and 1-(5-(4-chlorophenyl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (13) were potent inhibitors of E. coli FabH.
- Lv, Peng-Cheng,Sun, Juan,Luo, Yin,Yang, Ying,Zhu, Hai-Liang
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scheme or table
p. 4657 - 4660
(2010/09/16)
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- Synthesis and characterization of some new 2-amino-4-(4′-substituted) -6-(4″-substituted)diphenyl pyrimidines
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Synthesis and characterization of some novel 2-amino-4-(4′- substituted)-6-(4″-substituted)diphenyl pyrimidines has been carried out by the conversion of variably substituted acetophenones and benzaldehydes into corresponding chalcones followed by cyclization with guanidine hydrochloride in the presence of an oxidizing agent.
- Hasan, Aurangzeb,Khaleeq, Musfirah,Riaz, Uzma
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scheme or table
p. 5581 - 5587
(2012/08/07)
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- Novel domino reactions of (Z,Z)-2,2'-thiobis(1,3-diarylprop-2-en-1-ones) with acetylacetone and ethyl acetoacetate: Stereoselective synthesis of highly functionalized dihydrofurans
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The domino reactions of (Z,Z)-2,2'-thiobis(1,3-diarylprop-2-en-1-ones) with acetylacetone and ethyl acetoacetate in the presence of sodium ethoxide afforded the corresponding 4,5-dihydrofurans stereoselectively in moderate yields presumably via a Michael
- Vinosha, Beer Mohamed,Renuga, Subbiah,Gnanadeebam, Michael,Perumal, Subbu,Lycka, Antonin
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experimental part
p. 2776 - 2788
(2009/12/06)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
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