Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones
El-Sayed, NNE; Alafeefy, AM; Bakht, MA; Masand, VH; Aldalbahi, A; Chen, N; Fan, CH; Ben Bacha, A; El-Sayed, NNE (reprint author), King Saud Univ, Girls Sect, Coll Sci, Dept Chem, POB 22452, Riyadh 11495, Saudi Arabia.; El-Sayed, NNE (reprint author), Natl Org Drug Control & Res, Giza 35521, Egypt.
2016
发表期刊MOLECULES
ISSN1420-3049
卷号21期号:12页码:-
文章类型期刊论文
摘要Some novel hydrazone derivatives 6a-o were synthesized from the key intermediate 4-Chloro-N-(2-hydrazinocarbonyl-phenyl)-benzamide 5 and characterized using IR, H-1-NMR, C-13-NMR, mass spectroscopy and elemental analysis. The inhibitory potential against two secretory phospholipase A(2) (sPLA(2)), three protease enzymes and eleven bacterial strains were evaluated. The results revealed that all compounds showed preferential inhibition towards hGIIA isoform of sPLA2 rather than DrG-IB with compounds 6l and 6e being the most active. The tested compounds exhibited excellent antiprotease activity against proteinase K and protease from Bacillus sp. with compound 6l being the most active against both enzymes. Furthermore, the maximum zones of inhibition against bacterial growth were exhibited by compounds; 6a, 6m, and 6o against P. aeruginosa; 6a, 6b, 6d, 6f, 6l, 6m, 6n, and 6o against Serratia; 6k against S. mutans; and compounds 6a, 6d, 6e, 6m, and 6n against E. feacalis. The docking simulations of hydrazones 6a-o with GIIA sPLA2, proteinase K and hydrazones 6a-e with glutamine-fructose-6-phosphate transaminase were performed to obtain information regarding the mechanism of action.
关键词Aroylhydrazides Benzo[d][1 N-acylhydrazones 3]Oxazin-4-one Hydrazones Benzylidene Hydrazides Phospholipases Proteases Antimicrobial Evaluation Molecular Docking
DOI10.3390/molecules21121664
收录类别SCI
语种英语
WOS记录号WOS:000392140100058
引用统计
文献类型期刊论文
条目标识符http://ir.sinap.ac.cn/handle/331007/26647
专题中科院上海应用物理研究所2011-2018年
通讯作者El-Sayed, NNE (reprint author), King Saud Univ, Girls Sect, Coll Sci, Dept Chem, POB 22452, Riyadh 11495, Saudi Arabia.; El-Sayed, NNE (reprint author), Natl Org Drug Control & Res, Giza 35521, Egypt.
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El-Sayed, NNE,Alafeefy, AM,Bakht, MA,et al. Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones[J]. MOLECULES,2016,21(12):-.
APA El-Sayed, NNE.,Alafeefy, AM.,Bakht, MA.,Masand, VH.,Aldalbahi, A.,...&El-Sayed, NNE .(2016).Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones.MOLECULES,21(12),-.
MLA El-Sayed, NNE,et al."Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones".MOLECULES 21.12(2016):-.
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