Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones

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	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
刊名	MOLECULES
	2016
卷号	21 期号:12 页码:-
关键词	benzo[d][1,3]oxazin-4-one aroylhydrazides N-acylhydrazones hydrazones benzylidene hydrazides phospholipases proteases antimicrobial evaluation molecular docking
ISSN号	1420-3049
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.
英文摘要	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.
收录类别	SCI
语种	英语
WOS记录号	WOS:000392140100058
内容类型	期刊论文
源URL	[http://ir.sinap.ac.cn/handle/331007/26647]
专题	上海应用物理研究所_中科院上海应用物理研究所2011-2017年
推荐引用方式 GB/T 7714	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.,...&Ben Bacha, A.(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):-.