Synthesis, Antiphospholipase A2, Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones

مقال فى مجلة
El-Sayed, Nahed N. E. . 2016
نوع عمل المنشور
Research
رابط النشر على الانترنت
وسوم
benzo[d][1,3]oxazin-4-one, aroylhydrazide, N-acylhydrazones, hydrazones, benzylidene hydrazides
مجلة/صحيفة
Molecules
رقم الانشاء
12
رقم المجلد
21
الصفحات
1664
تاريخ المؤتمر
ملخص المنشورات

Some novel hydrazone derivatives 6ao were synthesized from the key intermediate 4-Chloro-N-(2-hydrazinocarbonyl-phenyl)-benzamide 5 and characterized using IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The inhibitory potential against two secretory phospholipase A2 (sPLA2), 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; 6a6m, and 6o against P. aeruginosa6a6b6d6f6l6m6n, and 6oagainst Serratia6k against S. mutans; and compounds 6a6d6e6m, and 6n against E. feacalis. The docking simulations of hydrazones 6ao with GIIA sPLA2, proteinase K and hydrazones 6ae with glutamine-fructose-6-phosphate transaminase were performed to obtain information regarding the mechanism of action.

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