CAS OpenIR  > 中科院上海应用物理研究所2011-2018年
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
Source PublicationMOLECULES
ISSN1420-3049
Volume21Issue:12Pages:-
Subtype期刊论文
AbstractSome 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.
KeywordAroylhydrazides Benzo[d][1 N-acylhydrazones 3]Oxazin-4-one Hydrazones Benzylidene Hydrazides Phospholipases Proteases Antimicrobial Evaluation Molecular Docking
DOI10.3390/molecules21121664
Indexed BySCI
Language英语
WOS IDWOS:000392140100058
Citation statistics
Cited Times:3[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.sinap.ac.cn/handle/331007/26647
Collection中科院上海应用物理研究所2011-2018年
Corresponding AuthorEl-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.
Recommended Citation
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.,...&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):-.
Files in This Item: Download All
File Name/Size DocType Version Access License
Synthesis, Antiphosp(2164KB)期刊论文作者接受稿开放获取CC BY-NC-SAView Download
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[El-Sayed, NNE]'s Articles
[Alafeefy, AM]'s Articles
[Bakht, MA]'s Articles
Baidu academic
Similar articles in Baidu academic
[El-Sayed, NNE]'s Articles
[Alafeefy, AM]'s Articles
[Bakht, MA]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[El-Sayed, NNE]'s Articles
[Alafeefy, AM]'s Articles
[Bakht, MA]'s Articles
Terms of Use
No data!
Social Bookmark/Share
File name: Synthesis, Antiphospholipase A(2), Antiprotease, Antibacterial Evaluation and Molecular Docking Analysis of Certain Novel Hydrazones.pdf
Format: Adobe PDF
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.