Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones

Some novel hydrazone derivatives 6a-o 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 p...

Full description

Bibliographic Details
Main Authors:	El-Sayed, Nahed Nasser Eid, Alafeefy, Ahmed Mahmoud, Bakht, Mohammed Afroz, Vijay H., Masand, Aldalbahi, Ali, N., Chen, C., Fan, Bacha, Abir Ben Ben
Format:	Article
Language:	English English
Published:	MDPI AG 2016
Subjects:	RM300 Drugs and their action
Online Access:	http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/1/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease.pdf http://irep.iium.edu.my/56527/2/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease_Scopus.pdf

id	iium-56527
recordtype	eprints
spelling	iium-565272017-10-20T07:50:29Z http://irep.iium.edu.my/56527/ Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones El-Sayed, Nahed Nasser Eid Alafeefy, Ahmed Mahmoud Bakht, Mohammed Afroz Vijay H., Masand Aldalbahi, Ali N., Chen C., Fan Bacha, Abir Ben Ben RM300 Drugs and their action Some novel hydrazone derivatives 6a-o 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; 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. MDPI AG 2016-12 Article PeerReviewed application/pdf en http://irep.iium.edu.my/56527/1/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease.pdf application/pdf en http://irep.iium.edu.my/56527/2/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease_Scopus.pdf El-Sayed, Nahed Nasser Eid and Alafeefy, Ahmed Mahmoud and Bakht, Mohammed Afroz and Vijay H., Masand and Aldalbahi, Ali and N., Chen and C., Fan and Bacha, Abir Ben Ben (2016) Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones. Molecules, 21 (12). pp. 1-17. ISSN 1420-3049 http://www.mdpi.com/1420-3049/21/12/1664/pdf 10.3390/molecules21121664
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English English
topic	RM300 Drugs and their action
spellingShingle	RM300 Drugs and their action El-Sayed, Nahed Nasser Eid Alafeefy, Ahmed Mahmoud Bakht, Mohammed Afroz Vijay H., Masand Aldalbahi, Ali N., Chen C., Fan Bacha, Abir Ben Ben Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
description	Some novel hydrazone derivatives 6a-o 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; 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.
format	Article
author	El-Sayed, Nahed Nasser Eid Alafeefy, Ahmed Mahmoud Bakht, Mohammed Afroz Vijay H., Masand Aldalbahi, Ali N., Chen C., Fan Bacha, Abir Ben Ben
author_facet	El-Sayed, Nahed Nasser Eid Alafeefy, Ahmed Mahmoud Bakht, Mohammed Afroz Vijay H., Masand Aldalbahi, Ali N., Chen C., Fan Bacha, Abir Ben Ben
author_sort	El-Sayed, Nahed Nasser Eid
title	Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
title_short	Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
title_full	Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
title_fullStr	Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
title_full_unstemmed	Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
title_sort	synthesis, antiphospholipase a2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones
publisher	MDPI AG
publishDate	2016
url	http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/ http://irep.iium.edu.my/56527/1/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease.pdf http://irep.iium.edu.my/56527/2/56527_Synthesis%2C%20antiphospholipase%20A2%2C%20antiprotease_Scopus.pdf
first_indexed	2023-09-18T21:19:45Z
last_indexed	2023-09-18T21:19:45Z
_version_	1777411802747895808

Synthesis, antiphospholipase A2, antiprotease, antibacterial evaluation and molecular docking analysis of certain novel hydrazones

Similar Items