Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors
A total of Twenty two (22) 22 ) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1 HNMR, 13 C NMR and screened against cholinesterase inhibitory potentials. All the adducts ( 1-22 ) showed varying degree of cholinesterase inhibitory potential IC50 50 ran...
Published in: | CHEMICAL DATA COLLECTIONS |
---|---|
Main Authors: | , , , , , , , , , , , , , |
Format: | Article |
Language: | English |
Published: |
ELSEVIER
2024
|
Subjects: | |
Online Access: | https://www-webofscience-com.uitm.idm.oclc.org/wos/woscc/full-record/WOS:001333598600001 |
author |
Zulfiqar Ahmad; Khan Irshad Ullah; Nabi Muhammad; Ullah Hayat; Iqbal Naveed; Zeb Benish; Hussain Amjad; Khan Daud; Rab Abdur; Junaid Sayyed Muhammad; Taha Muhammad; Shah Syed Adnan Ali; Rahim Fazal |
---|---|
spellingShingle |
Zulfiqar Ahmad; Khan Irshad Ullah; Nabi Muhammad; Ullah Hayat; Iqbal Naveed; Zeb Benish; Hussain Amjad; Khan Daud; Rab Abdur; Junaid Sayyed Muhammad; Taha Muhammad; Shah Syed Adnan Ali; Rahim Fazal Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors Chemistry |
author_facet |
Zulfiqar Ahmad; Khan Irshad Ullah; Nabi Muhammad; Ullah Hayat; Iqbal Naveed; Zeb Benish; Hussain Amjad; Khan Daud; Rab Abdur; Junaid Sayyed Muhammad; Taha Muhammad; Shah Syed Adnan Ali; Rahim Fazal |
author_sort |
Zulfiqar |
spelling |
Zulfiqar, Ahmad; Khan, Irshad Ullah; Nabi, Muhammad; Ullah, Hayat; Iqbal, Naveed; Zeb, Benish; Hussain, Amjad; Khan, Daud; Rab, Abdur; Junaid, Sayyed Muhammad; Taha, Muhammad; Shah, Syed Adnan Ali; Rahim, Fazal Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors CHEMICAL DATA COLLECTIONS English Article A total of Twenty two (22) 22 ) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1 HNMR, 13 C NMR and screened against cholinesterase inhibitory potentials. All the adducts ( 1-22 ) showed varying degree of cholinesterase inhibitory potential IC50 50 ranging between 13.23 f 0.02 to 59.09 f 1.22 mu M against acetylcholinesterase, with IC50 50 values ranging from 23.55 f 0.32 to 61.55 f 0.58 mu M against butyrylcholinesterase. Among the series analogs 1, 3, 8, 12, 14, 15, 17, 18 and 22 with IC50 50 values 20.05 f 0.13, 17.32 f 0.15, 14.32 f 0.97, 23.33 f 0.56, 18.02 f 0.09, 19.05 f 0.13, 15.11 f 0.23, 13.23 f 0.02, and 22.57 f 0.09 mu M respectively showed excellent inhibitory potential against acetylcholinesterase and with IC50 50 values 31.46 f 0.98, 26.06 f 0.08, 25.33 f 1.49, 30.12 f 0.78, 28.11 f 0.5, 29.33 f 0.19, 25.37 f 0.47, 23.55 f 0.32 and 33.12 f 0.78 against butylcholinesterase as compared to the standard Galanthamine. All other analogs showed moderate inhibitory potential. A structure- activity relationship has been established for all compounds. Through molecular docking studies, the interactions between compounds with the enzyme active sites were confirmed. ELSEVIER 2405-8300 2024 52 10.1016/j.cdc.2024.101151 Chemistry WOS:001333598600001 https://www-webofscience-com.uitm.idm.oclc.org/wos/woscc/full-record/WOS:001333598600001 |
title |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
title_short |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
title_full |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
title_fullStr |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
title_full_unstemmed |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
title_sort |
Synthesis and biological evaluation of substituted benzohydrazide Schiff base adduct as potential cholinesterase inhibitors |
container_title |
CHEMICAL DATA COLLECTIONS |
language |
English |
format |
Article |
description |
A total of Twenty two (22) 22 ) derivatives of benzohydrazide bearing Schiff base have been synthesized, characterized through 1 HNMR, 13 C NMR and screened against cholinesterase inhibitory potentials. All the adducts ( 1-22 ) showed varying degree of cholinesterase inhibitory potential IC50 50 ranging between 13.23 f 0.02 to 59.09 f 1.22 mu M against acetylcholinesterase, with IC50 50 values ranging from 23.55 f 0.32 to 61.55 f 0.58 mu M against butyrylcholinesterase. Among the series analogs 1, 3, 8, 12, 14, 15, 17, 18 and 22 with IC50 50 values 20.05 f 0.13, 17.32 f 0.15, 14.32 f 0.97, 23.33 f 0.56, 18.02 f 0.09, 19.05 f 0.13, 15.11 f 0.23, 13.23 f 0.02, and 22.57 f 0.09 mu M respectively showed excellent inhibitory potential against acetylcholinesterase and with IC50 50 values 31.46 f 0.98, 26.06 f 0.08, 25.33 f 1.49, 30.12 f 0.78, 28.11 f 0.5, 29.33 f 0.19, 25.37 f 0.47, 23.55 f 0.32 and 33.12 f 0.78 against butylcholinesterase as compared to the standard Galanthamine. All other analogs showed moderate inhibitory potential. A structure- activity relationship has been established for all compounds. Through molecular docking studies, the interactions between compounds with the enzyme active sites were confirmed. |
publisher |
ELSEVIER |
issn |
2405-8300 |
publishDate |
2024 |
container_volume |
52 |
container_issue |
|
doi_str_mv |
10.1016/j.cdc.2024.101151 |
topic |
Chemistry |
topic_facet |
Chemistry |
accesstype |
|
id |
WOS:001333598600001 |
url |
https://www-webofscience-com.uitm.idm.oclc.org/wos/woscc/full-record/WOS:001333598600001 |
record_format |
wos |
collection |
Web of Science (WoS) |
_version_ |
1814778545273044992 |