Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents

Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents

4-Thiazolidinone analogs 1-20 were synthesized, characterized by 1H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65 μM, if compared with standard thiourea having IC50 value of 21...

Full description

Bibliographic Details
Published in:Bioorganic Chemistry
Main Author: Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
Format: Article
Language:English
Published: Academic Press Inc. 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84945937324&doi=10.1016%2fj.bioorg.2015.10.005&partnerID=40&md5=cfe737f28b6a3625c62dfe6020251128
id 2-s2.0-84945937324
spelling 2-s2.0-84945937324
Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
2015
Bioorganic Chemistry
63

10.1016/j.bioorg.2015.10.005
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84945937324&doi=10.1016%2fj.bioorg.2015.10.005&partnerID=40&md5=cfe737f28b6a3625c62dfe6020251128
4-Thiazolidinone analogs 1-20 were synthesized, characterized by 1H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65 μM, if compared with standard thiourea having IC50 value of 21.25 ± 0.15 μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34 ± 0.02, 14.62 ± 0.03, 8.43 ± 0.01, 7.3 ± 0.04, 2.31 ± 0.002, 5.75 ± 0.003, 8.81 ± 0.005, and 1.73 ± 0.001 μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies. © 2015 Elsevier Inc. All rights reserved.
Academic Press Inc.
452068
English
Article
author Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
spellingShingle Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
author_facet Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
author_sort Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
title Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
title_short Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
title_full Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
title_fullStr Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
title_full_unstemmed Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
title_sort Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
publishDate 2015
container_title Bioorganic Chemistry
container_volume 63
container_issue
doi_str_mv 10.1016/j.bioorg.2015.10.005
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84945937324&doi=10.1016%2fj.bioorg.2015.10.005&partnerID=40&md5=cfe737f28b6a3625c62dfe6020251128
description 4-Thiazolidinone analogs 1-20 were synthesized, characterized by 1H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65 μM, if compared with standard thiourea having IC50 value of 21.25 ± 0.15 μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34 ± 0.02, 14.62 ± 0.03, 8.43 ± 0.01, 7.3 ± 0.04, 2.31 ± 0.002, 5.75 ± 0.003, 8.81 ± 0.005, and 1.73 ± 0.001 μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies. © 2015 Elsevier Inc. All rights reserved.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
_version_ 1809678486731751424

Similar Items