4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies

A series of 4-thiazolidinone derivatives (1-18) was synthesized and tested in vitro for its antimicrobial and anticancer potential. Synthesized compounds were found to be 5 more potent antimicrobial agents than anticancer agents. Anticancer screening results indicated that compound 13 (IC50 = 15.18...

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Published in:RSC Advances
Main Author: Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
Format: Article
Language:English
Published: Royal Society of Chemistry 2016
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84997418625&doi=10.1039%2fc6ra23006g&partnerID=40&md5=e66200abdfe28c80e8d382810bf07b05
id 2-s2.0-84997418625
spelling 2-s2.0-84997418625
Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
2016
RSC Advances
6
111
10.1039/c6ra23006g
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84997418625&doi=10.1039%2fc6ra23006g&partnerID=40&md5=e66200abdfe28c80e8d382810bf07b05
A series of 4-thiazolidinone derivatives (1-18) was synthesized and tested in vitro for its antimicrobial and anticancer potential. Synthesized compounds were found to be 5 more potent antimicrobial agents than anticancer agents. Anticancer screening results indicated that compound 13 (IC50 = 15.18 μM) was the most active anticancer agent and was more potent than the standard drug, carboplatin (IC50 > 100 μM). Antimicrobial activity results indicated that 14 was the most active antimicrobial agent (pMICec = 2.14 μM) and may serve as an important lead for the discovery of novel antimicrobial agents. The QSAR studies indicated that the antibacterial and antifungal activities of the synthesized derivatives against different microbial strains were governed by lipophilic parameter, logP, topological parameter, κα3 and electronic parameters cosE and Nu. E. © 2016 The Royal Society of Chemistry.
Royal Society of Chemistry
20462069
English
Article

author Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
spellingShingle Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
author_facet Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
author_sort Deep A.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mishra R.K.; Mani V.
title 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
title_short 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
title_full 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
title_fullStr 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
title_full_unstemmed 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
title_sort 4-Thiazolidinone derivatives: Synthesis, antimicrobial, anticancer evaluation and QSAR studies
publishDate 2016
container_title RSC Advances
container_volume 6
container_issue 111
doi_str_mv 10.1039/c6ra23006g
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84997418625&doi=10.1039%2fc6ra23006g&partnerID=40&md5=e66200abdfe28c80e8d382810bf07b05
description A series of 4-thiazolidinone derivatives (1-18) was synthesized and tested in vitro for its antimicrobial and anticancer potential. Synthesized compounds were found to be 5 more potent antimicrobial agents than anticancer agents. Anticancer screening results indicated that compound 13 (IC50 = 15.18 μM) was the most active anticancer agent and was more potent than the standard drug, carboplatin (IC50 > 100 μM). Antimicrobial activity results indicated that 14 was the most active antimicrobial agent (pMICec = 2.14 μM) and may serve as an important lead for the discovery of novel antimicrobial agents. The QSAR studies indicated that the antibacterial and antifungal activities of the synthesized derivatives against different microbial strains were governed by lipophilic parameter, logP, topological parameter, κα3 and electronic parameters cosE and Nu. E. © 2016 The Royal Society of Chemistry.
publisher Royal Society of Chemistry
issn 20462069
language English
format Article
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