2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line

Background: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer. Objective: The present study was aimed to synthesize and e...

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Published in:Mini-Reviews in Medicinal Chemistry
Main Author: Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
Format: Article
Language:English
Published: Bentham Science Publishers 2019
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85071752332&doi=10.2174%2f1389557518666181009151008&partnerID=40&md5=33a05942a654f4141b0ff0fa25ac4f8b
id 2-s2.0-85071752332
spelling 2-s2.0-85071752332
Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
2019
Mini-Reviews in Medicinal Chemistry
19
13
10.2174/1389557518666181009151008
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85071752332&doi=10.2174%2f1389557518666181009151008&partnerID=40&md5=33a05942a654f4141b0ff0fa25ac4f8b
Background: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer. Objective: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole. Methods: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]-imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively. Results: Compounds 8 (MICpa,an = 2.41, 1.20 µM/ml), 10 (MICse,sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity. Conclusion: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents. © 2019 Bentham Science Publishers.
Bentham Science Publishers
13895575
English
Article

author Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
spellingShingle Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
author_facet Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
author_sort Tahlan S.; Narasimhan B.; Lim S.M.; Ramasamy K.; Mani V.; Shah S.A.A.
title 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
title_short 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
title_full 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
title_fullStr 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
title_full_unstemmed 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
title_sort 2-mercaptobenzimidazole schiff bases: Design, synthesis, antimicrobial studies and anticancer activity on HCT-116 cell line
publishDate 2019
container_title Mini-Reviews in Medicinal Chemistry
container_volume 19
container_issue 13
doi_str_mv 10.2174/1389557518666181009151008
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85071752332&doi=10.2174%2f1389557518666181009151008&partnerID=40&md5=33a05942a654f4141b0ff0fa25ac4f8b
description Background: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer. Objective: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole. Methods: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]-imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively. Results: Compounds 8 (MICpa,an = 2.41, 1.20 µM/ml), 10 (MICse,sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity. Conclusion: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents. © 2019 Bentham Science Publishers.
publisher Bentham Science Publishers
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