Microwave assisted synthesis and biological evaluation of a series of 1,5-benzothiazepines as potential cytotoxic and antimicrobial agents

Subhash Yenupuri; Agastyaraju Venkata Lakshmi Narasimha Satyanarayana Hariharan; Bharat Kumar Bugata; Divakara Laxman Somayajulu Nori

doi:10.5155/eurjchem.5.1.138-143.924

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Published: Mar 31, 2014

DOI: https://doi.org/10.5155/eurjchem.5.1.138-143.924

Keywords:

Cytotoxicity, Podophyllotoxin, 1, 5-Benzothiazepines, Antimicrobial activity, Brine shrimp lethality, Agar well diffusion assay

Section

Research Article

Issue

Vol. 5 No. 1 (2014): March 2014

Dates

Received 2013-09-10
Accepted 2013-10-27
Published 2014-03-31

Subhash Yenupuri

Department of Chemistry (GIS), Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

Agastyaraju Venkata Lakshmi Narasimha Satyanarayana Hariharan

Gitam Institute of Technology, Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

Bharat Kumar Bugata

Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

Divakara Laxman Somayajulu Nori

Department of Chemistry (GIS), Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

Abstract

A series of 2,3-dihydro-2-(susbtituted)-4-(1-methyl-1H-pyrrol-2-yl)-1,5-benzothiazepines (4a-v) have been synthesized evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine shrimp lethality assay, compound 4q exhibited significant cytotoxicity at ED₅₀ values 3.45±0.15 µg/mL. This level of activity was found comparable to that of the reference drug podophyllotoxin with ED₅₀ value 3.61±0.17 µg/mL. Antimicrobial activity was assessed using agar well diffusion assay method against selected Gram-positive, Gram-negative and fungal strains. Among the compounds tested, 4q, 4r and 4l were found to be more active with MIC 16-32 µg/mL against all tested microorganisms.

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Yenupuri, S.; Hariharan, A. V. L. N. S.; Bugata, B. K.; Nori, D. L. S. Microwave Assisted Synthesis and Biological Evaluation of a Series of 1,5-Benzothiazepines As Potential Cytotoxic and Antimicrobial Agents. Eur. J. Chem. 2014, 5, 138-143.

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Supporting Agencies

Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

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