

Microwave assisted synthesis and biological evaluation of a series of 1,5-benzothiazepines as potential cytotoxic and antimicrobial agents
Subhash Yenupuri (1,*)




(1) Department of Chemistry (GIS), Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
(2) Gitam Institute of Technology, Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
(3) Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
(4) Department of Chemistry (GIS), Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
(*) Corresponding Author
Received: 10 Sep 2013 | Revised: 08 Oct 2013 | Accepted: 27 Oct 2013 | Published: 31 Mar 2014 | Issue Date: March 2014
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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European Journal of Chemistry
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DOI: 10.5155/eurjchem.5.1.138-143.924
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Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Citations
[1]. Satbir Mor, Savita Nagoria, Suchita Sindhu, Mohini Khatri, Gurdeep Sidhu, Virender Singh
Synthesis of Indane-Based 1,5-Benzothiazepines Derived from 3-Phenyl-2,3-dihydro-1H-inden-1-one and Antimicrobial Studies Thereof
Journal of Heterocyclic Chemistry 54(6), 3282, 2017
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[2]. Yasmine M. Abdel Aziz, Gehad Lotfy, Mohamed M. Said, El Sayed H. El Ashry, El Sayed H. El Tamany, Saied M. Soliman, Marwa M. Abu-Serie, Mohamed Teleb, Sammer Yousuf, Alexander Dömling, Luis R. Domingo, Assem Barakat
Design, Synthesis, Chemical and Biochemical Insights Into Novel Hybrid Spirooxindole-Based p53-MDM2 Inhibitors With Potential Bcl2 Signaling Attenuation
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Syntheses and Studies of 8-Substituted-2-(2-Chlorophenyl/3-chlorophenyl)- 4-(4-hydroxyphenyl/phenyl)-2,3/2,5-dihydro-1,5-benzothiazepines
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[5]. Hassan Y. Aboul-Enein, Oana Mihaela Antochi, Gheorghe Nechifor, Andrei A. Bunaciu
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