European Journal of Chemistry

Synthesis, characterization and in vitro evaluation of some new 5-benzylidene-1,3-thiazolidine-2,4-dione analogs as new class of α-glucosidase inhibitors

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Published: Mar 31, 2014
DOI: https://doi.org/10.5155/eurjchem.5.1.144-149.925
Keywords:
α-Glucosidase, Structure activity relationship, Aromatic/heteroaromatic ketone, Thiazolidine-2, 4-dione derivatives, Minimum inhibitory concentration, 5-Benzylidene-1, 3-thiazolidine-2, 4-dione
Section
Research Article
Issue
Vol. 5 No. 1 (2014): March 2014
Dates
Received 2013-09-10
Accepted 2013-10-29
Published 2014-03-31


Main Article Content

Divakara Laxman Somayajulu Nori
Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Kasapu Vishnu Veera Venkata Satyanarayan
Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Vasudeva Rao Avupati
Pharmaceutical Chemistry Division, Andhra University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530003, Andhra Pradesh, India
Bharat Kumar Bugata
Department of Biochemistry and Bioinformatics, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India
Subhash Yenupuri
Department of Chemistry, Gitam University, Rushikonda, Visakhapatnam-530045, Andhra Pradesh, India

Abstract

A series of 5-benzylidene-1,3-thiazolidine-2,4-dione derivatives (5a-u) were synthesized and tested against α-glucosidase. Preparation of the titled compounds was achieved by reaction of (Z)-4-((2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl)benzaldehyde (4) and aromatic/hetero aromatic ketone. Among the compounds tested, (5p) and (5o) were identified as the most active in vitro with minimum inhibitory concentration (MIC) of 6.56±0.81 and 8.92±0.21 µg/mL against α-glucosidase, respectively. Evaluation of the structure activity relationship of substituents within these series has followed the discovery of a variety of compounds.


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Nori, D. L. S.; Satyanarayan, K. V. V. V.; Avupati, V. R.; Bugata, B. K.; Yenupuri, S. Synthesis, Characterization and in Vitro Evaluation of Some New 5-Benzylidene-1,3-Thiazolidine-2,4-Dione Analogs As New Class of α-Glucosidase Inhibitors. Eur. J. Chem. 2014, 5, 144-149.

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