Journal :   Asian Journal of Research in Chemistry

Volume No. :   5

Issue No. :  9

Year :  2012

Pages :   1136-1142

ISSN Print :  0974-4169

ISSN Online :  0974-4150


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Docking studies, Synthesis, Characterisation of Substituted Benzothiazoles as DHFR inhibitors and Evaluation of their Antitubercular Activities



Address:   R. Priyadarsini1*, Dr. C.B. Tharani2 and Dr. A. Ajitha Das Aruna3
1Department of Pharmaceutical Chemistry, Madras Medical College, Chennai-600003.
2HOD,Department of Pharmacology, Saveetha Medical college, Chennai - 600077, India
3HOD,Department of Pharmaceutical Chemistry, Madurai Medical College, Madurai.
*Corresponding Author
DOI No:

ABSTRACT:
The re-emergence of tuberculosis (TB) and the rise of drug-resistant strains of Mycobacterium tuberculosis, emphasizes the need for new antiTB drugs. This prompted us to synthesize a novel series of substituted benzothiazoles inhibiting DHFR, a promising target for mycobacterial infections. The structure and purity of all the compounds were confirmed by TLC, FTIR, 1H NMR and Mass spectral data. Molecular docking studies were also performed against Dihydrofolate reductase (DHFR) using GLIDE. The potency to inhibit DHFR was determined by enzyme inhibition studies using DHFR assay kit and also evaluated for their possible in vitro antitubercular activities. When screened for dhfr inhibitory activity, some compounds were found to active, moderate comparing with standard methotrexate . All the newly synthesized compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain by invitro MABA assay and MIC method .Compounds BTZ4, BTZ5, BTZ6 , BTZ10 were found to actively inhibit Mycobacterium tuberculosis at a concentration of 0.01 µg/ml .
KEYWORDS:
DHFR, GLIDE, Benzothiazoles, MABA, Antitubercular activity.
Cite:
R. Priyadarsini, C.B. Tharani, A. Ajitha Das Aruna. Docking studies, Synthesis, Characterisation of Substituted Benzothiazoles as DHFR inhibitors and Evaluation of their Antitubercular Activities. Asian J. Research Chem. 5(9): September, 2012; Page 1136-1142.
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