Mon, 18 Dec 2017

Synthesis, Characterization and Biological Evaluation of Novel Thienopyrimidine and Triazolothienopyrimidine Derivatives as Anti-Tubercular and Antibacterial Agents

Ashraf Y. Khan1, Mallikarjun B. Kalashetti1, Ningaraddi S. Belavagi1, Narahari Deshapande1, Imtiyaz Ahmed M. Khazi*1

1. Department of Chemistry, Karnatak University, Dharwad 580003, Karnataka, India


ABSTRACT

A series of novel triazole fused thienopyrimidine derivatives are synthesized by Gewald reaction, which are well characterized by IR, 1HNMR, 13CNMR and Mass spectral analysis. These compounds are screened for their in vitro anti-tubercular and antibacterial activities. Most of these compounds exhibited MIC values in the range of 20 – 100 µM against Mycobacterium tuberculosis H37Rv. In the series, compound 5c was most active with MIC 20 µM. Furthermore, the title compounds were screened for antibacterial activity against Staphylococcus aureus ATCC 29213 (gram positive) and Escherichia coli ATCC 25922 (gram negative) bacteria. Some of these compounds exhibited MIC values in the range 8 - 64µM. Compound 5c was found to be the most active with an MIC of 5 and 8µM respectively.

Keywords: Gewald reaction, Thienopyrimidine, Triazolothienopyrimidine, Anti-tubercular activiy, Anti-bacterial activity.


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