DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF ANTI-TUBERCULAR AGENTS TARGETING MTFAB D, MALONYL COA - ACYL CARRIER PROTEIN TRANSACYLASE
Parakkot Ramakrishnan Surya and Ayyadurai Jerad Suresh*
Mycobacterium tuberculosis MTB, or TB (tubercle bacillus), is a common, and in many cases lethal, infectious disease caused by various strains of mycobacteria, usually Mycobacterium tuberculosis. Over the past 200 years, tuberculosis has been responsible for the death of over 100 million people. Moreover due to the emergence and reemergence of multi-drug resistant tuberculosis (MDR-TB), extremely - drug resistant tuberculosis (XDR-TB), totally -drug resistant tuberculosis (TDR-TB) and also because of the co-infection of TB with HIV there is an urgent need for new Anti-TB agents. Today hetero cyclic compounds have attained wide attention in the discovery of new drug candidates because of their diverse biological activity. Heterocyclic ring system encompasses the core of the active moiety as pharmacophore. For a period of decade’s heterocyclic therapeutic agents plays a pivotal role in chemotherapy. In view of the above facts, this research work deals with the designing of chalcones containing heterocyclic moiety and synthesizing it for potential anti-tubercular activity. So molecules were designed and docked against MTB enzyme mtFab D, malonyl CoA - acyl carrier protein transacylase The screened molecules were synthesized by condensation method, purified by chromatographic techniques, characterized by various spectral analytical techniques and evaluated for in-vitro anti mycobacterial activity against tuberculosis H37RV strain by Microplate Alamar Blue Assay (MABA) method. The experimental results show that Compound Y possesses better anti-tubercular activity with an MIC below 1.6 mcg/mL while NA, and PW showed moderate anti tubercular activity with an MIC below 6.25mcg/Ml, and Compound X exhibited good anti tubercular activity with an MIC below 12..5mcg/Ml.
Keywords: Mycobacterium tuberculosis, Chalcones, Docking, MABA.
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