Abstract

DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NOVEL HETEROCYCLIC DERIVATIVES AS ANTI-TUBERCULAR AGENTS

Surya Parakkot Ramakrishnan and Dr. Ayyadurai Jerad Suresh*

ABSTRACT

is a transmittable disease which is considered as the major cause of death. Tuberculosis associated deaths, of which[8] mostly occurred in developing countries. In addition, recently emerged drug resistant tuberculosis is a big challenge to control tuberculosis. Therefore, there is an urgent need for the newer molecule development and more efficient evaluation of new TB drugs which may have potential to cure the diseases and shorter treatment regimens. Literature survey evidences that, Imidazole derivatives exhibit various pharmacological activities, such as anti-bacterial and Anti-tubercular activity. Thus, a series of imidazole based molecules were designed and docked against crucial mtb enzyme target Mtfab D (Malonyl COA - Acyl Carrier Protein Transacylase). The docked molecules were screened against good docking-score and multiple interactions and opted for synthesis. Synthesized molecules repeatedly recrystallized to meet the purity. All the purified compounds were characterized by various spectral analytical techniques and evaluated for anti- mycobacterial activity against tuberculosis H37RV strain by Microplate Alamar Blue Assay (MABA) method. The experimental results shown that Compound (R2) possesses anti-tubercular activity with an MIC below 3.12 mcg/mL and (R4 and R6 ) showed moderate anti tubercular activity with an MIC below 12.5mcg/mL. Whereas R7 and RG1 with moderate activity at below 25 μg and 50mcg/mL.

Keywords: Imidazole, Schiff bases, Microplate Alamar Blue Assay.