DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NOVEL INDOLE DERIVATIVES AS ANTI TUBERCULAR AGENTS
S.S.D. Bhavani Raja*, Samyuktha Metta, Rapaka Arun Kumar, Namala Manasa and Naveena R.
ABSTRACT
The aim is to design and synthesize some novel heterocyclic analogues such as indole derivatives which will prove to be effective against Mycobacterium tuberculosis. The objectives are Design of Glutamine synthetase inhibitors by docking studies using Autodock ® software, Prediction of Insilico Drug likeness by Molinspiration® software, Insilico Toxicity Assessment done by OSIRIS® software, Laboratory synthesis of chosen compounds with top Docking Scores, Characterization of the synthesized compounds by TLC, Melting point, IR Spectroscopy, H1 NMR Spectroscopy, LC-Mass Spectrometry. Evaluation of In-vitro anti -tubercular activity of the synthesized compounds by (MABA). The present study deals with A series of Schiff bases of isatin derivatives were designed, docked, synthesized and evaluated against Glutamine synthetase 1 enzyme which is critical for the survival and growth of MTB.The Minimum Inhibitory Concentration of the synthesized compounds ranges from 50-1.6μg/ml. The work concludes that the Compounds Compounds PK2 and PK4 showed activity at 1.6 μg/ml concentrations which are comparable to the activity of the standard drugs Pyrazinamide, Streptomycin, Ciprofloxacin which are active at 3.125μg/ml,6.25μg/ml,3.125μg/ml concentrations.Further, structural refinement of the synthesized compounds is expected to yield promising molecules against the pathogen MTB.
Keywords: Synthesis, Characterization, Biological Evaluation, Novel Indole Derivatives.
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