Targeting Tuberculosis Through Diversity Oriented Synthesis (DOS) of Hydrazide Frameworks and Evaluation of Mycobacterium Activity Thereof

Title:Targeting Tuberculosis Through Diversity Oriented Synthesis (DOS) of Hydrazide Frameworks and Evaluation of Mycobacterium Activity Thereof

Volume: 18 Issue: 20

Author(s): Atul Manvar, Kuldip Upadhyay, Gautamkumar R. Patel and Anamik Shah

Affiliation:

Keywords: Coumarin, carbo-hydrazides, Mtb, H₃₇Rv, MABA.

Abstract: Continuing our research programme to develop the synthesis of small heterocyclic entities, in the present study we prepared carbohydrazides of privileged coumarins through highly attractive Meerwein arylation. The reaction condition is compatible with a wide variety of functional groups present on coumarin and aniline, delivered in moderate to good yields of the target scaffolds. The heterocyclic hydrazide skeletons are challenging to synthesize and have tremendous applications in the drug discovery area. The resulting structural diversity was screened for its antitubercular activity utilizing Mtb H₃₇Rv strains via the MABA assay method. The growth inhibition of the designed diversity was found to be in the range 50–97%. Several molecules were found to be promising for further chemical development and in silico analysis.

Cite this article as:

Manvar Atul, Upadhyay Kuldip, Patel R. Gautamkumar and Shah Anamik, Targeting Tuberculosis Through Diversity Oriented Synthesis (DOS) of Hydrazide Frameworks and Evaluation of Mycobacterium Activity Thereof, Current Organic Chemistry 2014; 18 (20) . https://dx.doi.org/10.2174/138527281820141028105256