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

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

Journal Name: Current Organic Chemistry

Volume 18 , Issue 20 , 2014

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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.

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

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Article Details

VOLUME: 18
ISSUE: 20
Year: 2014
Page: [2646 - 2651]
Pages: 6
DOI: 10.2174/138527281820141028105256
Price: $58

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