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.
Graphical Abstract
Current Organic Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/138527281820141028105256 |
Print ISSN 1385-2728 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5348 |
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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