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Synthesis, Antitrypanosomal and Antimycobacterial Activities of Coumarin N-acylhydrazonic Derivatives.

Authors :
Capelini C
Câmara VRF
Villar JDF
Barbosa JMC
Salomão K
de Castro SL
Junior PAS
Murta SMF
Couto TB
Lourenço MCS
Wardell JL
Low JN
da Silva EF
Carvalho SA
Source :
Medicinal chemistry (Shariqah (United Arab Emirates)) [Med Chem] 2021; Vol. 17 (6), pp. 630-637.
Publication Year :
2021

Abstract

Background: Near to 5-7 million people are infected with T. cruzi in the world, and about 10,000 people per year die of problems associated with this disease.<br />Methods: Herein, the synthesis, antitrypanosomal and antimycobacterial activities of seventeen coumarinic N-acylhydrazonic derivatives have been reported.<br />Results: These compounds were synthesized using methodology with reactions global yields ranging from 46%-70%. T. cruzi in vitro effects were evaluated against trypomastigote and amastigote, forming M. tuberculosis activity towards H37Rv sensitive strain and resistant strains.<br />Discussion: Against T. cruzi, the more active compounds revealed only moderate activity IC <subscript>50</subscript> /96h~20 μM for both trypomastigotes and amastigotes intracellular forms. (E)-2-oxo-N'- (3,4,5-trimethoxybenzylidene)-2H-chromene-3-carbohydrazide showed meaningful activity in INH resistant/RIP resistant strain.<br />Conclusion: These compound acting as multitarget could be good leads for the development of new trypanocidal and bactericidal agents.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Details

Language :
English
ISSN :
1875-6638
Volume :
17
Issue :
6
Database :
MEDLINE
Journal :
Medicinal chemistry (Shariqah (United Arab Emirates))
Publication Type :
Academic Journal
Accession number :
31965946
Full Text :
https://doi.org/10.2174/1573406416666200121105215