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Synthesis, Antitrypanosomal and Antimycobacterial Activities of Coumarin N-acylhydrazonic Derivatives.
- 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.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents pharmacology
Antiprotozoal Agents chemical synthesis
Antiprotozoal Agents chemistry
Antiprotozoal Agents pharmacology
Chemistry Techniques, Synthetic
Drug Resistance, Bacterial drug effects
Hydrazones chemistry
Mycobacterium tuberculosis drug effects
Coumarins chemistry
Hydrazones chemical synthesis
Hydrazones pharmacology
Nitrogen chemistry
Trypanosoma drug effects
Subjects
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