Journal
MOLECULES
Volume 18, Issue 6, Pages 6366-6382Publisher
MDPI
DOI: 10.3390/molecules18066366
Keywords
Trypanosoma cruzi; Piper nigrum; antiparasitic drugs; bioisosterism; molecular hybridization
Funding
- CAPES
- FAPERJ
- CNPq
- PROCAD-NF
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The work reported herein describes the synthesis and the assessment of the trypanocidal activity of thirteen new 1,2,4-triazole-3-thiones obtained from natural piperine, the main constituent of the dry fruits of Piper nigrum. It is part of a research program aiming to use abundant and easily available natural products as starting materials for the design and synthesis of new molecules potentially useful as antiparasitic drugs. The variously substituted triazole derivatives were synthesized from the natural amide in four steps with the use of microwave irradiation on overall yields ranging from 32% to 51%. The cyclohexyl substituted derivative showed the best trypanocidal profile on proliferative forms of Trypanosoma cruzi (Y strain), with IC(50)s = 18.3 and 8.87 mu M against epimastigotes and amastigotes, respectively.
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