Piplartine-Inspired 3,4,5-Trimethoxycinnamates: Trypanocidal, Mechanism of Action, and In Silico Evaluation.

ABSTRACT: Chagas disease (CD) is one of the main neglected tropical diseases that promote relevant socioeconomic impacts in several countries. The therapeutic options for the treatment of CD are limited, and parasite resistance has been reported. Piplartine is a phenylpropanoid imide that has diverse biological activities, including trypanocidal action. Thus, the objective of the present work was to prepare a collection of thirteen esters analogous to piplartine (1-13) and evaluate their trypanocidal activity against Trypanosoma cruzi. Of the tested analogues, compound 11 ((E)-furan-2-ylmethyl 3-(3,4,5-trimethoxyphenyl)acrylate) showed good activity with IC₅₀ values = 28.21 ± 5.34 μM and 47.02 ± 8.70 μM, against the epimastigote and trypomastigote forms,

SUBMITTER: Filho CSMB 

PROVIDER: S-EPMC10254306 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature