In vitro Evaluation of the Antileishmanial and Antischistosomal Activities of p‐Coumaric Acid Prenylated Derivatives

We have evaluated eight p‐coumaric acid prenylated derivatives in vitro for their antileishmanial activity against Leishmania amazonensis promastigotes and their antischistosomal activity against Schistosoma mansoni adult worms. Compound 7 ((E)‐3,4‐diprenyl‐4‐isoprenyloxycinnamic alcohol) was the mo...

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Bibliographic Details
Published in:Chemistry & biodiversity 2024-05, Vol.21 (5), p.e202400491-n/a
Main Authors: Vieira, Tatiana M., Barco, Júlia G., Paula, Lucas A. L., Felix, Paulo C. A., Bastos, Jairo K., Magalhães, Lizandra G., Crotti, Antônio E. M.
Format: Article
Language:English
Subjects:
Animals
Antiprotozoal Agents - chemical synthesis
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
artepillin C
Coumaric acid
Coumaric Acids - chemistry
Coumaric Acids - pharmacology
Dose-Response Relationship, Drug
Leishmania - drug effects
Leishmania amazonensis
Molecular Structure
O-prenylation
Parasitic Sensitivity Tests
plicatin B
Prenylation
Promastigotes
Propionates - chemistry
Propionates - pharmacology
Schistosoma mansoni
Schistosoma mansoni - drug effects
Schistosomicides - chemical synthesis
Schistosomicides - chemistry
Schistosomicides - pharmacology
Structure-Activity Relationship
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Summary:We have evaluated eight p‐coumaric acid prenylated derivatives in vitro for their antileishmanial activity against Leishmania amazonensis promastigotes and their antischistosomal activity against Schistosoma mansoni adult worms. Compound 7 ((E)‐3,4‐diprenyl‐4‐isoprenyloxycinnamic alcohol) was the most active against L. amazonensis (IC50=45.92 μM) and S. mansoni (IC50=64.25 μM). Data indicated that the number of prenyl groups, the presence of hydroxyl at C9, and a single bond between C7 and C8 are important structural features for the antileishmanial activity of p‐coumaric acid prenylated derivatives.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202400491