1. In vitro Evaluation of the Antileishmanial and Antischistosomal Activities of p-Coumaric Acid Prenylated Derivatives.
- Author
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Vieira TM, Barco JG, Paula LAL, Felix PCA, Bastos JK, Magalhães LG, and Crotti AEM
- Subjects
- Animals, Structure-Activity Relationship, Prenylation, Propionates pharmacology, Propionates chemistry, Molecular Structure, Schistosomicides pharmacology, Schistosomicides chemistry, Schistosomicides chemical synthesis, Dose-Response Relationship, Drug, Schistosoma mansoni drug effects, Coumaric Acids pharmacology, Coumaric Acids chemistry, Leishmania drug effects, Antiprotozoal Agents pharmacology, Antiprotozoal Agents chemistry, Antiprotozoal Agents chemical synthesis, Parasitic Sensitivity Tests
- Abstract
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 (IC
50 =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., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)- Published
- 2024
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