Solution-phase parallel synthesis of substituted chalcones and their antiparasitary activity against Giardia lamblia.
A library of 25-membered chalcones was prepared by parallel synthesis. Substituted acetophenones and benzaldehydes were condensed using the Claisen-Schmidt base-catalyzed aldol condensation. Several chalcones showed in vitro antiparasitic activity against Giardia lamblia. The highest activity observed for the IC(50) values were 12.72, 15.05 and 15.31 microg/mL, respectively; these are potential leads for the development of antigiardial compounds.
Montes-Avila
Julio
J
Centro de Graduados e Investigación, Instituto Tecnológico de Tijuana, PO Box 1166, 22000 Tijuana, B.C., Mexico.
Díaz-Camacho
Sylvia P
SP
Sicairos-Félix
Josefina
J
Delgado-Vargas
Francisco
F
Rivero
I A
IA
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016829:Giardia lamblia / Q000187:drug effects*; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D047188:Chalcones