Solution-phase parallel synthesis of an isoflavone library for the discovery of novel antigiardial agents.
Combinatorial chemistry has become a dramatically useful tool for the development of new medicinal agents. In the search to discover a novel and effective lead for the treatment of giardiasis, solution-phase synthesis of a library of isoflavone derivatives has been accomplished. Of the products screened, several compounds such as P(A1,B1) and P(A1,B11) exhibited potent antigiardial activity. The details of synthesis, in vitro antigiardial assay, and preliminary structure-activity relationships of these compounds are described.
Mineno
T
T
Department of Medicinal Chemistry and Pharmacology, School of Pharmacy, University of Mississippi, University, MS 38677, USA.
Stanford
K M
KM
Walker
L A
LA
Avery
M A
MA
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005873:Giardiasis / Q000188:drug therapy; D006801:Humans; D007529:Isoflavones / Q000138:chemical synthesis*; D012996:Solutions
D000981:Antiprotozoal Agents; D007529:Isoflavones; D012996:Solutions