Bioorganic & Medicinal Chemistry 2010-01-01

2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stagePlasmodiuminfections

Deniz Tasdemir, David Sanabria, Ina L. Lauinger, Alice Tarun, Rob Herman, Remo Perozzo, Mire Zloh, Stefan H. Kappe, Reto Brun, Néstor M. Carballeira, Deniz Tasdemir, David Sanabria, Ina L. Lauinger, Alice Tarun, Rob Herman, Remo Perozzo, Mire Zloh, Stefan H. Kappe, Reto Brun, Néstor M. Carballeira

Index: Bioorg. Med. Chem. 18 , 7475-85, (2010)

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Abstract

2-, 5-, 6-, and 9-hexadecynoic acids (HDAs) were synthesized and evaluated in vitro against various parasitic protozoa. 2-HDA inhibited both liver and blood stage Plasmodium infections and multiple plasmodial FAS-II target enzymes. 2-HDA was further studied through enzyme kinetics, docking studies and for pharmacokinetic properties.