Design, synthesis and 3-D characterization of 1-benzenesulfonyl-1,2,3,4-tetrahydroquinolines as lead scaffold for antiparasitic drug

R. PAGLIERO; A. PIERINI; R. BRUN ; M. R. MAZZIERI

BENTHAM SCIENCE PUBL LTD

Año: 2010 vol. 7 p. 461 - 461

en 1-benzenesulfonyl-1,2,3,4-tetrahydroquinoline (BSTHQ) were synthesized and characterizedand their antiprotozoal activities were investigated. This small library was designed by combiningtwo chemical moieties that are known to be biologically active by itself. The BS group seems to be favorable for the antiparasitic activity, since the derivatives presented lower IC50 than the precursor heterocycle. Most compounds were moderately active against T cruzi, but 3 showed a promising IC50 (9.76ìM) with low cytotoxicity (L6). Also, 3, 6 and 9 showed interesting activity and reasonable selectivity against P. falciparum. These derivatives are considered as lead scaffolds and merit further exploration through structure optimization.