Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design, Synthesis and 3-D Characterization of 1-Benzenesulfonyl-1,2,3,4- Tetrahydroquinolines as Lead Scaffold for Antiparasitic Drug

Author(s): R.J. Pagliero, A.B. Pierini, R. Brun, M.R. Mazzieri.

Abstract:

Ten 1-benzenesulfonyl-1,2,3,4-tetrahydroquinoline (BSTHQ) were synthesized and characterized and their antiprotozoal activities were investigated. This small library was designed by combining two 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 value than the precursor heterocycle. Most compounds were moderately active against T cruzi, but 3 showed a promising IC50 value (9.76μM) 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.

Keywords: Antiparasitic, Benzenesulfonyl, Tetrahydroquinolines, Stereoelectronic Properties

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Article Details

VOLUME: 7
ISSUE: 6
Year: 2010
Page: [461 - 470]
Pages: 10
DOI: 10.2174/157018010791306614
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