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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and M.R. Mazzieri

Volume 7, Issue 6, 2010

Page: [461 - 470] Pages: 10

DOI: 10.2174/157018010791306614

Price: $65


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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