期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 15, 期 24, 页码 7553-7560出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.09.007
关键词
quinolinylarylsulfonamides; quinolinylarylsulfonamide-copper and zinc complexes; leishmanicidal activity; trypanocidal activity; Vero cells; macrophages
In the present paper 12 N-quinolin-8-yl-arylsulfonamides synthesized by coupling 8-aminoquinolines with various arylsulfonylchlorides were assayed in vitro against Leishmania amazonensis, L. chagasi and Trypanosoma cruzi strains. This series of new compounds were found to be selective for Leishmania spp. promastigote and amastigote forms. The most active compound was the N-(8-quinolyl)-3,5-diflu. uoro-benzenesulfonamide 10 with an IC50 against L. amazonensis and L. chagasi of 2.12 and 0.45 mu M, respectively. The less cytotoxic biphenyl derivative 7 was very e. ffective against intracellular L. amazonensis with a reduction of macrophage cell infection of 82.1% at 25 mu M. In addition, a copper complex 17 of an inactive ligand was readily synthesized and showed high leishmanicidal and trypanocidal activity against both extra and intracellular forms. (c) 2007 Elsevier Ltd. All rights reserved.
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