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Letters in Drug Design & Discovery

Author(s): Maria Modica, Loredana Salerno, Valeria Pittala, Giuseppe Romeo, Mariangela Siracusa, Ilario Mereghetti, Alfredo Cagnotto and Tiziana Mennini

DOI: 10.2174/157018007780077426

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Synthesis and Binding Properties of New Endothelin Receptor Ligands

Page: [232 - 238] Pages: 7

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Abstract

In this paper we report the synthesis of a new series of benzenesulfonamides and the evaluation of their binding properties on ETAh and ETBh receptor subtypes. Some new derivatives behave as selective ETAh receptor ligands and among them, 2-{[(4-chloro-3-methyl-5-isoxazolyl)amino]sulfonyl}-N-(2,4,6- trimethylphenyl)benzamide (23) was the most interesting.

Keywords: Hypertension, Endothelins, G protein-coupled receptors, ET receptors, Benzenesulfonamides, Binding properties