Synthesis and Binding Properties of New Endothelin Receptor Ligands

Authors: Modica, Maria; Salerno, Loredana; Pittala, Valeria; Romeo, Giuseppe; Siracusa, Mariangela; Mereghetti, Ilario; Cagnotto, Alfredo; Mennini, Tiziana

Source: Letters in Drug Design & Discovery, Volume 4, Number 3, April 2007 , pp. 232-238(7)

Publisher: Bentham Science Publishers

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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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018007780077426

Affiliations: 1: Dipartimento di Scienze Farmaceutiche, Università di Catania, Viale A. Doria 6, 95125 Catania,Italy.

Publication date: 2007-04-01

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

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