Synthesis and binding properties of new endothelin receptor ligands

Maria Modica; Loredana Salerno; Valeria Pittalà; Giuseppe Romeo; Mariangela Siracusa; Ilario Mereghetti; Alfredo Cagnotto; Tiziana Mennini

doi:10.2174/157018007780077426

Synthesis and binding properties of new endothelin receptor ligands

Maria Modica, Loredana Salerno, Valeria Pittalà, Giuseppe Romeo, Mariangela Siracusa, Ilario Mereghetti, Alfredo Cagnotto, Tiziana Mennini

Istituto di Ricerche Farmacologiche "Mario Negri"

Research output: Contribution to journal › Article › peer-review

Abstract

In this paper we report the synthesis of a new series of benzenesulfonamides and the evaluation of their binding properties on ET _Ah and ET_Bh receptor subtypes. Some new derivatives behave as selective ET_Ah 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.

Original language	English
Pages (from-to)	232-238
Number of pages	7
Journal	Letters in Drug Design and Discovery
Volume	4
Issue number	3
DOIs	https://doi.org/10.2174/157018007780077426
Publication status	Published - Apr 2007

Keywords

Benzenesulfonamides
Binding properties
Endothelins
ET receptors
G protein-coupled receptors
Hypertension

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery
Molecular Medicine

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AU - Modica, Maria

AU - Salerno, Loredana

AU - Pittalà, Valeria

AU - Romeo, Giuseppe

AU - Siracusa, Mariangela

AU - Mereghetti, Ilario

AU - Cagnotto, Alfredo

AU - Mennini, Tiziana

PY - 2007/4

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AB - In this paper we report the synthesis of a new series of benzenesulfonamides and the evaluation of their binding properties on ET Ah 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.

KW - Benzenesulfonamides

KW - Binding properties

KW - Endothelins

KW - ET receptors

KW - G protein-coupled receptors

KW - Hypertension

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