Synthesis, screening, and molecular modeling of new potent and selective antagonists at the α1d adrenergic receptor

…, D Barlocco, F Montesano, G Cignarella…

Index: Leonardi, Amedeo; Barlocco, Daniela; Montesano, Federica; Cignarella, Giorgio; Motta, Gianni; Testa, Rodolfo; Poggesi, Elena; Seeber, Michele; De Benedetti, Pier G.; Fanelli, Francesca Journal of Medicinal Chemistry, 2004 , vol. 47, # 8 p. 1900 - 1918

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Citation Number: 52

Abstract

In the present study, more than 75 compounds structurally related to BMY 7378 have been designed and synthesized. Structural variations of each part of the reference molecule have been introduced, obtaining highly selective ligands for the α1d adrenergic receptor. The molecular determinants for selectivity at this receptor are essentially held by the phenyl substituent in the phenylpiperazine moiety. The integration of an extensive SAR analysis ...