New pyrimido [5, 4-b] indoles as ligands for α1-adrenoceptor subtypes

…, T Mennini, F Nicoletti, M Botta, F Russo…

Index: Romeo, Giuseppe; Materia, Luisa; Manetti, Fabrizio; Cagnotto, Alfredo; Mennini, Tiziana; Nicoletti, Ferdinando; Botta, Maurizio; Russo, Filippo; Minneman, Kenneth P. Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 2877 - 2894

Full Text: HTML

Citation Number: 44

Abstract

A new series of compounds were designed as structural analogues of the α1-AR ligand RN5 (4), characterized by a tricyclic 5 H-pyrimido [5, 4-b] indole-(1 H, 3 H) 2, 4-dione system connected through an alkyl chain to a phenylpiperazine (PP) moiety. These compounds were synthesized and tested in binding assays on human α1A-AR, α1B-AR, and α1D-AR subtypes expressed in HEK293 cells. Several structural modifications were performed on ...