New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: High affinity ligands for the α1-adrenoceptor subtypes

A number of new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives were synthesized and evaluated for their binding and functional properties at α1-adrenergic receptor (α1-AR) subtypes. They behaved as potent α1-AR antagonists. In binding experiments, some of them (RC24 and RC23) showed very high affinity for the α1D-AR subtype.

Graphical abstractThe synthesis and the binding and functional properties for the α1-AR subtypes of some new pyrimido[5,4-b]indole and [1]benzothieno[3,2-d]pyrimidine derivatives are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide