Recent advances in the design and synthesis of prazosin derivatives

Due to the large number of therapeutic indications, particularly for antagonists, a field of constant interest in medicinal chemistry is the design, synthesis and pharmacological evaluation of ligands that bind at α1-adrenoreceptors, which include α1a, α1b and α1d subtypes. This review, which is mainly based on literature over the past 10 years, focuses on the developments of some of the most potent, selective and widely used α1-adrenoreceptor antagonists that are structurally related to prazosin (which is characterised by a quinazoline moiety). Initially introduced in therapy for the management of hypertension, prazosin derivatives have become increasingly common in the treatment of benign prostatic hyperplasia. During the past few years, new perspectives have emerged for the use of these derivatives as a novel class of apoptosis-inducing agents in prostate cancer.