Abstract

The interest of researchers for ligands of the endothelin receptors ET_A and ET_B is due to their extensive therapeutic potential. In particular, receptor antagonists are useful in a number of diseases such as pulmonary hypertension, acute myocardial infarction, congestive heart failure, renal failure, and atherosclerosis. In the context of our research program aimed to the development of new endothelin receptor ligands, in this paper we describe the synthesis and structure- activity relationships of a new series of 1,3,5-substituted pyrrole-2-carboxylic acid derivatives 27-40 possessing the structural features for ET receptors binding. New synthesized compounds were tested on ET_A and ET_B receptors stably expressed in CHO cells and some of them showed interesting affinity and selectivity towards ET_A receptors.

Keywords: Endothelins, cardiovascular diseases, ET receptors, binding assays, 1, 3, 5-substituted pyrroles.