Synthesis and Endothelin Receptors Binding Affinity of New 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

Title:Synthesis and Endothelin Receptors Binding Affinity of New 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

Volume: 11 Issue: 2

Author(s): Loredana Salerno, Maria N. Modica, Giuseppe Romeo, Valeria Pittala, Alfredo Cagnotto and Maria A. Siracusa

Affiliation:

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

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.

Cite this article as:

Salerno Loredana, Modica N. Maria, Romeo Giuseppe, Pittala Valeria, Cagnotto Alfredo and Siracusa Maria A., Synthesis and Endothelin Receptors Binding Affinity of New 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives, Medicinal Chemistry 2015; 11 (2) . https://dx.doi.org/10.2174/1573406410666140917160653