Abstract
The interest of researchers for ligands of the endothelin receptors ETA and ETB 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 ETA and ETB receptors stably expressed in CHO cells and some of them showed interesting affinity and selectivity towards ETA receptors.
Keywords: Endothelins, cardiovascular diseases, ET receptors, binding assays, 1, 3, 5-substituted pyrroles.
Medicinal Chemistry
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 ETA and ETB 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 ETA and ETB receptors stably expressed in CHO cells and some of them showed interesting affinity and selectivity towards ETA receptors.
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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
DOI https://dx.doi.org/10.2174/1573406410666140917160653 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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