title: Synthesis and endothelin receptors binding affinity of new 1,3,5- substituted pyrrole-2-carboxylic acid derivatives.
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.
authors.forename: Loredana
authors.initials: L
authors.lastname: Salerno
authors.forename: Maria N
authors.initials: MN
authors.lastname: Modica
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Romeo
authors.forename: Valeria
authors.initials: V
authors.lastname: Pittala
authors.forename: Alfredo
authors.initials: A
authors.lastname: Cagnotto
authors.affiliation: Dipartimento di Scienze del Farmaco, Universita degli Studi di Catania, Viale A. Doria, 6, 95125 - Catania, Italy. mmodica@unict.it.
authors.forename: Maria A
authors.initials: MA
authors.lastname: Siracusa
mesh_terms: D000818:Animals; D016466:CHO Cells; D003412:Cricetulus; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D011392:Proline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011485:Protein Binding; D044022:Receptor, Endothelin A / Q000235:genetics / Q000378:metabolism*; D044023:Receptor, Endothelin B / Q000235:genetics / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; C002986:2-pyrrolecarboxylic acid; D011392:Proline