Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

Loredana Salerno; Maria N. Modica; Giuseppe Romeo; Valeria Pittalà; Alfredo Cagnotto; Maria A. Siracusa

Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

Loredana Salerno, Maria N. Modica, Giuseppe Romeo, Valeria Pittalà, Alfredo Cagnotto, Maria A. Siracusa

Istituto di Ricerche Farmacologiche "Mario Negri"

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	109-117
Number of pages	9
Journal	Medicinal Chemistry
Volume	11
Issue number	2
Publication status	Published - 2015

Keywords

1,3,5-substituted pyrroles
Binding assays
Cardiovascular diseases
Endothelins
ET receptors

ASJC Scopus subject areas

Drug Discovery
Medicine(all)

Cite this

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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.",

keywords = "1,3,5-substituted pyrroles, Binding assays, Cardiovascular diseases, Endothelins, ET receptors",

author = "Loredana Salerno and Modica, {Maria N.} and Giuseppe Romeo and Valeria Pittal{\`a} and Alfredo Cagnotto and Siracusa, {Maria A.}",

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journal = "Medicinal Chemistry",

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T1 - Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

AU - Salerno, Loredana

AU - Modica, Maria N.

AU - Romeo, Giuseppe

AU - Pittalà, Valeria

AU - Cagnotto, Alfredo

AU - Siracusa, Maria A.

PY - 2015

Y1 - 2015

N2 - 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.

AB - 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.

KW - 1,3,5-substituted pyrroles

KW - Binding assays

KW - Cardiovascular diseases

KW - Endothelins

KW - ET receptors

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SN - 1573-4064

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Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives

Abstract

Keywords

ASJC Scopus subject areas

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