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

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)109-117
Number of pages9
JournalMedicinal Chemistry
Volume11
Issue number2
Publication statusPublished - 2015

Fingerprint

Endothelin Receptors
Ligands
CHO Cells
Structure-Activity Relationship
Pulmonary Hypertension
Renal Insufficiency
Atherosclerosis
Heart Failure
Myocardial Infarction
Research Personnel
Research
2-pyrrolecarboxylic acid
Therapeutics

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Medicine(all)

Cite this

Salerno, L., Modica, M. N., Romeo, G., Pittalà, V., Cagnotto, A., & Siracusa, M. A. (2015). Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives. Medicinal Chemistry, 11(2), 109-117.

Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives. / Salerno, Loredana; Modica, Maria N.; Romeo, Giuseppe; Pittalà, Valeria; Cagnotto, Alfredo; Siracusa, Maria A.

In: Medicinal Chemistry, Vol. 11, No. 2, 2015, p. 109-117.

Research output: Contribution to journalArticle

Salerno, L, Modica, MN, Romeo, G, Pittalà, V, Cagnotto, A & Siracusa, MA 2015, 'Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives', Medicinal Chemistry, vol. 11, no. 2, pp. 109-117.
Salerno, Loredana ; Modica, Maria N. ; Romeo, Giuseppe ; Pittalà, Valeria ; Cagnotto, Alfredo ; Siracusa, Maria A. / Synthesis and endothelin receptors binding affinity of new 1,3,5- Substituted Pyrrole-2-Carboxylic Acid Derivatives. In: Medicinal Chemistry. 2015 ; Vol. 11, No. 2. pp. 109-117.
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