Isoindolines: a new series of potent and selective endothelin-A receptor antagonists

P J Kukkola; N A Bilci; T Ikler; P Savage; S S Shetty; D DelGrande; A Y Jeng

doi:10.1016/s0960-894x(01)00273-6

Isoindolines: a new series of potent and selective endothelin-A receptor antagonists

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1737-40. doi: 10.1016/s0960-894x(01)00273-6.

Authors

P J Kukkola¹, N A Bilci, T Ikler, P Savage, S S Shetty, D DelGrande, A Y Jeng

Affiliation

¹ Metabolic and Cardiovascular Diseases, Novartis Institute for Biomedical Research, 07901, Summit NJ, USA. paivi.kukkola@pharma.novartis.com

PMID: 11425549
DOI: 10.1016/s0960-894x(01)00273-6

Abstract

1,3-Disubstituted isoindolines have been discovered as a new class of potent functional ET(A) selective receptor antagonists through pharmacophore analysis of existing nonpeptide endothelin antagonists. The structure-activity relationships for both the trans and the cis series of isoindolines are discussed.

MeSH terms

Endothelin Receptor Antagonists*
Indoles / chemistry
Indoles / pharmacology*
Receptor, Endothelin A
Receptors, Endothelin / chemistry

Substances

Endothelin Receptor Antagonists
Indoles
Receptor, Endothelin A
Receptors, Endothelin