Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists

J C Barrow; K L Glass; H G Selnick; R M Freidinger; R S Chang; S S O'Malley; C Woyden

doi:10.1016/s0960-894x(00)00374-7

Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1917-20. doi: 10.1016/s0960-894x(00)00374-7.

Authors

J C Barrow¹, K L Glass, H G Selnick, R M Freidinger, R S Chang, S S O'Malley, C Woyden

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.

PMID: 10987417
DOI: 10.1016/s0960-894x(00)00374-7

Abstract

Several 1,3-diaminocyclopentane linked alpha1a-receptor antagonists were prepared using a divergent chemical strategy that allows for rapid analysis of all stereochemical permutations for their effect on alpha1-receptor binding.

MeSH terms

Adrenergic alpha-1 Receptor Antagonists*
Adrenergic alpha-Antagonists / chemical synthesis*
Adrenergic alpha-Antagonists / pharmacology
Animals
CHO Cells
Cricetinae
Humans
Pyrimidinones / chemical synthesis*
Pyrimidinones / pharmacology
Receptors, Adrenergic, alpha-1 / metabolism

Substances

Adrenergic alpha-1 Receptor Antagonists
Adrenergic alpha-Antagonists
Pyrimidinones
Receptors, Adrenergic, alpha-1