Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists

Haripada Khatuya; Richard H Hutchings; Gee-Hong Kuo; Virginia L Pulito; Linda K Jolliffe; Xiaobing Li; William V Murray

doi:10.1016/s0960-894x(02)00436-5

Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2443-6. doi: 10.1016/s0960-894x(02)00436-5.

Authors

Haripada Khatuya¹, Richard H Hutchings, Gee-Hong Kuo, Virginia L Pulito, Linda K Jolliffe, Xiaobing Li, William V Murray

Affiliation

¹ Drug Discovery Research, Johnson & Johnson Pharmaceutical Research and Development LLC, Raritan, NJ 08869, USA.

PMID: 12161153
DOI: 10.1016/s0960-894x(02)00436-5

Abstract

Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.

MeSH terms

Adrenergic Antagonists / chemical synthesis*
Adrenergic Antagonists / pharmacology
Adrenergic alpha-1 Receptor Antagonists*
Heterocyclic Compounds, 4 or More Rings / chemical synthesis
Heterocyclic Compounds, 4 or More Rings / pharmacology
Humans
Isoxazoles
Piperazines / chemical synthesis
Piperazines / pharmacology
Protein Binding
Receptors, Adrenergic, alpha-1
Sensitivity and Specificity
Structure-Activity Relationship

Substances

ADRA1A protein, human
Adrenergic Antagonists
Adrenergic alpha-1 Receptor Antagonists
Heterocyclic Compounds, 4 or More Rings
Isoxazoles
Piperazines
Receptors, Adrenergic, alpha-1