Endothelin receptor antagonists: synthesis and structure-activity relationships of substituted benzothiazine-1,1-dioxides

K A Berryman; J J Edmunds; A M Bunker; S Haleen; J Bryant; K M Welch; A M Doherty

doi:10.1016/s0968-0896(98)00080-7

Endothelin receptor antagonists: synthesis and structure-activity relationships of substituted benzothiazine-1,1-dioxides

Bioorg Med Chem. 1998 Sep;6(9):1447-56. doi: 10.1016/s0968-0896(98)00080-7.

Authors

K A Berryman¹, J J Edmunds, A M Bunker, S Haleen, J Bryant, K M Welch, A M Doherty

Affiliation

¹ Department of Chemistry, Parke-Davis Pharmaceutical Research, Warner-Lambert Company, Ann Arbor, MI 48105, USA.

PMID: 9801816
DOI: 10.1016/s0968-0896(98)00080-7

Abstract

The development of benzothiazine-1,1-dioxide derivatives as a new structural class of potent endothelin receptor antagonists is described. Structure-activity relationships (SAR) revealed that PD164800 (1) is a potent antagonist of the ETA receptor subtype.

MeSH terms

Animals
CHO Cells
Cricetinae
Dioxoles / chemical synthesis*
Dioxoles / chemistry
Dioxoles / pharmacology
Endothelin Receptor Antagonists*
Humans
Magnetic Resonance Spectroscopy
Recombinant Proteins / antagonists & inhibitors
Structure-Activity Relationship
Thiazines / chemical synthesis*
Thiazines / chemistry
Thiazines / pharmacology

Substances

Dioxoles
Endothelin Receptor Antagonists
PD 164800
Recombinant Proteins
Thiazines