Endothelin receptor antagonists: synthesis and structure-activity relationships of substituted benzothiazine-1,1-dioxides.
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.
Berryman
K A
KA
Department of Chemistry, Parke-Davis Pharmaceutical Research, Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Edmunds
J J
JJ
Bunker
A M
AM
Haleen
S
S
Bryant
J
J
Welch
K M
KM
Doherty
A M
AM
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D004149:Dioxoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065128:Endothelin Receptor Antagonists; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D004149:Dioxoles; D065128:Endothelin Receptor Antagonists; C116380:PD 164800; D011994:Recombinant Proteins; D013843:Thiazines