Synthesis and structure--activity relationships of aroylpyrrole alkylamide bradykinin (B2) antagonists.
The synthesis and structure-activity relationships of a novel series of aroylpyrrole alkylamides as potent selective bradykinin B(2) receptor antagonists are described. Several members of this series display nanomolar affinity at the B(2) receptor and show activity in an animal model of antinociception.
Youngman
Mark A
MA
Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA.
Carson
John R
JR
Lee
Jung S
JS
Dax
Scott L
SL
Zhang
Sui-Po
SP
Colburn
Ray W
RW
Stone
Dennis J
DJ
Codd
Ellen E
EE
Jetter
Michele C
MC
D000473:Alkanes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D065168:Bradykinin Receptor Antagonists; D007202:Indicators and Reagents; D007509:Irritants / Q000037:antagonists & inhibitors; D007616:Kaolin; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D043782:Receptor, Bradykinin B2; D013329:Structure-Activity Relationship
D000473:Alkanes; D000700:Analgesics; D065168:Bradykinin Receptor Antagonists; D007202:Indicators and Reagents; D007509:Irritants; D011758:Pyrroles; D043782:Receptor, Bradykinin B2; D007616:Kaolin