Small molecule inhibitors of plasma kallikrein.
Plasma kallikrein is a serine protease that is involved in pathways of inflammation, complement fixation, coagulation, and fibrinolysis. Herein, we describe the SAR and structural binding modes of a series of inhibitors of plasma kallikrein as well as the pharmacokinetics of a lead analog 11 in rat.
Young
Wendy B
WB
Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. wendy.young@yahoo.com
Rai
Roopa
R
Shrader
William D
WD
Burgess-Henry
Jana
J
Hu
Huiyong
H
Elrod
Kyle C
KC
Sprengeler
Paul A
PA
Katz
Bradley A
BA
Sukbuntherng
Juthamas
J
Mordenti
Joyce
J
D007610:Kallikreins / Q000037:antagonists & inhibitors* / Q000097:blood; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D015842:Serine Proteinase Inhibitors; D007610:Kallikreins