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Your search keyword '"Plasma Kallikrein antagonists & inhibitors"' showing total 2 results
Start Over Descriptor "Plasma Kallikrein antagonists & inhibitors" Journal chemical pharmaceutical bulletin
2 results on '"Plasma Kallikrein antagonists & inhibitors"'

1. Structure-inhibitory activity relationship of plasmin and plasma kallikrein inhibitors.

Author

Tsuda Y, Tada M, Wanaka K, Okamoto U, Hijikata-Okunomiya A, Okamoto S, and Okad Y

Subjects
Amines chemistry, Animals, Cattle, Fibrinolysis, Humans, Structure-Activity Relationship, Thrombin chemistry, Trypsin chemistry, Urokinase-Type Plasminogen Activator chemistry, Enzyme Inhibitors chemistry, Fibrinolysin chemistry, Plasma Kallikrein antagonists & inhibitors
Abstract

Based on the structure of Tra-Tyr(O-Pic)-octylamide, a portion of the octylamine was replaced with moieties bearing hydrophobic, basic or acidic groups. Replacement of the C-terminal residue with a moiety bearing a hydrophobic group gave the proper affinity of the inhibitor to both plasmin (PL) and plasma kallikrein (PK). While addition of a basic residue did not improve the affinity of the inhibitor, a carboxylic acid attached to the phenyl ring increased the PK selectivity of the inhibitor.

Published
2001
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2. Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship.

Author

Okada Y, Tsuda Y, Tada M, Wanaka K, Okamoto U, Hijikata-Okunomiya A, and Okamoto S

Subjects
Antifibrinolytic Agents chemistry, Antifibrinolytic Agents pharmacology, Fibrinolysin antagonists & inhibitors, Humans, Inhibitory Concentration 50, Protease Inhibitors chemistry, Protease Inhibitors pharmacology, Structure-Activity Relationship, Thrombin antagonists & inhibitors, Urokinase-Type Plasminogen Activator antagonists & inhibitors, Antifibrinolytic Agents chemical synthesis, Plasma Kallikrein antagonists & inhibitors, Protease Inhibitors chemical synthesis
Abstract

Based on structure-activity relationship studies, we designed and synthesized plasmin (PL) and plasma kallikrein (PK) inhibitors. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-Pic)-octylamide inhibited PL, PK, urokinase (UK) and thrombin (TH) with IC50 values of 0.53, 30, 5.3 and > 400 microm, respectively. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide inhibited PL, PK, UK and TH with IC50 values of 36, 0.56, 440 and > 1,000 microM, respectively.

Published
2000
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