Synthesis of histargin and related compounds and their inhibition of enzymes.
A novel method for the synthesis of histargin and its analogs is described. It includes two kinds of N-alkylation reactions that prevent the formation of side products. The inhibition of enzymes by these compounds was also measured. Some of the compounds strongly inhibited carboxypeptidase B, carboxypeptidase A, carboxypeptidase N (kininase I), and angiotensin converting enzyme.
Moriguchi
M
M
Central Research Laboratories, Takara Shuzo Co., Ltd., Japan.
Umeda
Y
Y
Miyazaki
K
K
Nakamura
T
T
Ogawa
K
K
Kojima
F
F
Iinuma
H
H
Aoyagi
T
T
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors*; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000806:Angiotensin-Converting Enzyme Inhibitors; D006146:Guanidines; D007093:Imidazoles; C043476:histargin; D002268:Carboxypeptidases