Novel amidine-containing peptidyl phosphonates as irreversible inhibitors for blood coagulation and related serine proteases
J Oleksyszyn, B Boduszek, CM Kam…
Index: Oleksyszyn, Jozef; Boduszek, Bogdan; Kam, Chih-Min; Powers, James C. Journal of Medicinal Chemistry, 1994 , vol. 37, # 2 p. 226 - 231
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Citation Number: 96
Abstract
A series of new peptidyl (a-aminoalky1) phosphonate diphenyl esters containing the 4- amidinophenyl group were synthesized and tested as irreversible inhibitors for thrombin and other trypsin-like enzymes. These phosphonates irreversibly inhibited several coagulation enzymes and trypsin. Boc-~-Phe-Pro-(4-AmPhGly)~(OPh) 2 is the best human thrombin inhibitor in the series with ak, b $[I] value of 11 000 Ml sl, and it inhibits thrombin more than ...
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