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 ...

~86%

Molecular design and structure–activity relationships leadin...

[Das, Jagabandhu; Kimball; Hall, Steven E.; Han, Wen-Ching; Iwanowicz, Edwin; Lin, James; Moquin, Robert V.; Reid, Joyce A.; Sack, John S.; Malley, Mary F.; Chang, Chiehying Y.; Chong, Saeho; Wang-Iverson, David B.; Roberts, Daniel G.M.; Seiler, Steven M.; Schumacher, William A.; Ogletree, Martin L. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 1 p. 45 - 49]

Total synthesis of the marine-derived cyclic depsipeptide al...

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