Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase
A series of β-carboxamido-phosphon(in)ic acids (2) was identified as a new structural motif for obtaining potent inhibitors of human mast cell chymase. For example, 1-naphthyl derivative 5f had an IC50 value of 29 nM and (E)-styryl derivative 6
Greco, Michael N.,Hawkins, Michael J.,Powell, Eugene T.,Almond Jr., Harold R.,De Garavilla, Lawrence,Hall, Jeffrey,Minor, Lisa K.,Wang, Yuanping,Corcoran, Thomas W.,Di Cera, Enrico,Cantwell, Angelene M.,Savvides, Savvas N.,Damiano, Bruce P.,Maryanoff, Bruce E.
p. 1727 - 1730
(2008/02/02)
Regioselective cationic reduction of 2-aryl-1-N-(ethoxycarbonyl)enamines to 2-arylethylamine carbamates
2-Aryl-1-N-carboalkoxyenamines (enamides) are selectively reduced to the corresponding 2-arylethylamine carbamates by Et3SiH in the presence of CF3COOH in excellent yields. The reduction proceeds by addition of hydride at C-1 and the
Masuno, Makoto N,Molinski, Tadeusz F
p. 8263 - 8266
(2007/10/03)
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