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)
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