Journal of Medicinal Chemistry p. 1727 - 1730 (2007)
Update date:2022-07-30
Topics: nonpeptide inhibitors Discovery Potent Selective Orally Active
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.
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
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