Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, the benzamidine functionality was identified as the most potent charged group investigated.
Dener
J M
JM
Departments of Medicinal Chemistry, Biochemistry, and Enzymology, Axys Pharmaceuticals, Inc., 180 Kimball Way, South 94080, San Francisco, CA, USA. dener@chemrx.com
Rice
K D
KD
Newcomb
W S
WS
Wang
V R
VR
Young
W B
WB
Gangloff
A R
AR
Kuo
E Y
EY
Cregar
L
L
Putnam
D
D
Wong
M
M
D001550:Benzamidines / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008407:Mast Cells / Q000201:enzymology*; D012697:Serine Endopeptidases / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053802:Tryptases
D001550:Benzamidines; D004791:Enzyme Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases