Novel benzo-fused lactam scaffolds as factor Xa inhibitors.
Rigid benzolactam P3-P2 dipeptide mimics were designed and prepared as potential inhibitors of blood coagulation factor Xa. Methoxy substitution of the tetrahydrobenzazepinone scaffold led to potent and selective inhibitors. The synthesis and biological activities of these derivatives are reported herein.
Tamura
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SY
Corvas International, Inc., Department of Medicinal Chemistry, San Diego, California 92121, USA.
Goldman
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EA
Bergum
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PW
Semple
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JE
D015195:Drug Design; D065427:Factor Xa Inhibitors; D007769:Lactams / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D065427:Factor Xa Inhibitors; D007769:Lactams; D015842:Serine Proteinase Inhibitors