Investigation of the terminal P4 domain in a series of d-phenylglycinamide-based factor Xa inhibitors

Several P4 domain derivatives of the d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. An additional subset containing various P1 indole constructs was evaluated for their oral exposure properties.