PMID:18053714

Citation	Young, RJ, Borthwick, AD, Brown, D, Burns-Kurtis, CL, Campbell, M, Chan, C, Charbaut, M, Convery, MA, Diallo, H, Hortense, E, Irving, WR, Kelly, HA, King, NP, Kleanthous, S, Mason, AM, Pateman, AJ, Patikis, AN, Pinto, IL, Pollard, DR, Senger, S, Shah, GP, Toomey, JR, Watson, NS, Weston, HE and Zhou, P (2008) Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs. Bioorg. Med. Chem. Lett. 18:28-33
Abstract	Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activities and encouraging oral pharmacokinetic profiles.
Links	PubMed Online version:10.1016/j.bmcl.2007.11.019
Keywords	Animals; Anticoagulants/chemistry; Anticoagulants/pharmacokinetics; Anticoagulants/pharmacology; Bicyclo Compounds, Heterocyclic/chemistry; Bicyclo Compounds, Heterocyclic/pharmacokinetics; Bicyclo Compounds, Heterocyclic/pharmacology; Factor Xa/antagonists & inhibitors; Hydrophobic and Hydrophilic Interactions; Male; Models, Molecular; Pyrrolidinones/chemistry; Pyrrolidinones/pharmacokinetics; Pyrrolidinones/pharmacology; Rats; Rats, Sprague-Dawley; Serine Proteinase Inhibitors/chemistry; Serine Proteinase Inhibitors/pharmacokinetics; Serine Proteinase Inhibitors/pharmacology; Stereoisomerism; Structure-Activity Relationship
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