PMID:18054228

Citation	Young, RJ, Borthwick, AD, Brown, D, Burns-Kurtis, CL, Campbell, M, Chan, C, Charbaut, M, Chung, CW, Convery, MA, Kelly, HA, Paul King, N, Kleanthous, S, Mason, AM, Pateman, AJ, Patikis, AN, Pinto, IL, Pollard, DR, Senger, S, Shah, GP, Toomey, JR, Watson, NS and Weston, HE (2008) Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs. Bioorg. Med. Chem. Lett. 18:23-7
Abstract	Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups, producing highly potent inhibitors with encouraging oral pharmacokinetic profiles and significant but sub-optimal anticoagulant activities.
Links	PubMed Online version:10.1016/j.bmcl.2007.11.023
Keywords	Animals; Anticoagulants/chemistry; Anticoagulants/pharmacokinetics; Anticoagulants/pharmacology; Drug Design; Factor Xa/antagonists & inhibitors; 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; Structure-Activity Relationship; Sulfonamides/chemistry; Sulfonamides/pharmacokinetics; Sulfonamides/pharmacology
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