1293979-51-7Relevant articles and documents
Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs
Young, Robert J.,Adams, Carl,Blows, Mike,Brown, David,Burns-Kurtis, Cynthia L.,Chan, Chuen,Chaudry, Laiq,Convery, Máire A.,Davies, David E.,Exall, Anne M.,Foster, Graham,Harling, John D.,Hortense, Eric,Irvine, Stephanie,Irving, Wendy R.,Jackson, Steve,Kleanthous, Savvas,Pateman, Anthony J.,Patikis, Angela N.,Roethka, Theresa J.,Senger, Stefan,Stelman, Gary J.,Toomey, John R.,West, Robert I.,Whittaker, Caroline,Zhou, Ping,Watson, Nigel S.
, p. 1582 - 1587 (2011/05/05)
The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with excellent oral pharmacokinetic profiles; however, significant time dependant P450 inhibition was an issue for the aminoindane series, but this was not observed with the phenylpyrrolidine motif, which produced candidate quality molecules with potential for once-daily oral dosing in humans.
