Orally available and efficacious α4β1/α4β7 integrin inhibitors. Ying-zi Xu , Jenifer L Smith , Christopher M Semko , Kassandra I Rossiter , Juri Y Fukuda , Michael S Dappen , David A Quincy , Andrei W Konradi , Wenxian Mao , Brent Welch , Mark L Dreyer , Bhushan Samant , Hongbin Zhang , Judevin Lugar , Zhenmei Liao , Carrol Henschel , Eric Petersen , Christopher Vandevert , Mark Shoemaker , Nancy Wehner , Linda Mutter , George Shopp , Michael Krimm , Linda Chen , Brian Wipke , Lilibeth Dofiles , Ian Gallager , John-Michael Sauer , Elizabeth K Messersmith , Michael A Pleiss , Frederique Bard , Ted A Yednock Bioorganic & Medicinal Chemistry Letters（2013）
摘要
A series of potent α4β1/α4β7 integrin inhibitors is reported, including an inhibitor 12d with remarkable oral exposure and efficacy in rat models of rheumatoid arthritis and Crohn’s disease.
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