Orally available and efficacious α4β1/α4β7 integrin inhibitors

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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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-08, Vol.23 (15), p.4370-4373
Hauptverfasser:	Xu, Ying-zi, Smith, Jenifer L., Semko, Christopher M., Rossiter, Kassandra I., Fukuda, Juri Y., Dappen, Michael S., Quincy, David A., Konradi, Andrei W., Mao, Wenxian, Welch, Brent, Dreyer, Mark L., Samant, Bhushan, Zhang, Hongbin, Lugar, Judevin, Liao, Zhenmei, Henschel, Carrol, Petersen, Eric, Vandevert, Christopher, Shoemaker, Mark, Wehner, Nancy, Mutter, Linda, Shopp, George, Krimm, Michael, Chen, Linda, Wipke, Brian, Dofiles, Lilibeth, Gallager, Ian, Sauer, John-Michael, Messersmith, Elizabeth K., Pleiss, Michael A., Bard, Frederique, Yednock, Ted A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral animal models Animals Area Under Curve Arthritis, Rheumatoid - chemically induced Arthritis, Rheumatoid - drug therapy chemistry Crohn Disease - drug therapy Disease Models, Animal Half-Life Humans Integrin alpha4beta1 - antagonists & inhibitors Integrin alpha4beta1 - metabolism integrins Integrins - antagonists & inhibitors Integrins - metabolism Jurkat Cells Microsomes, Liver - metabolism oral exposure Rats rheumatoid arthritis
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.05.076