Bioorganic and Medicinal Chemistry Letters p. 1741 - 1743 (2011)
Update date:2022-08-02
Topics:
Semko, Christopher M.
Chen, Linda
Dressen, Darren B.
Dreyer, Mark L.
Dunn, Whitney
Farouz, Francine S.
Freedman, Stephen B.
Holsztynska, Elizabeth J.
Jefferies, Michael
Konradi, Andrei W.
Liao, Anna
Lugar, Judevin
Mutter, Linda
Pleiss, Michael A.
Quinn, Kevin P.
Thompson, Thomas
Thorsett, Eugene D.
Vandevert, Christopher
Xu, Ying-Zi
Yednock, Ted A.
A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave 14, a very potent VLA-4 inhibitor which is orally active in a sheep asthma model.
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