期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 19, 页码 5803-5806出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.111
关键词
VLA-4; Antagonist; Multiple scelerosis
A series of prolyl-N-isonicotinoyl-(L)-4-aminophenylalanine derivatives substituted at the proline 4-position with cyclic amines was evaluated as VLA-4 antagonists. The ring size and presence or absence of fluorine affected potency and receptor occupancy. The analog with 3,3-difluoropiperidine at the proline 4-position (13) was the most potent compound and had very good duration of receptor occupancy in vitro. The ethyl ester prodrug of 13 demonstrated excellent receptor occupancy after oral dosing in rats. (C) 2009 Elsevier Ltd. All rights reserved.
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