Amidines as amide bond replacements in VLA-4 antagonists

VLA-4 (alpha(4)beta(1), very late activating antigen-4), a key cell surface integrin plays an important role in inflammation by promoting leukocyte attachment and extravasation from the vasculature into the peripheral tissues. As such, VLA-4 antagonists may be useful in the treatment, prevention, an...

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Published in:Bioorganic & medicinal chemistry letters 2004-05, Vol.14 (9), p.2323-2326
Main Authors: KAMENECKA, Theodore M, PARK, You-Jung, WEI TANG, COLLETTI, Adria, TEFFERA, Yohannes, STEARNS, Ralph, MACCOSS, Malcolm, SCHMIDT, John A, HAGMANN, William K, LIN, Linus S, DE LASZLO, Stephen, MCCAULEY, Ermengilda D, VAN RIPER, Gail, EGGER, Linda, KIDAMBI, Usha, MUMFORD, Richard A, TONG, Sharon
Format: Article
Language:English
Subjects:
Amides - chemistry
Amidines - chemistry
Area Under Curve
Biological and medical sciences
Integrin alpha4beta1 - antagonists & inhibitors
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
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Summary:VLA-4 (alpha(4)beta(1), very late activating antigen-4), a key cell surface integrin plays an important role in inflammation by promoting leukocyte attachment and extravasation from the vasculature into the peripheral tissues. As such, VLA-4 antagonists may be useful in the treatment, prevention, and suppression of diseases where cell adhesion and migration are important such as asthma, rheumatoid arthritis, and multiple sclerosis. Herein, we report on the discovery, synthesis, and biological evaluation of amidines as small molecule antagonists of VLA-4.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.01.100