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N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.

Authors :
Li B
de Laszlo SE
Kamenecka TM
Kopka IE
Durette PL
Lanza T Jr
MacCoss M
Tong S
Mumford RA
McCauley ED
Van Riper G
Schmidt JA
Hagmann WK
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Aug 19; Vol. 12 (16), pp. 2141-4.
Publication Year :
2002

Abstract

A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC(50) <1 nM). Evaluation of rat pharmacokinetic revealed generally high clearance.

Details

Language :
English
ISSN :
0960-894X
Volume :
12
Issue :
16
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
12127523
Full Text :
https://doi.org/10.1016/s0960-894x(02)00366-9