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Bioorg Med Chem Lett. 2004 Aug 2;14(15):4069-74.

A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist.

Author information

1
Department of Chemistry, University of Virginia, PO Box 400319, McCormick Road, Charlottesville, VA 22904, USA. bhh4x@virginia.edu

Abstract

A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selectivity at LPA receptors is described. This study has resulted in the development of the first nonhydrolyzable and presumably phosphatase-resistant LPA(3)-selective antagonist reported to date.

PMID:
15225728
DOI:
10.1016/j.bmcl.2004.05.023
[Indexed for MEDLINE]

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