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2005
Lipids
U 0750
03- 201
Synthesis of Benzimidazole Based Analogues of Sphingosine-1-phosphate: Discovery of Potent, Subtype-Selective S1P4 Receptor Agonists. — Sphingosine-1-phosphate analogues incorporating a benzimidazole ring system in the 'linker' region of the
pharmacophore are synthesized. Interestingly, the synthesis of structures of type (VI)
involves a condensation-cyclization-dehydration event promoted by the PyBOP reagent. Compound (X) is a highly potent and fully efficacious S1P4 receptor selective
agonist. A slight preference in potency for the 2S-configuration is observed. Also, to
achieve significant potency, a phosphate head group is necessary. Furthermore, a reasonable toleration of 1-methylation of the benzimidazole analogues is demonstrated
whereas 2-methylation causes a drastic loss in agonism. — (CLEMENS*, J. J.;
DAVIS, M. D.; LYNCH, K. R.; MACDONALD, T. L.; Bioorg. Med. Chem. Lett. 14
(2004) 19, 4903-4906; Dep. Chem., Univ. Va., Charlottesville, VA 22903, USA;
Eng.) — H. Hoennerscheid
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