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2005
Receptor binding activity
X 0280
Design and Synthesis of Conformationally Constrained 3-(N-alkylamino)propylAcids as Potent Agonists of Sphingosine-1-phosphate (S1P) Recep01- 205 phosphonic
tors. — Analogues of 3-(N-tetradecylamino)propylphosphonic acid, a potent agonist
of S1P receptors, in which the nitrogen and a neighboring carbon atom or a pair of adjacent carbons are tethered with short alkyl chains are synthesized to identify novel
scaffolds for S1P receptor agonists. Three different scaffolds are tolerated for S1P receptor agonists. Further investigations show that the proper incorporation of a phenyl
ring into the long alkyl chains significantly enhances their binding affinities and pyrrolidines (I) and (II) induce a maximal peripheral lowering of lymphocytes. Pyrrolidines (I), (II), and cyclohexane (IV) possess greatly enhanced affinity for S1P1 as
compared to their n-alkyl counterparts, and pyrrolidine (III) and cyclohexane (IV) reveal 30 and 50-fold selectivity of S1P1 over S1P3, respectively. — (YAN*, L.; et al.;
Bioorg. Med. Chem. Lett. 14 (2004) 19, 4861-4866; Dep. Med. Chem., Merck Res.
Lab., Rahway, NJ 07065, USA; Eng.) — H. Hoennerscheid
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