Literature DB >> 19081720

Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.

Ghotas Evindar1, Sylvie G Bernier, Malcolm J Kavarana, Elisabeth Doyle, Jeanine Lorusso, Michael S Kelley, Keith Halley, Amy Hutchings, Albion D Wright, Ashis K Saha, Gerhard Hannig, Barry A Morgan, William F Westlin.   

Abstract

In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally.

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Year:  2008        PMID: 19081720     DOI: 10.1016/j.bmcl.2008.11.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.

Authors:  Hongfeng Deng; Sylvie G Bernier; Elisabeth Doyle; Jeanine Lorusso; Barry A Morgan; William F Westlin; Ghotas Evindar
Journal:  ACS Med Chem Lett       Date:  2013-08-27       Impact factor: 4.345

2.  Crystal structure of diethyl [(4-chloro-anilino)(4-hy-droxy-phen-yl)meth-yl]phospho-nate N,N-di-methyl-formamide monosolvate.

Authors:  Qing-Ming Wang; Ming-Juan Zhu; Jin-Ming Yang; Shan-Shan Wang; Yan-Fang Shang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-08-01
  2 in total

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