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Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. doi: 10.1016/j.bmcl.2010.07.076. Epub 2010 Jul 21.

The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.

Author information

1
Merck Frosst Centre for Therapeutic Research, 16711 Trans-Canada Hwy, Kirkland, Québec., Canada H9H 3L1. renee_aspiotis@merck.com

Abstract

The SAR study of a series of 6-aryloxymethyl-8-aryl substituted quinolines is described. Optimization of the series led to the discovery of compound 26b, a highly potent (IC50=0.6 nM) and selective PDE4D inhibitor with a 75-fold selectivity over the A, B, and C subtypes and over 18,000-fold selectivity against other PDE family members. Rat pharmacokinetics and tissue distribution are also summarized.

PMID:
20709547
DOI:
10.1016/j.bmcl.2010.07.076
[Indexed for MEDLINE]

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