Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 1, Pages 137-140Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.010
Keywords
PDE4; COPD; Quinoline; Cinnoline; Cynomolgus monkey; PK
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Species specific conversion of the lead PDE4 inhibitor 1 to the quinolone 3 was identified as the major route of metabolism in the cynomolgus monkey. Modification of the template to give the cinnoline 9 retained potency and selectivity, and greatly improved the pharmacokinetic pro. le in the cynomolgus monkey compared with 1. Additional SAR studies aimed at improving the solubility of 9 are also described. (C) 2009 Elsevier Ltd. All rights reserved.
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