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Bioorg Med Chem. 2011 Feb 1;19(3):1242-55. doi: 10.1016/j.bmc.2010.12.027. Epub 2010 Dec 23.

Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.

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Department of Medicinal Chemistry, Pfizer Inc., 700 Chesterfield Parkway West, St. Louis, MO 63017, USA.


Installation of sites for metabolism in the lead compound PHA-767408 was the key focus of the IKK-2 inhaled program. This paper reports our efforts to identify a novel series of aminopyridinecarboxamide-based IKK-2 inhibitors, which display low nanomolar potency against IKK-2 with long duration of action (DOA), and metabolically labile to phase I and/or phase II metabolizing enzymes with potential capability for multiple routes of clearance. Several compounds have demonstrated their potential usefulness in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

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