| Literature DB >> 21236687 |
Jin Xie1, Gennadiy I Poda, Yiding Hu, Natalie X Chen, Richard F Heier, Serge G Wolfson, Matthew T Reding, Patrick J Lennon, Ravi G Kurumbail, Shaun R Selness, Xiong Li, Nandini N Kishore, Cynthia D Sommers, Lori Christine, Sheri L Bonar, Neetu Venkatraman, Sumathy Mathialagan, Sarah J Brustkern, Horng-Chih Huang.
Abstract
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).Entities:
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Year: 2010 PMID： 21236687 DOI： 10.1016/j.bmc.2010.12.027
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641