کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361683 | 981469 | 2011 | 14 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure–activity relationship Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure–activity relationship](/preview/png/1361683.png)
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).
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 with potential capability for multiple routes of clearance. Several lead compounds have demonstrated their potential usefulness in the treatment of asthma and chronic obstructive pulmonary disease (COPD).Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 3, 1 February 2011, Pages 1242–1255