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Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Owen, Dafydd Walker, John K. Jacobsen, E. Jon Freskos, John N. Hughes, Robert Owen Brown, David L. Bell, Andrew Simon Brown, Dean G. Phillips, Christopher Mischke, Brent V. Molyneaux, John M. Fobian, Yvette M. Heasley, Steve E. Moon, Joseph B. Stallings, William C. Rogier, D. Joseph Fox, David A. Palmer, Michael John Ringer, Tracy J. Rodriquez-Lens, Margarita Cubbage, Jerry W. Blevis-Bal, Radhika M. Benson, Alan G. Acker, Brad A. Maddux, Todd Michael Tollefson, Michael Brent Bond, Brian R. Macinnes, Alan Yu, Yung Hoon |
| Copyright Year | 2009 |
| Abstract | A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which show potent inhibition of the PDE5 enzyme. Synthetic details and some structure-activity relationships are also presented. |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/j.bmcl.2009.06.012 |
| PubMed reference number | 19540112 |
| Journal | Medline |
| Volume Number | 19 |
| Issue Number | 15 |
| Alternate Webpage(s) | https://kar.kent.ac.uk/34240/1/j_bmcl_2009_06_012.pdf |
| Alternate Webpage(s) | https://doi.org/10.1016/j.bmcl.2009.06.012 |
| Journal | Bioorganic & medicinal chemistry letters |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
