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p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design |
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| Authors: | Natarajan Swaminathan R Heller Stephen T Nam Kiyean Singh Suresh B Scapin Giovanna Patel Sangita Thompson James E Fitzgerald Catherine E O'Keefe Stephen J |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. ravi_natarajan@merck.com |
| Abstract: | p38 inhibitors based on 3,4-dihydropyrido4,3-d]pyrimidazin-2-one template were synthesized and their SAR explored. Benchmark compounds 30, 35, and 36 were found to be potent against the enzyme. Crystal structure of p38 in complex with 30 indicated a key pi-stacking interaction with the pendant tyrosine residue-35 in the glycine-rich loop. |
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