Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition
Journal Article
·
· Bioorg. Med. Chem. Lett.
- Pfizer
The structure based drug design, synthesis and structure-activity relationship of a series of C6 sulfur linked triazolopyridine based p38 inhibitors are described. The metabolic deficiencies of this series were overcome through changes in the C6 linker from sulfur to methylene, which was predicted by molecular modeling to be bioisosteric. X-ray of the ethylene linked compound 61 confirmed the predicted binding orientation of the scaffold in the p38 enzyme.
- Research Organization:
- Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1002635
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (2) ; 01, 2010 Vol. 20; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
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