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Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation.
- Source :
-
Bioorganic & Medicinal Chemistry . Feb2023, Vol. 80, pN.PAG-N.PAG. 1p. - Publication Year :
- 2023
-
Abstract
- [Display omitted] A series of pyrazole-fused oleanolic acid derivatives were designed and synthesized. The modification of these analogues focused on the substituents screening on the pyrazole ring. The cytotoxicity of these compounds and their anti-inflammatory activities via inhibiting interleukin-1β (IL-1β) production were evaluated in RAW264.7 cells. Most of the derivatives showed significantly improved potency compared with oleanolic acid. Among them, compound 7n exhibited the most potent anti-inflammatory activity on decreasing IL-1β production with low cytotoxicity. Moreover, the further study found 7n could inhibit RANKL-induced osteoclast differentiation on bone marrow-derived macrophages (BMMs). These findings may provide a potential direction for the drug development of osteoarthritis. [ABSTRACT FROM AUTHOR]
- Subjects :
- *BIOSYNTHESIS
*ANTI-inflammatory agents
*DRUG development
*PYRAZOLES
*OSTEOARTHRITIS
Subjects
Details
- Language :
- English
- ISSN :
- 09680896
- Volume :
- 80
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 161721408
- Full Text :
- https://doi.org/10.1016/j.bmc.2023.117177