Bioorganic and medicinal chemistry letters (2020)
Update date:2022-08-17
Topics:
Chen, Dawei
Jiang, Yuyang
Li, Anqi
Liu, Zijian
Lu, Kuan
Wu, Weibin
Xiao, Boren
Yuan, Zigao
Zhai, Xin
Zhang, Cunlong
Small molecule JAK inhibitors have been demonstrated efficacy in rheumatoid arthritis, inflammatory bowel disease, and psoriasis with the approval of several drugs. Aiming to develop potent JAK1/2 inhibitors, two series of triazolo [1,5-a] pyridine derivatives were designed and synthesized by various strategies. The pharmacological results identified the optimized compounds J-4 and J-6, which exerted high potency against JAK1/2, and selectivity over JAK3 in enzyme assays. Furthermore, J-4 and J-6 effectively suppressed proliferation of JAK1/2 high-expression BaF3 cells accompanied with acceptable metabolic stability in liver microsomes. Therefore, J-4 and J-6 might serve as promising JAK1/2 inhibitors for further investigation.
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