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发现用于局部治疗牛皮癣的新型PDE4抑制剂，小鼠、大鼠和人肝微粒体的代谢稳定性实验通过z6尊龙测定

2023-06-28
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2-PDE4-is-an-effective-target-for-the-treatment-of-inflammatory-diseases-such-as-psoriasis--1.jpg

Psoriasis is a common immune-mediated skin disorder manifesting in abnormal skin plaques, and PDE4 is an effective target for the treatment of inflammatory diseases such as psoriasis.

Researchers designed and synthesized the lead compound with high PDE4 inhibitory potency and remarkable metabolite profiles in liver microsomes.The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon.

Reference

Zhendong Song, et al. Discovery and Structural Optimization of Toddacoumalone Derivatives as Novel PDE4 Inhibitors for the Topical Treatment of Psoriasis. J Med Chem. 2022 Mar 10;65(5):4238-4254. doi: 10.1021/acs.jmedchem.1c02058.

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