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發現用於局部治療牛皮癬的新型PDE4抑製劑，小鼠、大鼠和人肝微粒體的代謝穩定性實驗通過hjc黄金城測定

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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