Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease,Bioorganic & Medicinal Chemistry Letters

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Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-08-13 , DOI: 10.1016/j.bmcl.2022.128942
Jonathan S Foot ₁ , Alberto Buson ₁ , Mandar Deodhar ₁ , Alison D Findlay ₁ , Alan D Robertson ₁ , Craig I Turner ₁ , Tin Yow ₁ , Wenbin Zhou ₁ , Wolfgang Jarolimek ₁

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The discovery of a dual MAO-B/SSAO inhibitor PXS-5131 is reported. The compound offers a compact and rigid three-dimensional structure with superior selectivity over MAO-A. Potency and selectivity are linked to both the double bond geometry and stereochemistry of the allylamine moiety, highlighting the importance of optimal set up of these features in the class of amine oxidase inhibitors. PXS-5131 possesses an attractive preclinical pharmacokinetic profile and has anti-inflammatory properties in models of acute inflammation and neuroinflammation.

中文翻译：

结合单胺氧化酶 B 和氨基脲敏感的胺氧化酶抑制来治疗炎症性疾病

据报道，发现了双重 MAO-B/SSAO 抑制剂PXS-5131 。与 MAO-A 相比，该化合物具有紧凑且刚性的三维结构，具有更高的选择性。效力和选择性与烯丙胺部分的双键几何形状和立体化学有关，突出了在胺氧化酶抑制剂类中优化设置这些特征的重要性。PXS-5131具有有吸引力的临床前药代动力学特征，并在急性炎症和神经炎症模型中具有抗炎特性。

更新日期：2022-08-13

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