benzothiazinone

Macozinone (PBTZ169) 是具有杀菌作用的苯并噻嗪酮，也有抗结核作用。它也是一种 DprE1有效抑制剂，可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。

BTZ043 Racemate (Benzothiazinone 10526038) 是一种癸二烯基磷酰-β-D-核糖 2'-差向异构酶(DprE1) 抑制剂，用作新的抗分枝杆菌剂。

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

Antitubercular agent-32 是Benzothiazinone 衍生物，对结核分枝杆菌 M. tuberculosis 具有抑制作用，并表现出良好的代谢稳定性及水溶性。 Antitubercular agent-32 可以作用于 decaprenylphosphoryl-β-D-ribose 2'-氧化酶 (DprE1,IC50: 3.9 μM)，表现出抗结核效果。