Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity.,Journal of Medicinal Chemistry

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Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-04-09 , DOI: 10.1021/acs.jmedchem.0c00211
Andrea Angeli _{1,

2} , Mikel Etxebeste-Mitxeltorena ₃ , Carmen Sanmartín ₃ , Socorro Espuelas ₃ , Esther Moreno ₃ , Amaya Azqueta ₃ , Seppo Parkkila ₄ , Fabrizio Carta ₁ , Claudiu T Supuran ₁

Affiliation

We report for the first time a novel series of tellurides bearing sulfonamide as selective and potent inhibitors of the β-class carbonic anhydrase (CA; EC 4.2.1.1) enzyme expressed in Leishmania donovani protozoa. Such derivatives showed high activity against axenic amastigotes, and among them, compound 5g (4-(((3,4,5-trimethoxyphenyl)tellanyl)methyl)benzenesulfonamide) showed an IC50 of 0.02 μM being highly selective for the parasites over THP-1 cells with a selectivity index of 300. The in vitro and in vivo toxicity experiments showed compound 5g to possess a safe profile and thus paving the way for tellurium-containing compounds as novel drug entities.

中文翻译：

带有磺酰胺类的碲化物作为具有有效抗leishmanmanial活性的leishmanial碳酸酐酶的新型抑制剂。

我们首次报道了一系列新的含碲酰胺的碲化物，它们是在利什曼原虫中的β-类碳酸酐酶（CA； EC 4.2.1.1）酶的选择性和有效抑制剂。此类衍生物显示出对抗苯磺酸线虫的高活性，其中化合物5g（4-（（（（3,4,5-三甲氧基苯基）tellanyl）甲基）苯磺酰胺）的IC50为0.02μM，对THP- 1个细胞的选择性指数为300。体外和体内毒性实验表明，化合物5g具有安全特性，因此为含碲化合物作为新型药物实体铺平了道路。

更新日期：2020-04-24

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