Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity

被引：28

作者：

Angeli, Andrea ^{[1
,2
]}

Etxebeste-Mitxeltorena, Mikel ^{[3
]}

Sanmartin, Carmen ^{[3
]}

Espuelas, Socorro ^{[3
]}

Moreno, Esther ^{[3
]}

Azqueta, Amaya ^{[3
]}

Parkkila, Seppo ^{[4
,5
]}

Carta, Fabrizio ^{[1
]}

Supuran, Claudiu T. ^{[1
]}

机构：

[1] Univ Florence, NEUROFARBA Dept, Sez Sci Farmaceut & Nutraceut, I-50019 Florence, Italy

[2] Petru Poni Inst Macromol Chem, Ctr Adv Res Bionanoconjugates & Biopolymers Dept, Iasi 700487, Romania

[3] Univ Navarra, Sch Pharm & Nutr, Dept Pharmaceut Technol & Chem, Pamplona 31008, Spain

[4] Univ Tampere, Fac Med & Life Sci, Tampere 33100, Finland

[5] Tampere Univ Hosp, Fimlab Ltd, Tampere 33100, Finland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2020年 / 63卷 / 08期

关键词：

ACTIVATION;

D O I：

10.1021/acs.jmedchem.0c00211

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report for the first time a novel series of tellurides bearing sulfonamide as selective and potent inhibitors of the beta-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 mu M 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.

引用

页码：4306 / 4314

页数：9

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