دورية أكاديمية
Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae
| العنوان: | Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae |
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| المؤلفون: | Alessio Nocentini, Chad S. Hewitt, Margaret D. Mastrolorenzo, Daniel P. Flaherty, Claudiu T. Supuran |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1061-1066 (2021) |
| بيانات النشر: | Taylor & Francis Group, 2021. |
| سنة النشر: | 2021 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | carbonic anhydrase, inhibitor, anion, neisseria gonorrhoeae, dithiocarbamate, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | The bacterial pathogen Neisseria gonorrhoeae encodes for an α-class carbonic anhydrase (CA, EC 4.2.1.1), NgCA, which was investigated for its inhibition with a series of inorganic and organic anions. Perchlorate and hexafluorophosphate did not significantly inhibit NgCA CO2 hydrase activity, whereas the halides, azide, bicarbonate, carbonate, stannate, perosmate, diphosphate, divanadate, perruthenate, and trifluoromethanesulfonate showed inhibition constants in the range of 1.3–9.6 mM. Anions/small molecules such as cyanate, thiocyanate, nitrite, nitrate, bisulphite, sulphate, hydrogensulfide, phenylboronic acid, phenylarsonic acid, selenate, tellurate, tetraborate, perrhenate, peroxydisulfate, selenocyanate, iminodisulfonate, and fluorosulfonate showed KIs in the range of 0.15–1.0 mM. The most effective inhibitors detected in this study were sulfamide, sulfamate, trithiocarbonate and N,N-diethyldithiocarbamate, which had KIs in the range of 5.1–88 µM. These last compounds incorporating the CS2- zinc-binding group may be used as leads for developing even more effective NgCA inhibitors in addition to the aromatic/heterocyclic sulphonamides, as this enzyme was recently validated as an antibacterial drug target for obtaining novel antigonococcal agents |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1475-6366 1475-6374 14756366 |
| Relation: | https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374 |
| DOI: | 10.1080/14756366.2021.1929202 |
| URL الوصول: | https://doaj.org/article/17b4898b97d74981b8db84dbdf49ee91 |
| رقم الأكسشن: | edsdoj.17b4898b97d74981b8db84dbdf49ee91 |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2021.1929202 |