Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors

Tanini Damiano; Capperucci Antonella; Ferraroni Marta; Carta Fabrizio; Angeli Andrea; Supuran Claudiu T.

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Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors

机译：直接和直接进入取代烷基硒醇作为新型碳酸酐酶抑制剂

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Functionalised aliphatic selenols, straightforwardly obtained through ring-opening reaction of strained heterocycles, represent a new chemotype acting as carbonic anhydrase inhibitors (CAIs). These compounds showed pronounced selectivity towards the cytosolic human (h) isoforms such as the hCA I, II and VII rather than the membrane tumor associate hCA IX. In addition, we reported for the first time the X-ray crystal structure of an aliphatic selenol bound to the hCA E zinc ion, and that afforded the opportunity to decipher in detail the inhibition mechanism underpinning such a new class of CAIs. In this context selenols are interesting leads worth developing for the obtainment of novel and efficient selective CAIs potentially useful for the management of a variety of diseases including glaucoma, retinitis pigmentosa, epilepsy and arthritis. (C) 2019 Elsevier Masson SAS. All rights reserved.

机译：通过应变杂环的开环反应直接获得的官能化脂族硒醇，代表一种作为碳酸酐酶抑制剂（CAIS）的新化学型。这些化合物对胞质人（H）同种型（例如HCA I，II和VII）显示出明显的选择性，而不是膜肿瘤助剂HCA IX。此外，我们报道了第一次与HCA E锌离子结合的脂族硒醇的X射线晶体结构，并提供了解土的机会，详细解读了支撑了这种新的CAIS的抑制机制。在这种上下文中，Selenols是有趣的，值得开发用于获取新颖和有效的选择性CAIS，可能对各种疾病的管理有用，包括青光眼，视网膜炎，癫痫和关节炎等各种疾病。（c）2019年Elsevier Masson SAS。版权所有。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2020年第2020期|共6页
作者
Tanini Damiano; Capperucci Antonella; Ferraroni Marta; Carta Fabrizio; Angeli Andrea; Supuran Claudiu T.;
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作者单位

Univ Florence Dept Chem Ugo Schiff Via Lastruccia 3-13 I-50019 Sesto Fiorentino Italy;

Univ Florence Dept Chem Ugo Schiff Via Lastruccia 3-13 I-50019 Sesto Fiorentino Italy;

Univ Florence Dept Chem Ugo Schiff Via Lastruccia 3-13 I-50019 Sesto Fiorentino Italy;

Dept Univ Florence NEUROFARBA Dept Sez Sci Farmaceut Via Ugo Schiff 6 I-50019 Florence Italy;

Dept Univ Florence NEUROFARBA Dept Sez Sci Farmaceut Via Ugo Schiff 6 I-50019 Florence Italy;

Dept Univ Florence NEUROFARBA Dept Sez Sci Farmaceut Via Ugo Schiff 6 I-50019 Florence Italy;

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正文语种 eng
中图分类药学;
关键词
Carbonic anhydrase; Inhibitor; Metalloenzymes; Selenium; Selenol;

机译：碳酸酐酶;抑制剂;金属酶;硒;Selenol;

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专利

1. Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors [J] . Tanini Damiano, Capperucci Antonella, Ferraroni Marta, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2020,第期

机译：直接和直接进入取代烷基硒醇作为新型碳酸酐酶抑制剂
2. A Straightforward Access to Stable beta-Functionalized Alkyl Selenols [J] . Tanini Damiano, Tiberi Caterina, Gellini Cristina, Advanced synthesis & catalysis . 2018,第17期

机译：直接进入稳定β-官能化烷基硒醇
3. Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. [J] . Smaine FZ, Pacchiano F, Rami M, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：碳酸酐酶抑制剂：2-取代的1,3,4-噻二唑-5-磺酰胺可作为线粒体同工酶VA和VB的强力和选择性抑制剂，作用于胞质和膜相关的碳酸酐酶I，II和IV。
4. STABILITY STUDY IN PLASMA OF NOVEL ESTER-LINKED NSAID - CARBONIC ANHYDRASE INHIBITOR HYBRIDS [C] . Silvia Bua, Marta Menicatti, Paola Gratteri, International Mass Spectrometry Conference . 2018

机译：新型酯连接NSAID - 碳酸酐酶抑制剂杂交种血浆稳定性研究
5. Kinetics and mechanisms of the ligand substitution reactions of cyclopentadienyl M tetracarbonyl, indenyl M tetracarbonyl, M = niobium or tantalum, and molybdenum(2) (carbon monoxide)(6) [mu-eta(5),eta(5)-cyclopentadienylide-carbon alkyl(2)-cyclopentadienylide] with tributylphosphine, triphenylphosphine and triphenylphosphite. Photo-assisted carbonylation of supercritical ethane, ethane and methane in supercritical carbon dioxide by trans-chlorocarbonylbis(trimethylphosphine)rhodium(I). [D] . Lukmanova-Kline, Dinara Maratovna. 2001

机译：动力学和机制的环戊二烯基M四羰基，茚基M四羰基，M =铌或钽和钼（2）（一氧化碳）（6）[mu-eta（5），eta（5）-cyclopentadienylide-碳烷基（2）-环戊二烯基]与三丁基膦，三苯基膦和亚磷酸三苯酯。通过反氯羰基双（三甲基膦）铑（I）在超临界二氧化碳中对超临界乙烷，乙烷和甲烷进行光辅助羰基化。
6. Direct access to 2-aryl substituted pyrrolinium salts for carbon centre based radicals without pyrrolidine-2-ylidene alias cyclic(alkyl)(amino)carbene (CAAC) as a precursor [O] . Debdeep Mandal, Sebastian Sobottka, Ramapada Dolai, 2019

机译：可直接获得2-芳基取代的吡咯鎓盐而无需吡咯烷-2-亚烷基别名环（烷基）（氨基）卡宾（CAAC）作为碳中心基团
7. Straightforward access to densely substituted chiral succinimides through enantioselective organocatalyzed Michael addition of α-alkyl-cyclic ketones to maleimides [O] . Lai Wei, Li Chen, Franck Le Bideau, 2020

机译：通过对映选择性有机催化的Michael加入α-烷基环酮转移到马来酰亚胺的致注重取代的手性琥珀酰亚胺的直接进入

Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors

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