Ethylene bis-imidazoles are highly potent and selective activators for isozymes VA and VII of carbonic anhydrase, with a potential nootropic effect

Bogdan Draghici; Daniela Vullo; Suleyman Akocak; Ellen A. Walker; Claudiu T. Supuran; Marc A. Ilies

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Ethylene bis-imidazoles are highly potent and selective activators for isozymes VA and VII of carbonic anhydrase, with a potential nootropic effect

机译：乙烯双咪唑类是碳酸酐酶同工酶VA和VII的强效选择性活化剂，具有促智作用

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A series of ethylene bis-imidazoles was synthesized via a novel microwave-mediated synthesis. Biological testing on eight isozymes of carbonic anhydrase (CA) present in the human brain revealed compounds with nanomolar potency against CA VA and CA Ⅶ, also displaying excellent selectivity against other CA isozymes present in this organ.

机译：通过新型微波介导的合成方法合成了一系列乙烯双咪唑。对人脑中存在的8种碳酸酐酶（CA）同工酶进行的生物学测试表明，这些化合物具有针对CA VA和CA nano的纳摩尔浓度，对这些器官中存在的其他CA同工酶也具有出色的选择性。

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《Chemical Communications》 |2014年第45期|5980-5983|共4页
作者
Bogdan Draghici; Daniela Vullo; Suleyman Akocak; Ellen A. Walker; Claudiu T. Supuran; Marc A. Ilies;
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Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA;

NEUROFARM Department, Pharmaceutical Sciences Section, Universita degli Studi di Firenze, Polo Scientifico, Via Ugo Schiff no. 6, 50019 Sesto Fiorentino, Florence, Italy;

Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA;

Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA;

NEUROFARM Department, Pharmaceutical Sciences Section, Universita degli Studi di Firenze, Polo Scientifico, Via Ugo Schiff no. 6, 50019 Sesto Fiorentino, Florence, Italy;

Department of Pharmaceutical Sciences and Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N Broad Street, Philadelphia, PA-19140, USA;

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入库时间 2022-08-17 13:15:51

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机译：氨基醇肟醚从人脑中激活碳酸酐酶：朝向人碳酸酐酶VII选择性活化剂
2. Carbonic anhydrase activators: L-Adrenaline plugs the active site entrance of isozyme II, activating better isoforms I, IV, VA, VII, and XIV. [J] . Temperini C, Innocenti A, Scozzafava A, Bioorganic and Medicinal Chemistry Letters . 2007,第3期

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机译：碳酸酐酶激活剂。用L-和D-组氨酸激活同工酶I，II，IV，VA，VII和XIV及其同工型II的加合物的晶体学分析：酶活性位点内的工程质子转移过程
4. Growth and Invasion of Human Cancer Cells: The Roles of Carbonic Anhydrase Isozymes [C] . . 2005

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5. Identification of Primary Carbonic Anhydrase Isozymes in Rana pipiens Tissue Fractions [D] . Kirkman, Allison E. 2017

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6. Activation of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators [O] . Alessio Nocentini, Doretta Cuffaro, Lidia Ciccone, 2021

机译：氨基醇肟醚从人脑中激活碳酸酐酶：朝向人碳酸酐酶VII选择性活化剂
7. Carbonic Anhydrase Activators. VII. Isozyme II Activation by Bisazolyl-methanes, -ethanes and Related Azoles. [O] . Claudiu T. SUPURAN, Alexandru T. BALABAN, Pilar CABILDO, 1993

机译：碳酸酐酶活化剂。 VII。异氮杂基 - 甲烷 - 甲烷基， - 乙烷和相关氮杂化的Isozyme II活化。

Ethylene bis-imidazoles are highly potent and selective activators for isozymes VA and VII of carbonic anhydrase, with a potential nootropic effect

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