Mechanochemical synthesis of antifungal bis(benzoxaboroles)

Borys Krzysztof M.; Wieczorek Dorota; Tarkowska Magdalena; Jankowska Agnieszka; Lipok Jacek; Adamczyk-Wozniak Agnieszka

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Mechanochemical synthesis of antifungal bis(benzoxaboroles)

机译：机械化学合成抗真菌（Benzoxaboroles）

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Several piperazine bis(benzoxaboroles) have been obtained both in solution as well as in the solid state. The environmentally friendly mechanochemical approach - hitherto not applied for the preparation of benzoxaboroles - was particularly beneficial in the case of two products afforded in low yields in solution. Thein vitrostudies showed high potential of the studied bis(fluorobenzoxaboroles) as antifungal agents, highlighting also the influence of the fluorine substituent position on their microbiological activity. The highest activity againstA. niger,A. terreus,P. ochrochloron,C. tenuisandC. albicanswas displayed by the analogue of the known benzoxaborole antifungal drug Kerydin (R) (Tavaborole).

机译：已经在溶液以及固态中获得了几种哌嗪双（苯并氧基硼酸盐）。环保机械化学方法 - 迄今为止不适用于制备苯并氧基洛杉矶 - 在溶液中低产率提供两种产品的情况下特别有益。 Thein Vitrostudies表现出研究的双（氟苯氧基毒剂）作为抗真菌剂的高潜力，突出了氟取代基对微生物活性的影响。最高的活动反对。尼日尔，一个。 Terreus，p。 OChrochloron，C。 Tenuisandc。已知的苯并氧基抗原药物Kerydin（R）（Tavaborole）的类似物显示的albicanswas。

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《RSC Advances》 |2020年第61期|共7页
作者
Borys Krzysztof M.; Wieczorek Dorota; Tarkowska Magdalena; Jankowska Agnieszka; Lipok Jacek; Adamczyk-Wozniak Agnieszka;
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Warsaw Univ Technol Fac Chem Noakowskiego 3 PL-00664 Warsaw Poland;

Univ Opole Fac Chem Oleska 48 PL-45052 Opole Poland;

Warsaw Univ Technol Fac Chem Noakowskiego 3 PL-00664 Warsaw Poland;

Warsaw Univ Technol Fac Chem Noakowskiego 3 PL-00664 Warsaw Poland;

Univ Opole Fac Chem Oleska 48 PL-45052 Opole Poland;

Warsaw Univ Technol Fac Chem Noakowskiego 3 PL-00664 Warsaw Poland;

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正文语种 eng
中图分类化学;
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1. Mechanochemical synthesis of antifungal bis(benzoxaboroles) [J] . Borys Krzysztof M., Wieczorek Dorota, Tarkowska Magdalena, RSC Advances . 2020,第61期

机译：机械化学合成抗真菌（Benzoxaboroles）
2. Synthesis and structural elucidation of novel antifungal N-(fluorophenyl)piperazinyl benzoxaboroles and their analogues [J] . Borys Krzysztof M., Matuszewska Alicja, Wieczorek Dorota, Journal of Molecular Structure . 2019,第期

机译：新型抗真菌N-（氟苯基）哌嗪基苯氧基毒剂及其类似物的合成及结构阐明
3. Synthesis of isotopically labelled (3-14C)- and (3,3-2H2)-5-fluoro-1,3-dihydro-1 -hydroxy-2,1 -benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis [J] . STEPHEN J. BAKER*, YONG-KANG ZHANG, TSUTOMU AKAMA, Journal of Labelled Compounds and Radiopharmaceuticals . 2007,第3期

机译：同位素标记的（3-14C）-和（3,3-2H2）-5-氟-1,3-二氢-1-羟基-2,1-苯并恶唑硼烷（AN2690）的合成，一种潜在的新型抗真菌剂灰指甲病
4. Synthesis of n-type Bi_(4-x)La_xTi_3O_(12) (x=0 to 0.45) by Alternative Mechanochemical Method [C] . Nagbasavanna Sharanappa DAE Solid State Physics Symposium . 2017

机译：通过替代机械化学方法合成N型BI_（4-X）LA_XTI_3O_（12）（x = 0至0.45）
5. Part I. Synthesis of N-substituted 2,5-bis-[4-guanidinophenyl]thiophenes as potential antileishmanial compunds. Part II. Synthesis of novel potential prodrugs of bis-guanidino and bis-amidino molecules. [D] . Gonzalez-Roman, Jose Luis. 2002

机译：第一部分：N-取代的2,5-双-[4-胍基苯基]噻吩的合成作为潜在的抗衰老化合物。第二部分双胍基和双-基分子的新型潜在前药的合成。
6. Bis-benzoxaboroles: Design Synthesis and BiologicalEvaluation as Carbonic Anhydrase Inhibitors [O] . Adèle Larcher, Alessio Nocentini, Claudiu T. Supuran, 2019

机译：双苯并氧化：设计合成和生物学作为碳酸酐酶抑制剂的评价
7. Mechanochemical synthesis of antifungal bis(benzoxaboroles) [O] . Krzysztof M. Borys, Dorota Wieczorek, Magdalena Tarkowska, 2020

机译：机械化学合成抗真菌（Benzoxaboroles）

Mechanochemical synthesis of antifungal bis(benzoxaboroles)

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