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新型吡唑啉及其硼氟配合物的合成以及抗菌、抗氧化和酶抑制活性研究

Synthesis of Novel Pyrazolines, Their Boron-Fluorine Complexes, and Investigation of Antibacterial, Antioxidant, and Enzyme Inhibition Activities.

作者信息

Kahriman Nuran, Haşimoğlu Zeynep, Serdaroğlu Vildan, Beriş Fatih Şaban, Barut Burak, Yaylı Nurettin

机构信息

Faculty of Science, Department of Chemistry, Karadeniz Technical University, Trabzon, Turkey.

Faculty of Arts and Sciences, Department of Biology, Recep Tayyip Erdoğan University, Rize, Turkey.

出版信息

Arch Pharm (Weinheim). 2017 Feb;350(2). doi: 10.1002/ardp.201600285. Epub 2016 Dec 29.

Abstract

New 3,5-disubstituted-2-pyrazoline derivatives (4-6), their boron-fluorine complexes (boron (3-(2'-aminophenyl),5-(2'-/3'-/4'-pyridyl)pyrazoline, BOAPPY) (7-9) and boron 1,2'-diazaflavone complex (BODAF) (11) were synthesized starting from azachalcones (1-3) to diazaflavone (10), respectively. Biological evaluation of compounds 4-9 and 11 showed remarkable antioxidant, antibacterial, and acetylcholinesterase and tyrosinase enzyme inhibition activities. All newly synthesized compounds 4-9 and 11 showed respectable antibacterial effect with minimum inhibitory concentrations in the range of 4.7-150 μg/mL.

摘要

新型3,5-二取代-2-吡唑啉衍生物(4-6)、它们的硼氟配合物(硼(3-(2'-氨基苯基),5-(2'-/3'-/4'-吡啶基)吡唑啉,BOAPPY)(7-9)以及硼1,2'-二氮杂黄酮配合物(BODAF)(11)分别从氮杂查尔酮(1-3)开始合成至二氮杂黄酮(10)。对化合物4-9和11的生物学评价显示出显著的抗氧化、抗菌以及乙酰胆碱酯酶和酪氨酸酶抑制活性。所有新合成的化合物4-9和11均表现出可观的抗菌效果,最低抑菌浓度在4.7-150μg/mL范围内。

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