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Quinine Esters with 1,2-Azole, Pyridine and Adamantane Fragments
Molecules ( IF 4.2 ) Pub Date : 2022-05-27 , DOI: 10.3390/molecules27113476
Gulim K Mukusheva 1 , Aigerym R Zhasymbekova 1 , Roza B Seidakhmetova 1 , Oralgazy A Nurkenov 2 , Ekaterina A Akishina 3 , Sergey K Petkevich 3 , Evgenij A Dikusar 3 , Vladimir I Potkin 3
Molecules ( IF 4.2 ) Pub Date : 2022-05-27 , DOI: 10.3390/molecules27113476
Gulim K Mukusheva 1 , Aigerym R Zhasymbekova 1 , Roza B Seidakhmetova 1 , Oralgazy A Nurkenov 2 , Ekaterina A Akishina 3 , Sergey K Petkevich 3 , Evgenij A Dikusar 3 , Vladimir I Potkin 3
Affiliation
An efficient method of producing quinine derivatives via reaction of acylation with 4,5-dichloroisothiazole-3-, 5-arylisoxazole-3-, adamantane- and hydrochlorides of pyridine-3- and pyridine-4-carbonyl chlorides was developed. All synthesized compounds were tested for antiviral, antimicrobial and analgesic activity. The most pronounced antibacterial activity was shown by the compounds 2e, 3b, 3c and 3e with isoxazole and pyridine fragments. It was found that most of the tested compounds showed significant analgesic activity reducing the pain response of animals to the irritating effect of acetic acid.
中文翻译:
含 1,2-唑、吡啶和金刚烷片段的奎宁酯
开发了一种通过与 4,5-二氯异噻唑-3-、5-芳基异恶唑-3-、金刚烷-以及吡啶-3-和吡啶-4-碳酰氯的盐酸盐进行酰化反应制备奎宁衍生物的有效方法。测试了所有合成的化合物的抗病毒、抗微生物和镇痛活性。化合物2e、3b、3c和3e与异恶唑和吡啶片段显示出最显着的抗菌活性。发现大多数受试化合物显示出显着的镇痛活性,可降低动物对乙酸刺激作用的疼痛反应。
更新日期:2022-05-28
中文翻译:

含 1,2-唑、吡啶和金刚烷片段的奎宁酯
开发了一种通过与 4,5-二氯异噻唑-3-、5-芳基异恶唑-3-、金刚烷-以及吡啶-3-和吡啶-4-碳酰氯的盐酸盐进行酰化反应制备奎宁衍生物的有效方法。测试了所有合成的化合物的抗病毒、抗微生物和镇痛活性。化合物2e、3b、3c和3e与异恶唑和吡啶片段显示出最显着的抗菌活性。发现大多数受试化合物显示出显着的镇痛活性,可降低动物对乙酸刺激作用的疼痛反应。