Synthesis and antimicrobial activity of 4-benzyloctahydropyrrolo- [3,4-b][1,4]oxazine derivatives

Eswarappa Bheemappaa; rashekar Aswathanarayanappab; Yadav D. Bodkeb; Peethamber S. K.

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Synthesis and antimicrobial activity of 4-benzyloctahydropyrrolo- [3,4-b][1,4]oxazine derivatives

机译：4-苄基八氢吡咯并[3,4-b] [1,4]恶嗪衍生物的合成及抑菌活性

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The novel bridged bicyclic morpholine derivatives, 4-benzyloctahydropyrrolo-[3,4-b][1,4]oxazine derivatives (6a-j) have been synthesized in six steps. The target compounds (6a-j) were obtained by reacting active intermediate 4- benzyloctahydropyrrolo-[3,4-b][1,4]oxazine (5) with various alkyl or aryl halide substituents in the presence of potassium carbonate. Thesebridged bicyclic morpholineswhich were fused to an additional hetero ring, pyrrolidinewere screened for their antibacterial and antifungal potency. These derivatives,N-substituted with cyclohexomethyl, isopropyl, p-methylbenzyl and phenylethylexhibited promising antimicrobial activity; compounds 6a-c were effective against the tested bacterial strains; compounds 6a, 6c, 6g were effective against antifungal strains; and compounds 6d and 6e were not active for these studies.

机译：新型的桥联双环吗啉衍生物，4-苄基八氢吡咯并-[3,4-b] [1,4]恶嗪衍生物（6a-j）已通过六个步骤合成。通过使活性中间体4-苄基八氢吡咯并-[3,4-b] [1,4]恶嗪（5）与各种烷基或芳基卤化物取代基在碳酸钾存在下反应，获得目标化合物（6a-j）。将这些桥连的双环吗啉与另外的杂环稠合，对吡咯烷进行抗菌和抗真菌作用的筛选。这些被N-环己甲基，异丙基，对甲基苄基和苯乙基取代的衍生物具有良好的抗菌活性。化合物6a-c对测试的细菌菌株有效。化合物6a，6c，6g对抗真菌菌株有效。化合物6d和6e对这些研究没有活性。

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《Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry》 |2014年第3期|共8页
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Eswarappa Bheemappaa; rashekar Aswathanarayanappab; Yadav D. Bodkeb; Peethamber S. K.;
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Synthesis and antimicrobial activity of 4-benzyloctahydropyrrolo- [3,4-b][1,4]oxazine derivatives

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