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Synthesis and Biological Evaluation of Some New Fused Heterobicyclic Derivatives Containing 1,2,4-Triazolo/1,2,4-Triazinopyridinone Moieties

机译:某些新的含1,2,4-三唑/ 1,2,4-三嗪并吡啶酮部分的稠合杂环双环衍生物的合成及生物评价

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摘要

Syntheses of fused lieterobicyclic systems containing l,2,4-triazolo/l,2,4-triazinopyridinone moieties were accomplished by heterocyclizatkm of 4-(4-chlorophenyl)-l,6-diamino-2-oxo-l,2-dihydropyridine-3,5-dicarbonitrile (III) or 6-amino-4-(4-chlorophenyl)-2-oxo-l-(5,6-diphenyl-l,2,4-triazin-3-ylamino)-l,2-dihydropyridine-3,5-dicarbonitrile (XII) with a,/3-bifunctional oxygen and halooxo compounds in different media in order to establish a relation between structure and their activities. Compounds III and XII which contain 1,2-biamino group are more favoured to the ring-closure reactions. Structure assignments of new products have been established on the basis of elemental analysis and spectral data. The antimicrobial activity of the products has been also evaluated where some compounds showed a better activity against selected tested microbes in comparison with control.
机译:含有1,2,4-三唑/ l,2,4-三嗪并吡啶酮部分的稠合双环系统的合成是通过4-(4-氯苯基)-1,6-二氨基-2-氧-l,2-二氢吡啶的杂环化来完成的-3,5-二腈(III)或6-氨基-4-(4-氯苯基)-2-氧-1-(5,6-二苯基-1,2,4-三嗪-3-基氨基)-1, 2-dihydropyridine-3,5-dicarbonitrile(XII)与a,/ 3-双功能氧和haloxo化合物在不同的介质中建立结构与其活性之间的关系。含有1,2-二氨基的化合物III和XII更优选于闭环反应。在元素分析和光谱数据的基础上,建立了新产品的结构分配。还评估了产品的抗菌活性,与对照相比,其中某些化合物对选定的测试微生物表现出更好的活性。

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