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新型N-(1-苯基-4-羧基吡唑-5-基)-、N-(吲唑-3-基)-和N-(吲唑-5-基)-2-碘苯甲酰胺的合成及其抗真菌活性

Synthesis and antifungal activity of new N-(1-phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides.

作者信息

Raffa Demetrio, Daidone Giuseppe, Plescia Fabiana, Schillaci Domenico, Maggio Benedetta, Torta Livio

机构信息

Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli Studi di Palermo, Italy.

出版信息

Farmaco. 2002 Mar;57(3):183-7. doi: 10.1016/s0014-827x(01)01190-9.

Abstract

N-(1-Phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides 6, with a Benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 5 with potassium iodide for 1 h in order to study the role on the antifungal activity of the N-substitution with an aromatic heterocyclic system on benzamide moiety. Among the tested iododerivatives, compounds 6d,f,g,h possess interesting activities toward some phytopathogenic fungal strains.

摘要

为了研究苯甲酰胺部分上用芳族杂环系统进行N-取代对其抗真菌活性的作用,通过在乙酸中使相应的苯并三嗪酮5与碘化钾回流1小时,合成了具有类似苯菌灵结构的N-(1-苯基-4-羧基吡唑-5-基)-、N-(吲唑-3-基)-和N-(吲唑-5-基)-2-碘苯甲酰胺6。在所测试的碘衍生物中,化合物6d、f、g、h对一些植物病原真菌菌株具有有趣的活性。

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