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通过Ugi-叠氮化物合成3-四唑基甲基-4H-色烯-4-酮及其对溶组织内阿米巴、蓝氏贾第鞭毛虫和阴道毛滴虫的生物学评价

Synthesis of 3-tetrazolylmethyl-4H-chromen-4-ones via Ugi-azide and biological evaluation against Entamoeba histolytica, Giardia lamblia and Trichomona vaginalis.

作者信息

Cano Pedro A, Islas-Jácome Alejandro, González-Marrero Joaquín, Yépez-Mulia Lilian, Calzada Fernando, Gámez-Montaño Rocío

机构信息

Departamento de Química, DCNE, Universidad de Guanajuato, Noria Alta S/N, Guanajuato C.P. 36050, Guanajuato, Mexico.

Unidad Profesional Interdisciplinaria de Ingeniería, Instituto Politécnico Nacional, Av. Mineral de Valenciana 200, Col. Fracc. Industrial Puerto Interior, Silao de la Victoria C.P. 36275, Guanajuato, Mexico.

出版信息

Bioorg Med Chem. 2014 Feb 15;22(4):1370-6. doi: 10.1016/j.bmc.2013.12.069. Epub 2014 Jan 11.

Abstract

The synthesis of novel 3-tetrazolylmethyl-4H-chromen-4-ones via an Ugi-azide multicomponent reaction and their biological evaluation against Entamoeba histolytica, Giardia lamblia and Trichomona vaginalis are described. Reported yields are moderate to good and biological results show that these compounds could be considered as candidates to anti-parasitic drugs, especially against G. lamblia.

摘要

描述了通过乌吉-叠氮化物多组分反应合成新型3-四唑基甲基-4H-色烯-4-酮及其对溶组织内阿米巴、蓝氏贾第鞭毛虫和阴道毛滴虫的生物学评价。报道的产率为中等至良好,生物学结果表明这些化合物可被视为抗寄生虫药物的候选物,尤其是针对蓝氏贾第鞭毛虫。

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