新型二氟甲基唑类作为抗利什曼原虫药物的合成与评价
Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents.
作者信息
Ferreira Sabrina B, Costa Marilia S, Boechat Núbia, Bezerra Rômulo J S, Genestra Marcelo S, Canto-Cavalheiro Marilene M, Kover Warner B, Ferreira Vitor F
机构信息
Universidade Federal do Rio de Janeiro Departamento de Química Orgânica, Instituto de Química, Cidade Universitária, 21949-900 Rio de Janeiro, RJ, Brazil.
出版信息
Eur J Med Chem. 2007 Nov-Dec;42(11-12):1388-95. doi: 10.1016/j.ejmech.2007.02.020. Epub 2007 Mar 12.
Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds.
几种具有重大药理学意义的化合物含有三唑环和咪唑环。为了寻找具有抗利什曼原虫活性的新药，我们合成并评估了带有醛基或二氟亚甲基官能团的新型咪唑和三唑化合物对亚马逊利什曼原虫前鞭毛体形式的活性。在所测试的化合物中，二氟亚甲基唑类化合物4b和8f显著抑制了寄生虫的生长。我们的结果表明，二氟亚甲基部分的引入已将无活性的醛类转化为有活性的抗利什曼原虫化合物。
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