新型脂肪酸酰胺的合成及抗结核活性。
Synthesis and antituberculosis activity of new fatty acid amides.
机构信息
Laboratório Kolbe de Síntese Orgânica, Escola de Química e Alimentos, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
出版信息
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5255-7. doi: 10.1016/j.bmcl.2010.06.149. Epub 2010 Jul 7.
This work reports the synthesis of new fatty acid amides from C16:0, 18:0, 18:1, 18:1 (OH), and 18:2 fatty acids families with cyclic and acyclic amines and demonstrate for the first time the activity of these compounds as antituberculosis agents against Mycobacterium tuberculosis H(37)Rv, M. tuberculosis rifampicin resistance (ATCC 35338), and M. tuberculosis isoniazid resistance (ATCC 35822). The fatty acid amides derivate from ricinoleic acid were the most potent one among a series of tested compounds, with a MIC 6.25 microg/mL for resistance strains.
这项工作报道了新型脂肪酸酰胺的合成，这些脂肪酸酰胺来自 C16:0、18:0、18:1、18:1(OH) 和 18:2 脂肪酸家族，与环和非环胺反应，并首次证明这些化合物作为抗结核药物对抗结核分枝杆菌 H(37)Rv、结核分枝杆菌利福平耐药 (ATCC 35338) 和结核分枝杆菌异烟肼耐药 (ATCC 35822) 的活性。一系列测试化合物中，蓖麻油酸衍生的脂肪酸酰胺是最有效的一种，对耐药菌株的 MIC 值为 6.25μg/mL。
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