标题：甲酯 4-（7-羟基-4,4,8-三甲基-3-氧杂二环[3.3.1]壬烷-2-基）苯甲酸酯的合成与评价及其与米替福新的协同抗利什曼原虫作用
Synthesis and Evaluation of Methyl 4-(7-Hydroxy-4,4,8-Trimethyl-3-Oxabicyclo[3.3.1]Nonan-2-yl)Benzoate as an Antileishmanial Agent and Its Synergistic Effect with Miltefosine.
机构信息
Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Assam, India.
Department of Chemistry, Indian Institute of Technology Guwahati, Assam, India.
出版信息
Antimicrob Agents Chemother. 2018 Jan 25;62(2). doi: 10.1128/AAC.01810-17. Print 2018 Feb.
Abstract
In our interest in oxabicyclic compounds as potent antileishmanial agents, the present work deals with the chemical synthesis of a new oxabicyclic derivative, methyl 4-(7-hydroxy-4,4,8-trimethyl-3-oxabicyclo[3.3.1]nonan-2-yl)benzoate (PS-207). This oxabicyclic derivative showed a good antileishmanial effect on the parasite, on both the promastigote and the amastigote. The mode of parasitic death from PS-207 seemed to be apoptosis-like. Interestingly, the combination of PS-207 with a low dose of miltefosine showed a synergistic effect against the parasite.
摘要
在我们对作为强效抗利什曼原虫药物的氧杂双环化合物的研究兴趣中，本工作涉及一种新的氧杂双环衍生物——甲酯 4-(7-羟基-4,4,8-三甲基-3-氧杂双环[3.3.1]壬烷-2-基)苯甲酸酯（PS-207）的化学合成。该氧杂双环衍生物对寄生虫表现出良好的抗利什曼原虫作用，无论是对前鞭毛体还是无鞭毛体。PS-207 引起寄生虫死亡的方式似乎类似于细胞凋亡。有趣的是，PS-207 与低剂量米替福新联合使用对寄生虫表现出协同作用。
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