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首页> 外文期刊>Letters in drug design & discovery >In vivo assessment of antileishmanial property of 4-(4,4,8-trimethyl-7-oxo- 3-oxabicyclo[3.3.1]non-2-yl)-benzoic acid methyl ester, an oxabicyclo[ 3.3.1]nonanones
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In vivo assessment of antileishmanial property of 4-(4,4,8-trimethyl-7-oxo- 3-oxabicyclo[3.3.1]non-2-yl)-benzoic acid methyl ester, an oxabicyclo[ 3.3.1]nonanones

机译:体内评估4-(4,4,8-三甲基-7-氧代-3-氧杂双环[3.3.1]壬-2-基)-苯甲酸甲酯,一种氧杂双环[3.3.1]壬酸

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摘要

The high toxicity and the growing resistance are the major drawbacks of available antileishmanials. Our previous in vitro studies have identified oxabicyclo[3.3.1]nonanones as antileishmanial agents that act on the redox enzymes of the parasite. In the current study, antileishmanial activity of 4-(4,4,8-trimethyl-7-oxo-3-oxabicyclo[3.3.1]non-2-yl)-benzoic acid methyl ester (PS 203) the most potent oxabicyclo[3.3.1]nonanone identified in our previous study is evaluated using the hamster model. There was 77.29 ± 3.0 % inhibition of parasite growth observed after a 5-day treatment of 5 mg/kg body weight dose. Further, the in vivo toxicity study of the compound in Swiss albino mice revealed no hepatic or renal toxicity.
机译:高毒性和不断增长的耐药性是现有抗臭剂的主要缺点。我们以前的体外研究已确定氧杂双环[3.3.1]壬酸为抗寄生虫药,作用于寄生虫的氧化还原酶。在当前的研究中,4-(4,4,8-三甲基-7-氧代-3-氧杂双环[3.3.1]非-2-基)-苯甲酸甲酯(PS 203)的抗草胺活性最强[3.3.1]我们先前的研究中确定的壬酮是使用仓鼠模型评估的。 5 mg / kg体重剂量的5天治疗后观察到77.29±3.0%的寄生虫生长抑制。此外,该化合物在瑞士的白化病小鼠中的体内毒性研究显示没有肝或肾毒性。

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