Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), Kukrail Picnic Spot Road, PO CIMAP, Lucknow 226 015, UP, India.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):508-12. doi: 10.1016/j.bmcl.2009.11.107. Epub 2009 Nov 26.
Phytol, a diterpene alcohol was modified to several semisynthetic analogues. Some of the modifications were done logically to enhance lipophilicity of the molecule. Analogues 14, 16 and 18 exhibited antitubercular activity (MIC 15.6-50microg/mL) better than phytol (100microg/mL). The most potent analogue 18 was evaluated for in vivo toxicity in Swiss albino mice and was well tolerated by the experimental animals up to 300mg/kg body weight as a single oral acute dose.
植物醇是一种二萜醇,被修饰成了几种半合成类似物。其中一些修饰是为了提高分子的亲脂性而进行的合理修饰。类似物 14、16 和 18 表现出比植物醇(100μg/mL)更好的抗结核活性(MIC 15.6-50μg/mL)。最有效的类似物 18 在瑞士白化小鼠中进行了体内毒性评估,在单次口服急性剂量高达 300mg/kg 体重时,实验动物能够很好地耐受。