Article ID Journal Published Year Pages File Type
1375340 Bioorganic & Medicinal Chemistry Letters 2010 5 Pages PDF
Abstract

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 15.6–50 μg/mL) better than phytol (100 μg/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 300 mg/kg body weight as a single oral acute dose.

Graphical abstractPhytol, 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 15.6–50 μg/mL) better than phytol (100 μg/mL). The most potent analogue 18, was evaluated for in vivo toxicity in Swiss albino mice and was found to be well tolerated by the experimental animals up to 300 mg/kg body weight as a single oral acute dose.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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