Design and synthesis of bile acid-based amino sterols as antimicrobial agents |
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| Authors: | Nilkanth G. Aher Vandana S. Pore Nripendra N. Mishra Praveen K. Shukla Rajesh G. Gonnade |
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| Affiliation: | aOrganic Chemistry Division, National Chemical Laboratory, Pune 411 008, India;bDivision of Fermentation Technology, Central Drug Research Institute, Lucknow 226 001, India;cCentre for Material Characterization, National Chemical Laboratory, Pune 411 008, India |
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| Abstract: | New bile acid-based amino sterols were synthesized in good yields from C-3β-oxiranes as key intermediates. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. These compounds showed better antibacterial activity as compared to antifungal activity. Compounds 21 and 22 showed comparable antibacterial activity to gentamicin against Staphylococcus aureus with IC50 values of 5.14 and 4.46 μg/mL. This is the first report for the synthesis of C-3β-oxiranes on the steroids having A/B cis ring junction and these oxiranes have been used for the synthesis of amino sterols 17, 18, 21, and 22. |
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| Keywords: | Bile acid Oxirane Antibacterial agent Amino sterols |
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