A concise synthesis and antimicrobial activities of 3-polyamino-23,24-bisnorcholanes as steroid–polyamine conjugates

A series of steroid–polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C-3 on activity against various human pathogens. All the conjugates exhibited strong antimicrobial activities against Gram-positive strains. Compound 18 was found to be the most potent in these series with a MIC value as low as 1 μg/mL against the bacterium Staphylococcus aureus ATCC6538P.

Graphical abstractA series of steroid–polyamine conjugates were synthesized and evaluated for their antimicrobial activity. The 3β-sperminyl-23,24-bisnor-5β-cholane (18) was the most potent in this series with a MIC value as low as 1 μg/mL against Staphylococcus aureus ATCC6538P.Figure optionsDownload full-size imageDownload as PowerPoint slide