Facially Amphiphilic Cholic Acid-Lysine Conjugates as Promising Antimicrobials.
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ABSTRACT: The emergence of multidrug-resistant microbes is a significant health concern posing a constant need for new antimicrobials. Membrane-targeting antibiotics are promising candidates with reduced ability of microbes to develop resistance. In the present investigation, the principal reason behind choosing cholic acid as the crucial scaffold lies in the fact that it has a facially amphiphilic nature, which provides ample opportunity to refine the amphiphilicity by linking the amino acid lysine. A total of 16 novel amphipathic cholic acid derivatives were synthesized by sequentially linking lysine to C3-β-amino cholic acid methyl ester to maintain the hydrophobic/hydrophilic balance, which could be the essential requirement for the antimicrobial activity. Among the synthesized conjugates, a ser
SUBMITTER: Singla P
PROVIDER: S-EPMC7057326 | biostudies-literature | 2020 Mar
REPOSITORIES: biostudies-literature
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