title: N-cholesteryl amino acid conjugates and their antimicrobial activities.
abstract: A series of N-cholesteryl amino acid conjugates have been synthesized using a reductive amination protocol in good yield and purity. All the synthesized conjugates were evaluated for their in vitro antimicrobial activities against Gram positive and Gram negative bacteria. Among the conjugates tested, N-cholesteryl GABA 12 showed the highest potency toward the methicillin-resistant Staphylococcus aureus with the lowest MIC value of 2 μg/mL. Hemolytic activities of the compounds 3, 4, 11, and 12 were determined. All compounds tested had no significant hemolytic activity up to >50 μg/mL.
authors.affiliation: Department of Applied Chemistry, Kyungpook National University, Daegu 702-701, Republic of Korea.
authors.forename: Jyoti R
authors.initials: JR
authors.lastname: Jadhav
authors.forename: Hong-Seok
authors.initials: HS
authors.lastname: Kim
authors.forename: Jin-Hwan
authors.initials: JH
authors.lastname: Kwak
mesh_terms: D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002478:Cells, Cultured; D002784:Cholesterol / Q000737:chemistry*; D004912:Erythrocytes / Q000187:drug effects / Q000473:pathology; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000254:growth & development; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests
chemical_list: D000596:Amino Acids; D000900:Anti-Bacterial Agents; D002784:Cholesterol
keywords: Antimicrobial agents; Methicillin-resistant Staphylococcus aureus; N-Cholesteryl amino acid conjugates; SAR study