Synthesis, structure and biological activity of pseudopeptidic macrolides based on an amino alcohol.
A series of new pseudopeptidic macrolides 2a-f based on an amino alcohol were synthesized and evaluated for in vitro antibacterial and antifungal activities. The structure-activity relationships of these compounds were studied and the results showed that compounds 2a and 2d exhibited moderate antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli, whereas compound 2e showed potent antifungal activity against all the fungal species tested, showing a promising broad-spectrum antifungal activity. All the compounds have been studied in vitro for the hemolytic activity as a measure of their cytotoxicity, showing that these compounds have low lytic properties.
Lv
Jian
J
Department of Chemistry, The Key Laboratory of Elemento-organic Chemistry, Nankai University, Tianjin 300071, China.
Liu
Tingting
T
Wang
Yongmei
Y
D000605:Amino Alcohols / Q000737:chemistry*; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D018360:Crystallography, X-Ray; D005658:Fungi / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000605:Amino Alcohols; D000890:Anti-Infective Agents; D018942:Macrolides