Synthesis and antimicrobial activity of beta-lactam-bile acid conjugates linked via triazole.
Synthesis of novel 1,2,3-triazole-linked beta-lactam-bile acid conjugates 17-24 using 1,3-dipolar cycloaddition reaction of azido beta-lactam and terminal alkyne of bile acids in the presence of Cu(I) catalyst (click chemistry) have been realized. These molecules were evaluated in vitro for their antifungal and antibacterial activities. Most of the compounds exhibited significant antifungal and moderate antibacterial activity against all the tested strains.
Vatmurge
Namdev S
NS
Organic Chemistry Division, National Chemical Laboratory, Pune 411 008, India.
Hazra
Braja G
BG
Pore
Vandana S
VS
Shirazi
Fazal
F
Chavan
Pradnya S
PS
Deshpande
Mukund V
MV
D000480:Alkynes / Q000737:chemistry; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001647:Bile Acids and Salts / Q000737:chemistry*; D003300:Copper / Q000494:pharmacology; D003460:Crystallization; D003500:Cyclization; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D005658:Fungi / Q000187:drug effects / Q000254:growth & development; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D014230:Triazoles / Q000737:chemistry*; D047090:beta-Lactams / Q000737:chemistry*
D000480:Alkynes; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D001647:Bile Acids and Salts; D014230:Triazoles; D047090:beta-Lactams; D003300:Copper