N/C-4 substituted azetidin-2-ones: synthesis and preliminary evaluation as new class of antimicrobial agents.
A series of 3-chloro-4-(3-methoxy-4-acetyloxyphenyl)-1-[3-oxo-3-(phenylamino)propanamido] azetidin-2-ones 3a-g and 3-chloro-4-[2-hydroxy-5-(nitro substituted phenylazo)phenyl]-1-phenylazetidin-2-ones 6a-h were synthesized using appropriate synthetic route. Structures of all the synthesized compounds were established on the basis of elemental analysis and spectroscopic data. The antimicrobial activity of the synthesized compounds was screened against several microbes. Several of these molecules showed potent antimicrobial activity against Bacillus anthracis, Staphylococcus aureus and Candida albicans and significant structure-activity relationship (SAR) trends.
Halve
Anand K
AK
School of Studies in Chemistry, Jiwaji University, Gwalior 474011, India. drhalve_chemjiwaji@rediffmail.com
Bhadauria
Deepti
D
Dubey
Rakesh
R
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001384:Azetidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000254:growth & development; D003500:Cyclization; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D005658:Fungi / Q000187:drug effects / Q000254:growth & development; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D001384:Azetidines; D007202:Indicators and Reagents