Studies on the antifungal properties of N-thiolated beta-lactams.
N-thiolated beta-lactams had previously been shown to have antibacterial activity against a narrow selection of pathogenic bacteria including Staphylococcus aureus and Bacillus anthracis, as well as apoptotic-inducing activity in a variety of human cancer cell lines. We now have found that these lactams also possess antifungal activity against Candida and other fungi by exerting powerful cytostatic effects that disrupt the structural integrity of cytoplasmic membranes. The mode of action and structure-activity trends of these lactams as antifungals parallel that previously seen in our antibacterial studies.
O'Driscoll
Marci
M
Center for Molecular Diversity in Drug Design, Discovery, and Delivery, Department of Chemistry, 4202 East Fowler Avenue, CHE 205, University of South Florida, Tampa, FL 33620, USA.
Greenhalgh
Kerriann
K
Young
Ashley
A
Turos
Edward
E
Dickey
Sonja
S
Lim
Daniel V
DV
D000935:Antifungal Agents / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D005779:Immunodiffusion; D008826:Microbial Sensitivity Tests; D046529:Microscopy, Electron, Transmission; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000494:pharmacology*; D014343:Trypan Blue / Q000737:chemistry; D047090:beta-Lactams / Q000494:pharmacology*
D000935:Antifungal Agents; D013438:Sulfhydryl Compounds; D047090:beta-Lactams; D014343:Trypan Blue