Design, synthesis and antimicrobial properties of non-hemolytic cationic alpha-cyclopeptoids.
The synthesis and screening of neutral and cationic, linear and cyclic peptoids (N-alkylglycine peptidomimetics) is described. Structure-activity relationship studies show that the in vitro activities of the tested peptoids depend on both cyclization and decoration with cationic groups. The most powerful N-lysine cyclopeptoid derivatives showed good antifungal activity against Candida albicans (ATCC90029 and L21) and Candida famata (SA550, Amph B-resistant) and low hemolytic activity. The effects of the cyclic peptoids on membrane permeabilization were evaluated by the propidium iodide exclusion assay.
Comegna
Daniela
D
Deparment of Chemistry, University of Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
Benincasa
Monica
M
Gennaro
Renato
R
Izzo
Irene
I
De Riccardis
Francesco
F
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002412:Cations / Q000737:chemistry*; D002463:Cell Membrane Permeability / Q000187:drug effects; D015195:Drug Design; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis; D006801:Humans; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D002412:Cations; D010456:Peptides, Cyclic