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.
Deparment of Chemistry, University of Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
Daniela
D
Comegna
Monica
M
Benincasa
Renato
R
Gennaro
Irene
I
Izzo
Francesco
F
De Riccardis
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