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.
Design, synthesis and antimicrobial properties of non-hemolytic cationic alpha-cyclopeptoids / Comegna, D.; Benincasa, Monica; Gennaro, Renato; Izzo, I.; De Riccardis, F.. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 18:(2010), pp. 2010-2018. [10.1016/j.bmc.2010.01.026]
Design, synthesis and antimicrobial properties of non-hemolytic cationic alpha-cyclopeptoids.
BENINCASA, MONICA;GENNARO, RENATO;
2010-01-01
Abstract
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.Pubblicazioni consigliate
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