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EnglishThe 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.
| Titolo: | Design, synthesis and antimicrobial properties of non-hemolytic cationic alpha-cyclopeptoids. |
| Autori: | |
| Data di pubblicazione: | 2010 |
| Rivista: | |
| 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. |
| Handle: | http://hdl.handle.net/11368/2297822 |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmc.2010.01.026 |
| Appare nelle tipologie: | 1.1 Articolo in Rivista |
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