{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,16]],"date-time":"2026-10-16T19:11:59Z","timestamp":1792177919579,"version":"4.4.0"},"reference-count":42,"publisher":"Wiley","issue":"9","license":[{"start":{"date-parts":[[2012,7,17]],"date-time":"2012-07-17T00:00:00Z","timestamp":1342483200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"name":"Ministero dell' Istruzione, dell'Universit\u00e0 e della Ricerca"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Journal of Peptide Science"],"published-print":{"date-parts":[[2012,9]]},"abstract":"<jats:p>Worldwide efforts are underway to develop new antimicrobial agents against bacterial resistance. To identify new compounds with a good antimicrobial profile, we designed and synthesized two series of small cationic antimicrobial peptidomimetics (1\u20138) containing unusual arginine mimetics (to introduce cationic charges) and several aromatic amino acids (bulky moieties to improve lipophilicity). Both series were screened for <jats:italic>in vitro<\/jats:italic> antibacterial activity against a representative panel of Gram\u2010positive (<jats:italic>Staphylococcus aureus<\/jats:italic> and <jats:italic>Staphylococcus epidermidis<\/jats:italic>) and Gram\u2010negative (<jats:italic>Escherichia coli<\/jats:italic> and <jats:italic>Klebsiella pneumoniae<\/jats:italic>) bacterial strains, and <jats:italic>Candida albicans<\/jats:italic>. The biological screening showed that peptidomimetics containing tryptophan residues are endowed with the best antimicrobial activity against <jats:italic>S. aureus<\/jats:italic> and <jats:italic>S. epidermidis<\/jats:italic> in respect to the other synthesized derivatives (MIC values range 7.5\u201350\u2009\u00b5g\/ml). Moreover, small antimicrobial peptidomimetics derivatives 2 and 5 showed an appreciable activity against the tested Gram\u2010negative bacteria and <jats:italic>C. albicans<\/jats:italic>. The most active compounds (1\u20132 and 5\u20136) have been tested against Gram\u2010positive established biofilm, too. Results showed that the biofilm inhibitory concentration values of these compounds were never up to 200\u2009\u00b5g\/ml. The replacement of tryptophan with phenylalanine or tyrosine resulted in considerable loss of the antibacterial action (compounds 3\u20134 and 7\u20138) against both Gram\u2010positive and Gram\u2010negative bacterial strains. Furthermore, by evaluating hemolytic activity, the synthesized compounds did not reveal cytotoxic activities, except for compound 5. 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