Seven mutant forms of the antibacterial peptide apidaecin with increased activity were created by combinatorial mutagenesis targeted to the three N-terminal amino acid residues that had previously been identified as a nonessential region. An in vitro MIC assay revealed that the amino acid substitutions in the functionally variable region were effective in improving differential activity toward the four gram-negative bacteria tested, while a gram-positive bacterium was unaffected.
Twenty N,N'-dialkylpolymethylendiamine derivatives were synthesized, and a study was made of their antimicrobial activities in vitro against four oral microorganisms which are related to dental caries. The maximum activity was shown by N,N'-dinonyl or N,N'-didecyl derivatives among the complete homologous series of compounds studied.
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