期刊
APPLIED SCIENCES-BASEL
卷 12, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/app12115571
关键词
antimicrobial; antibiofilm; N-acyl-alpha-amino acid; 4H-1,3-oxazol-5-one; N-acyl-alpha-amino acid ester; N-acyl-alpha-amino ketone; 1,3-oxazole
类别
资金
- Carol Davila University of Medicine and Pharmacy, Bucharest, Romania
In this study, the antimicrobial activity of 49 compounds derived from alanine or phenylalanine was evaluated. These compounds showed promising antimicrobial and antibiofilm activity depending on their chemical scaffold and lipophilic character, as determined through in silico and in vitro assays.
In this paper, we report on the antimicrobial activity assessment of 49 compounds previously synthesized as derivatives of alanine or phenylalanine that incorporate a 4-(4-X-phenylsulfonyl)phenyl fragment (X = H, Cl, or Br), namely 21 acyclic compounds (6 x N-acyl-alpha-amino acids, 1 x N-acylct-amino acid ester, and 14 x N-acyl-alpha-amino ketones) and 28 pentatomic heterocycles from the oxazole-based compound class (6 x 4H-1,3-oxazol-5-ones, 16 x 5-aryl-1,3-oxazoles, and 6 x ethyl 1,3-oxazol-5-yl carbonates). Both in silico and in vitro qualitative and quantitative assays were used to investigate the antimicrobial potential of these derivatives against planktonic and biofilm-embedded microbial strains. Some of the tested compounds showed promising antimicrobial and antibiofilm activity depending on their chemical scaffold and lipophilic character.
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