In Silico and In Vitro Assessment of Antimicrobial and Antibiofilm Activity of Some 1,3-Oxazole-Based Compounds and Their Isosteric Analogues

Autor: Theodora-Venera Apostol, Mariana Carmen Chifiriuc, George Mihai Nitulescu, Octavian Tudorel Olaru, Stefania-Felicia Barbuceanu, Laura-Ileana Socea, Elena Mihaela Pahontu, Crina Maria Karmezan, Luminita Gabriela Marutescu
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Applied Sciences, Vol 12, Iss 11, p 5571 (2022)
Druh dokumentu: article
ISSN: 2076-3417
DOI: 10.3390/app12115571
Popis: 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 × N-acyl-α-amino acids, 1 × N-acyl-α-amino acid ester, and 14 × N-acyl-α-amino ketones) and 28 pentatomic heterocycles from the oxazole-based compound class (6 × 4H-1,3-oxazol-5-ones, 16 × 5-aryl-1,3-oxazoles, and 6 × 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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