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<p>The antibacterial properties <i>in vitro</i> against strains of Gram-positive and Gram-negative bacteria were studied, MIC values were established, and theoretical indices of the lipophilicity and solubility and topological polar surface area indices were calculated for a number of condensation products of 4-oxo-4-arylbutanoic acids with aliphatic, aromatic, and aliphatic-aromatic <i>N</i>,<i>N</i>- and <i>N</i>,<i>O</i>-binucleophiles of both open structure (amides) and cyclic structure (bi- and tricycles depending on the nucleophile used). Among the synthesized 3a-phenyltetrahydrobenzopyrrolo[1,2-<i>a</i>]imidazol-1-one, 3a-phenyldihydrobenzopyrrolo[2,1-<i>b</i>]oxazol-1-one, phenyl- and 4-methoxyphenyltetrahydro[2,1-<i>b</i>]quinazolin-1-one, phenyldecahydropyrrolo[1,2-<i>a</i>][1,3]-diazecin-10(2<i>H</i>)-one, and amides of 4-oxobutanoic acids, those with the highest lipophilicity index values in the series, 3a-phenyldihydrobenzopyrrolo[2,1-<i>b</i>]oxazol-1-one and phenyldecahydropyrrolo[1,2-<i>a</i>][1,3]-diazecin-10(2<i>H</i>)-one, were the most active. The effect of the latter was comparable to the bactericidal effect of the antibiotics kanamycin and tetracycline at active concentrations of 30 mg/mL.</p>

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Antibacterial Activity In Vitro and Assessment of Bioavailability In Silico of Condensation Products of 4-Oxo-4-Arylbutanoic Acids with N,N- and N,O-Binucleophiles

  • 期刊论文

  • 发表日期：

    2025年4月1日

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  • E. Sklyar,
  • S. S. Evstigneeva,
  • A. Yu. Yegorova,
  • V. S. Grinev

摘要

The antibacterial properties in vitro against strains of Gram-positive and Gram-negative bacteria were studied, MIC values were established, and theoretical indices of the lipophilicity and solubility and topological polar surface area indices were calculated for a number of condensation products of 4-oxo-4-arylbutanoic acids with aliphatic, aromatic, and aliphatic-aromatic N,N- and N,O-binucleophiles of both open structure (amides) and cyclic structure (bi- and tricycles depending on the nucleophile used). Among the synthesized 3a-phenyltetrahydrobenzopyrrolo[1,2-a]imidazol-1-one, 3a-phenyldihydrobenzopyrrolo[2,1-b]oxazol-1-one, phenyl- and 4-methoxyphenyltetrahydro[2,1-b]quinazolin-1-one, phenyldecahydropyrrolo[1,2-a][1,3]-diazecin-10(2H)-one, and amides of 4-oxobutanoic acids, those with the highest lipophilicity index values in the series, 3a-phenyldihydrobenzopyrrolo[2,1-b]oxazol-1-one and phenyldecahydropyrrolo[1,2-a][1,3]-diazecin-10(2H)-one, were the most active. The effect of the latter was comparable to the bactericidal effect of the antibiotics kanamycin and tetracycline at active concentrations of 30 mg/mL.