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<p>A synthesis of 11 new functionalized polycyclic compounds with benzofuran, benzodiazocine, triazene, and hydrazone fragments was developed. Their antileprotic activity against <i>Mycobacterium lufu</i> was studied. It was established that methyl <i>N</i>-{4<i>b</i>,9<i>b</i>-dihydroxy-6-[(methoxycarbonyl)amino]-10-oxo-9<i>b</i>,10-dihydro-4<i>bH</i>-indeno[1,2-<i>b</i>]benzofuran-8-yl}carbamate (MIC 1.0 ± 0 μg/ml, MBC 14 ± 2 μg/ml), 4-methyl-<i>N′</i>-(2-oxo-1,2-dihydro-3<i>H</i>-indol-3-ylidene)benzenesulfonohydrazide (MIC 1.25 ± 0.25 μg/ml, MBC 9 ± 2.52 μg/ml), and 2,4-dihydroxybenzenecarbaldehyde <i>N</i>-(2-oxo-1,2-dihydro-3<i>H</i>-indol-3-ylidene)hydrazone (MIC 1.5 ± 0.29 μg/ml, MBC 12 ± 2.31 μg/ml) were most promising for further research.</p>

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Synthesis and Antileprotic Activity of Compounds with Benzofuran, Indene, Triazene, and Hydrazone Fragments

  • 期刊论文

  • 发表日期：

    2025年5月1日

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  • A. V. Velikorodov,
  • A. S. Zukhairaeva,
  • L. V. Saroyants,
  • E. N. Kutlalieva,
  • E. A. Shustova,
  • A. V. Naumov

摘要

A synthesis of 11 new functionalized polycyclic compounds with benzofuran, benzodiazocine, triazene, and hydrazone fragments was developed. Their antileprotic activity against Mycobacterium lufu was studied. It was established that methyl N-{4b,9b-dihydroxy-6-[(methoxycarbonyl)amino]-10-oxo-9b,10-dihydro-4bH-indeno[1,2-b]benzofuran-8-yl}carbamate (MIC 1.0 ± 0 μg/ml, MBC 14 ± 2 μg/ml), 4-methyl-N′-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)benzenesulfonohydrazide (MIC 1.25 ± 0.25 μg/ml, MBC 9 ± 2.52 μg/ml), and 2,4-dihydroxybenzenecarbaldehyde N-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazone (MIC 1.5 ± 0.29 μg/ml, MBC 12 ± 2.31 μg/ml) were most promising for further research.