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Abstract <p>Novel pyrazole–tetrahydropyrimidinethione hybrids were synthesized via a modified Biginelli reaction with a new 1,3-dicarbonyl compound derived from 1-methyl-1<i>H</i>-pyrazol-3-amine and ethyl aceto­acetate. 6-Methyl-<i>N</i>-(1-methyl-1<i>H</i>-pyrazol-3-yl)-4-(substituted phenyl)-2-sulfanylidene-1,2,3,4-tetrahydro­pyrimidine-5-carboxamide derivatives were obtained in high yields using concentrated HCl as a catalyst. The products were characterized by NMR (<sup>1</sup>H and <sup>13</sup>C) spectroscopy and mass spectrometry and evaluated for their antitubercular activity against <i>M. tuberculosis</i> H37Rv. The 4-(trifluoromethyl)phenyl derivative showed the best activity (MIC = 3.12 μg/mL), while 4-fluorophenyl and 4-nitrophenyl analogues showed moderate efficacy (MIC = 6.25 and 12.5 μg/mL, respectively).</p>

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One-Pot Biginelli Synthesis of New Pyrazole–Tetrahydropyrimidinethione Hybrids as Promising Antimycobacterial Agents

  • 期刊论文

  • 发表日期：

    2025年3月1日

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  • H. B. Vasveliya,
  • J. H. Pandya,
  • H. K. Tilavat,
  • A. J. Jivani

摘要

Abstract

Novel pyrazole–tetrahydropyrimidinethione hybrids were synthesized via a modified Biginelli reaction with a new 1,3-dicarbonyl compound derived from 1-methyl-1H-pyrazol-3-amine and ethyl aceto­acetate. 6-Methyl-N-(1-methyl-1H-pyrazol-3-yl)-4-(substituted phenyl)-2-sulfanylidene-1,2,3,4-tetrahydro­pyrimidine-5-carboxamide derivatives were obtained in high yields using concentrated HCl as a catalyst. The products were characterized by NMR (1H and 13C) spectroscopy and mass spectrometry and evaluated for their antitubercular activity against M. tuberculosis H37Rv. The 4-(trifluoromethyl)phenyl derivative showed the best activity (MIC = 3.12 μg/mL), while 4-fluorophenyl and 4-nitrophenyl analogues showed moderate efficacy (MIC = 6.25 and 12.5 μg/mL, respectively).