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<p>A simple and efficient method was employed for the synthesis of novel hydrazones derived from 2-mercaptobenzothiazole, yielding structurally diverse Schiff base of benzothiazole derivatives (<b>2–11</b>) in high yields (76–96%). The synthesized hydrazones were fully characterized using FT-IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HRMS. Their antimicrobial and bactericidal activities were systematically evaluated against Gram-positive and Gram-negative bacterial isolates. Notably, compounds <b>4</b> and <b>9</b> exhibited the highest potency against Gram-positive bacteria, particularly <i>Bacillus subtilis</i> and <i>Bacillus polymyxa</i>, with low minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values. Against Gram-negative bacteria, compound <b>4</b> demonstrated the most significant activity, especially against <i>Pseudomonas aeruginosa</i> and <i>Escherichia coli</i>. In contrast, compounds <b>6</b> and<b> 7</b> displayed minimal or no antimicrobial activity. Streptomycin, used as a reference, showed greater efficacy against Gram-positive bacteria than Gram-negative bacteria. The findings highlight compounds <b>4</b> is a promising broad-spectrum antimicrobial candidate, warranting further investigation through mechanistic studies, toxicity assessments, and in vivo evaluations to explore their therapeutic potential.</p>

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Design, Synthesis, and Antibacterial Assessment of Novel Schiff Bases Derived from 2-Mercaptobenzothiazole

  • 期刊论文

  • 发表日期：

    2025年8月22日

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  • Olajide B. Omoyeni,
  • Francis J. Faleye,
  • Olubunmi A. Akinwunmi,
  • Olugbenga K. Popoola,
  • Felix O. Gboyero,
  • Nusrat O. Omisore

摘要

A simple and efficient method was employed for the synthesis of novel hydrazones derived from 2-mercaptobenzothiazole, yielding structurally diverse Schiff base of benzothiazole derivatives (2–11) in high yields (76–96%). The synthesized hydrazones were fully characterized using FT-IR, 1H-NMR, 13C-NMR, and HRMS. Their antimicrobial and bactericidal activities were systematically evaluated against Gram-positive and Gram-negative bacterial isolates. Notably, compounds 4 and 9 exhibited the highest potency against Gram-positive bacteria, particularly Bacillus subtilis and Bacillus polymyxa, with low minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values. Against Gram-negative bacteria, compound 4 demonstrated the most significant activity, especially against Pseudomonas aeruginosa and Escherichia coli. In contrast, compounds 6 and 7 displayed minimal or no antimicrobial activity. Streptomycin, used as a reference, showed greater efficacy against Gram-positive bacteria than Gram-negative bacteria. The findings highlight compounds 4 is a promising broad-spectrum antimicrobial candidate, warranting further investigation through mechanistic studies, toxicity assessments, and in vivo evaluations to explore their therapeutic potential.