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<p>The present manuscript demonstrated an efficient microwave assisted Multicomponent reaction approach in modifying the existing drug 5-fluorocytosine (Flucytosine). Previously reported flucytosine-based hybrids exhibited antifungal activity largely in combination with standard drugs, therefore not act as standalone agents/drugs. In contrast, the current methodology generated two diversity points on a single molecule by utilizing one class (nucleoside analogue, 5-Fluorocytosine) of antifungals as a reactant and generating the second class (azole) of antifungal within the molecule through GBB reaction approach leads to hybrid pharmacophores with enhanced potential as compared to reported drugs. Among all the tested compounds, compound (4&#xa0;h) depicted higher antifungal activity against <i>Aspergillus fumigatus</i> when compared to reported drugs 5-flucytosine and fluconazole with MIC value of 0.312&#xa0;mg/ml.</p>

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Microwave-assisted GBB-MCR modification of flucytosine for novel bicyclic-azine antifungals with dual diversity points against Aspergillus fumigatus

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年7月7日

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  • Pratibha Shukla,
  • A. K. Narula,
  • Deepa Deswal

摘要

The present manuscript demonstrated an efficient microwave assisted Multicomponent reaction approach in modifying the existing drug 5-fluorocytosine (Flucytosine). Previously reported flucytosine-based hybrids exhibited antifungal activity largely in combination with standard drugs, therefore not act as standalone agents/drugs. In contrast, the current methodology generated two diversity points on a single molecule by utilizing one class (nucleoside analogue, 5-Fluorocytosine) of antifungals as a reactant and generating the second class (azole) of antifungal within the molecule through GBB reaction approach leads to hybrid pharmacophores with enhanced potential as compared to reported drugs. Among all the tested compounds, compound (4 h) depicted higher antifungal activity against Aspergillus fumigatus when compared to reported drugs 5-flucytosine and fluconazole with MIC value of 0.312 mg/ml.