Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties

In this study, twentythree trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties were designed and synthesized. These compounds were confirmed structurally through IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, and HRMS analyses. Bioassay results revealed that some of the synthesized compounds exhibited higher antifungal activity compared to commercial drug. Particularly, compounds <b>7s</b> and <b>7t</b> demonstrated antifungal rates of 80.13% and 81.70% against <i>Sclerotinia sclerotiorum</i> at 50 <i>μ</i>g/mL, outperforming the control agent Pyrimethanil (68.39%). Furthermore, their EC<sub>50</sub> values of 14.68 and 13.06 <i>μ</i>g/mL, respectively, were better than that of Pyrimethanil (46.94 <i>μ</i>g/mL). These findings suggest that compounds <b>7s</b> and <b>7t</b> hold promise for future drug development due to their efficient synthesis and notable biological activities.

Publication Details

Journal
Figshare
Published
2025-01-01
DOI
https://doi.org/10.6084/m9.figshare.28690385.v1
Primary Topic
Synthesis and biological activity
Type
article
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article

Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties

Figshare
Synthesis and biological activity
article

Synthesis, antifungal and antibacterial evaluation of trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties

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Abstract

In this study, twentythree trifluoromethylpyrimidine derivatives containing 1,3,4-thiadiazole and 1,2,4-triazole thioether moieties were designed and synthesized. These compounds were confirmed structurally through IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, and HRMS analyses. Bioassay results revealed that some of the synthesized compounds exhibited higher antifungal activity compared to commercial drug. Particularly, compounds <b>7s</b> and <b>7t</b> demonstrated antifungal rates of 80.13% and 81.70% against <i>Sclerotinia sclerotiorum</i> at 50 <i>μ</i>g/mL, outperforming the control agent Pyrimethanil (68.39%). Furthermore, their EC<sub>50</sub> values of 14.68 and 13.06 <i>μ</i>g/mL, respectively, were better than that of Pyrimethanil (46.94 <i>μ</i>g/mL). These findings suggest that compounds <b>7s</b> and <b>7t</b> hold promise for future drug development due to their efficient synthesis and notable biological activities.

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Synthesis and biological activity
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