1,2,4-Oxadiazole-Based Bio-Isosteres of Benzamides: Synthesis, Biological Activity and Toxicity to Zebrafish Embryo
To discover new compounds with broad spectrum and high activity, we designed a series of novel benzamides containing 1,2,4-oxadiazole moiety by bioisosterism, and 28 benzamides derivatives with antifungal activity were synthesized. These compounds were evaluated against four fungi: <i>Botrytis...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-02-01
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| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/22/5/2367 |
| Summary: | To discover new compounds with broad spectrum and high activity, we designed a series of novel benzamides containing 1,2,4-oxadiazole moiety by bioisosterism, and 28 benzamides derivatives with antifungal activity were synthesized. These compounds were evaluated against four fungi: <i>Botrytis cinereal</i>, <i>FusaHum graminearum</i>, <i>Marssonina mali</i>, and <i>Thanatephorus cucumeris</i>. The results indicated that most of the compounds displayed good fungicidal activities, especially against <i>Botrytis cinereal</i>. For example, <b>10a</b> (84.4%), <b>10d</b> (83.6%), <b>10e</b> (83.3%), <b>10f</b> (83.1%), <b>10i</b> (83.3%), and <b>10l</b> (83.6%) were better than pyraclostrobin (81.4%) at 100 mg/L. In addition, the acute toxicity of <b>10f</b> to zebrafish embryo was 20.58 mg/L, which was classified as a low-toxicity compound. |
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| ISSN: | 1661-6596 1422-0067 |