Synthesis and antifungal activity of 3-(1,3,4-oxadiazol-5-yl)-indoles and 3-(1,3,4-oxadiazol-5-yl)methyl-indoles
| Autor: | Yu-Cheng Gu, David Beattie, Nick Mulholland, Ming-Zhi Zhang, Qiong Chen, John Martin Clough, Guang-Fu Yang, Dianne Irwin |
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| Rok vydání: | 2013 |
| Předmět: |
Pharmacology
Indole test Antifungal Oxadiazoles Antifungal Agents Indoles Natural product Molecular Structure Chemistry medicine.drug_class Organic Chemistry Fungi Biological activity Microbial Sensitivity Tests General Medicine Pimprinine Combinatorial chemistry Structure-Activity Relationship chemistry.chemical_compound Models Chemical Drug Discovery medicine Bioassay Oxazoles |
| Zdroj: | European Journal of Medicinal Chemistry. 63:22-32 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2013.01.038 |
| Popis: | On the basis of the principle of combination of active structural moieties, a modified and efficient synthetic method for three series of novel indole-based 1,3,4-oxadiazoles is described. Bioassays conducted at Syngenta showed that several of the synthesized compounds exhibit higher antifungal activity than pimprinine, the natural product which inspired this synthesis. Two main structural alterations were found to broaden the spectrum of biological activity in most cases. Compounds 3g, 6c, 6e, 6h, 9d, 9e, 9h and 9m (Fig. 1) were identified as the most active on the biological assays, and will be studied further. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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