Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
Compounds 1-18, new oxadiazole-thiosemicarbazide hybrids, were synthesized using a five-step reaction sequence in excellent yields. All the synthesized analogs exhibited exceptional α-glucosidase inhibitory potentials in the range of 0.4-38.1 μM. Among the current series, it was observed that the fl...
| Published in: | RSC Advances |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Royal Society of Chemistry
2016
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84964523904&doi=10.1039%2fc5ra28012e&partnerID=40&md5=aa6dbb8465ae9ee063c8c7663e2f2783 |
| Summary: | Compounds 1-18, new oxadiazole-thiosemicarbazide hybrids, were synthesized using a five-step reaction sequence in excellent yields. All the synthesized analogs exhibited exceptional α-glucosidase inhibitory potentials in the range of 0.4-38.1 μM. Among the current series, it was observed that the fluoro-substituted analogues were exceptionally potent inhibitors of α-glucosidase. The study provides a proof of concept that inductively strong electron withdrawing groups result in enhanced inhibitory potentials. The binding interactions of these compounds were analyzed in silico for possible prediction and identification of the improved inhibitory potential. © The Royal Society of Chemistry 2016. |
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| ISSN: | 20462069 |
| DOI: | 10.1039/c5ra28012e |