Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis

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...

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Published in:RSC Advances
Main Author: Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
Format: Article
Language:English
Published: Royal Society of Chemistry 2016
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84964523904&doi=10.1039%2fc5ra28012e&partnerID=40&md5=aa6dbb8465ae9ee063c8c7663e2f2783
id 2-s2.0-84964523904
spelling 2-s2.0-84964523904
Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
2016
RSC Advances
6
40
10.1039/c5ra28012e
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84964523904&doi=10.1039%2fc5ra28012e&partnerID=40&md5=aa6dbb8465ae9ee063c8c7663e2f2783
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.
Royal Society of Chemistry
20462069
English
Article
author Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
spellingShingle Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
author_facet Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
author_sort Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
title Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
title_short Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
title_full Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
title_fullStr Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
title_full_unstemmed Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
title_sort Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
publishDate 2016
container_title RSC Advances
container_volume 6
container_issue 40
doi_str_mv 10.1039/c5ra28012e
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84964523904&doi=10.1039%2fc5ra28012e&partnerID=40&md5=aa6dbb8465ae9ee063c8c7663e2f2783
description 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.
publisher Royal Society of Chemistry
issn 20462069
language English
format Article
accesstype
record_format scopus
collection Scopus
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