Oxindole based oxadiazole hybrid analogs: Novel α -glucosidase inhibitors
Тип публикации: Journal Article
Дата публикации: 2018-02-01
scimago Q1
wos Q1
БС1
SJR: 0.786
CiteScore: 8.3
Impact factor: 4.7
ISSN: 00452068, 10902120
PubMed ID:
29223804
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Краткое описание
Inhibition of α-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these α-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of α-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC50 values ranging between 1.25 ± 0.05 and 268.36 ± 4.22 µM when compared with the standard drug acarbose having IC50 value 895.09 ± 2.04 µM. Our study identifies novel series of potent α-glucosidase inhibitors and further investigation on this may led to the lead compounds. A structure activity relationship has been established for all compounds. The interactions of the active compounds and enzyme active site were established with the help of molecular docking studies.
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ГОСТ
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Taha M. et al. Oxindole based oxadiazole hybrid analogs: Novel α -glucosidase inhibitors // Bioorganic Chemistry. 2018. Vol. 76. pp. 273-280.
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Taha M., Imran S., Rahim F., Wadood A., A Khan N. Oxindole based oxadiazole hybrid analogs: Novel α -glucosidase inhibitors // Bioorganic Chemistry. 2018. Vol. 76. pp. 273-280.
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TY - JOUR
DO - 10.1016/j.bioorg.2017.12.001
UR - https://doi.org/10.1016/j.bioorg.2017.12.001
TI - Oxindole based oxadiazole hybrid analogs: Novel α -glucosidase inhibitors
T2 - Bioorganic Chemistry
AU - Taha, Muhammad
AU - Imran, Syahrul
AU - Rahim, Fazal
AU - Wadood, Abdul
AU - A Khan, Naveed
PY - 2018
DA - 2018/02/01
PB - Elsevier
SP - 273-280
VL - 76
PMID - 29223804
SN - 0045-2068
SN - 1090-2120
ER -
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BibTex (до 50 авторов)
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@article{2018_Taha,
author = {Muhammad Taha and Syahrul Imran and Fazal Rahim and Abdul Wadood and Naveed A Khan},
title = {Oxindole based oxadiazole hybrid analogs: Novel α -glucosidase inhibitors},
journal = {Bioorganic Chemistry},
year = {2018},
volume = {76},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.bioorg.2017.12.001},
pages = {273--280},
doi = {10.1016/j.bioorg.2017.12.001}
}