Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies
3-Thiazolylcoumarin derivatives 1–14 were synthesized via one-pot two step reactions, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed inhibitory activity in the range of IC50 = 0.12 ± 0.01–16.20 ± 0.23 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM), an...
| Published in: | European Journal of Medicinal Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
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Elsevier Masson SAS
2016
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84976472588&doi=10.1016%2fj.ejmech.2016.06.037&partnerID=40&md5=f498e2221e64c88ef04a256a505b03b8 |
| Summary: | 3-Thiazolylcoumarin derivatives 1–14 were synthesized via one-pot two step reactions, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed inhibitory activity in the range of IC50 = 0.12 ± 0.01–16.20 ± 0.23 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM), and also found to be nontoxic. Molecular docking study was carried out in order to establish the structure-activity relationship (SAR) which demonstrated that electron rich centers at one and electron withdrawing centers at the other end of the molecules showed strong inhibitory activity. All the synthesized compounds were characterized by spectroscopic techniques such as EI-MS, HREI-MS,1H NMR and13C NMR. CHN analysis was also performed. © 2016 Elsevier Masson SAS |
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| ISSN: | 2235234 |
| DOI: | 10.1016/j.ejmech.2016.06.037 |