Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases
Biscoumarin analogs 1-18 have been synthesized, characterized by EI-MS and 1H NMR and evaluated for α-glucosidase inhibitory potential. All compounds showed variety of α-glucosidase inhibitory potential ranging in between 13.5 ± 0.39 and 104.62 ± 0.3 μM when compared with standard acarbose having IC...
| Published in: | Bioorganic Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Academic Press Inc.
2015
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84942945274&doi=10.1016%2fj.bioorg.2015.09.004&partnerID=40&md5=550982f9b5743c78d8ad9a3e07dd6408 |
| Summary: | Biscoumarin analogs 1-18 have been synthesized, characterized by EI-MS and 1H NMR and evaluated for α-glucosidase inhibitory potential. All compounds showed variety of α-glucosidase inhibitory potential ranging in between 13.5 ± 0.39 and 104.62 ± 0.3 μM when compared with standard acarbose having IC50 value 774.5 ± 1.94 μM. The binding interactions of the most active analogs were confirmed through molecular docking. The compounds showed very good interactions with enzyme. All synthesized compounds 1-18 are new. Our synthesized compounds can further be studied to developed lead compounds. © 2015 Elsevier Inc. All rights reserved. |
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| ISSN: | 452068 |
| DOI: | 10.1016/j.bioorg.2015.09.004 |