Thiadiazole derivatives as New Class of β-glucuronidase inhibitors
Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 ± 0.01-58.06 ± 1.60 μM as compare to standard d-saccharic acid 1,4-lacton...
| Published in: | Bioorganic and Medicinal Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
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Elsevier Ltd
2016
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84961126449&doi=10.1016%2fj.bmc.2016.03.020&partnerID=40&md5=77d703360524d538921852b32b015a5b |
| Summary: | Thiadiazole derivatives 1-24 were synthesized via a single step reaction and screened for in vitro β-glucuronidase inhibitory activity. All the synthetic compounds displayed good inhibitory activity in the range of IC50 = 2.16 ± 0.01-58.06 ± 1.60 μM as compare to standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Molecular docking study was conducted in order to establish the structure-activity relationship (SAR) which demonstrated that thiadiazole as well as both aryl moieties (aryl and N-aryl) involved to exhibit the inhibitory potential. All the synthetic compounds were characterized by spectroscopic techniques 1H, 13C NMR, and EIMS. © 2016 Elsevier Ltd. All rights reserved. |
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| ISSN: | 9680896 |
| DOI: | 10.1016/j.bmc.2016.03.020 |