Novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone: A new class of β-glucuronidase inhibitors and in silico studies
Abstract A library of novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone (3a-3r) was synthesized and evaluated for their potential as β-glucuronidase inhibitors. Several compounds such as 3a-3d, 3e-3j, 3l-3o, 3q and 3r showed excellent inhibitory potentials much better than the sta...
| Published in: | Bioorganic and Medicinal Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
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Elsevier Ltd
2015
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84937437445&doi=10.1016%2fj.bmc.2015.04.081&partnerID=40&md5=9b76ed8fe1d93152c79a084d6a809102 |
| Summary: | Abstract A library of novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone (3a-3r) was synthesized and evaluated for their potential as β-glucuronidase inhibitors. Several compounds such as 3a-3d, 3e-3j, 3l-3o, 3q and 3r showed excellent inhibitory potentials much better than the standard (IC50 = 48.4 ± 1.25 μM: d-saccharic acid 1,4-lactone). All the synthesized compounds were characterized satisfactorily by using different spectroscopic methods. We further evaluated the interaction of the active compounds and the enzyme active site with the help of docking studies. © 2015 Elsevier Ltd. |
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| ISSN: | 9680896 |
| DOI: | 10.1016/j.bmc.2015.04.081 |