Synthesis and evaluation of unsymmetrical heterocyclic thioureas as potent β-glucuronidase inhibitors
Thiourea analogs 1-20 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. The compounds 9 (0.86 ± 0.01 μM), 6 (1.24 ± 0.01 μM), 16 (1.64 ± 0.02 μM) and 15 (2.12 ± 0.02 μM) showed potent activity. Other analogs 1-5, 7, 8, 10, 11, 13, 17, 20 showed better activity t...
| Published in: | Medicinal Chemistry Research |
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| Main Author: | |
| Format: | Article |
| Language: | English |
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Birkhauser Boston
2015
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84937730306&doi=10.1007%2fs00044-015-1369-x&partnerID=40&md5=ffd0582f288ac79483ed2b6ce61d2930 |
| Summary: | Thiourea analogs 1-20 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. The compounds 9 (0.86 ± 0.01 μM), 6 (1.24 ± 0.01 μM), 16 (1.64 ± 0.02 μM) and 15 (2.12 ± 0.02 μM) showed potent activity. Other analogs 1-5, 7, 8, 10, 11, 13, 17, 20 showed better activity than standard drug d-saccharic acid 1,4-lactone (47.34 ± 0.21 μM) ranging 4.36-34.4 μM. All synthetic compounds were characterized by different spectroscopic methods. This study has identified a new class of potent inhibitors β-glucuronidase. © 2015 Springer Science+Business Media New York. |
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| ISSN: | 10542523 |
| DOI: | 10.1007/s00044-015-1369-x |