Synthesis and evaluation of unsymmetrical heterocyclic thioureas as potent β-glucuronidase inhibitors
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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.
KeywordsThioureas β-Glucuronidase inhibition Heterocyclic
Authors would like to acknowledge The Ministry of Agriculture (MOA) Malaysia and Universiti Teknologi MARA under MOA Grant File No. 100-RMI/MOA 16/6/2 (1/2013) and Higher Education Commission (HEC) Pakistan, under National Research Program for Universities (Project No. 20-1910) for the financial support.
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