Synthesis of sulfadiazinyl acyl/aryl thiourea derivatives as calf intestinal alkaline phosphatase inhibitors, pharmacokinetic properties, lead optimization, Lineweaver-Burk plot evaluation and binding analysis.

Bioorganic & Medicinal Chemistry(2018)

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摘要
•Sulfadiazine based acyl/aryl thioureas has been synthesized and were screen against calf intestinal alkaline phosphatase (CIAP).•Compound 4c was found to be potent derivative in the series.•Lineweaver-Burk plots revealed mixed type of enzyme inhibition mechanism.•All the derivatives 4a–4j obey Lipinski’s Rule.
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关键词
Sulfadiazine drug derivatives,Acyl/aryl thioureas,Calf intestinal alkaline phosphatase,Kinetic studies,Pharmacokinetics,Binding analysis
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