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  • Title: Synthesis and Structure-Activity Relationships of Imidazole-Coumarin Conjugates against Hepatitis C Virus.
    Author: Tsay SC, Lin SY, Huang WC, Hsu MH, Hwang KC, Lin CC, Horng JC, Chen IC, Hwu JR, Shieh FK, Leyssen P, Neyts J.
    Journal: Molecules; 2016 Feb 18; 21(2):. PubMed ID: 26901180.
    Abstract:
    A series of new conjugated compounds with a -SCH₂- linkage were synthesized by chemical methods from imidazole and coumarin derivatives. The experimental results indicate that of the twenty newly synthesized imidazole-coumarin conjugates, three of them exhibited appealing EC50 values (5.1-8.4 μM) and selective indices >20 against hepatitis C virus. Their potency and selectivity were increased substantially by modification of their structure with two factors: imidazole nucleus with a hydrogen atom at the N(1) position and coumarin nucleus with a substituent, such as Cl, F, Br, Me, and OMe. These guidelines provide valuable information for further development of conjugated compounds as anti-viral agents.
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