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.
Highlights
Hepatitis C virus (HCV) infection afflicts ~150 million people worldwide (~3% of the global population), with approximately 3–4 million new cases occurring annually [1]
To investigate the effects of different moieties or functional groups attached to the core, our research group synthesized four series of imidazole–coumarin conjugated compounds
Conjugates with a coumarin moiety attached at the C(2)-position of the imidazole group via a thiomethylene joint were synthesized
Summary
Hepatitis C virus (HCV) infection afflicts ~150 million people worldwide (~3% of the global population), with approximately 3–4 million new cases occurring annually [1]. The traditional therapeutic treatment involves administering interferon α-2 or its PEGylated form, either alone or in combination with ribavirin [2,3]. In 2011, boceprevir and telaprevir were approved for the treatment of chronic hepatitis C genotype 1 infection in combination with peg-interferon α and ribavirin. The above therapeutic treatments, still have substantial adverse effects [6]. During the past two years, the U.S Food and Drug Administration has approved HarvoniTM (ledipasvir/sofosbuvir), simeprevir, sofosbuvir, and Viekira PakTM (ombitasvir/paritaprevir/ritonavir tablet; dasabuvir tablet). HarvoniTM and Viekira PakTM are combination pills in which each of the Molecules 2016, 21, 228; doi:10.3390/molecules21020228 www.mdpi.com/journal/molecules
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