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Jin Cai

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Name: 蔡进; Jin Cai
Organization: Southeast University , China
Department: School of Chemistry & Chemical Engineering
Title: Associate Professor(PhD)
Design and synthesis of imidazole N–H substituted amide prodrugs as inhibitors of hepatitis C virus replication
Co-reporter:Xi Zong, Jin Cai, Junqing Chen, Peng Wang, Gaoxin Zhou, Bo Chen, Wei Li, Min Ji
Bioorganic & Medicinal Chemistry Letters 2015 Volume 25(Issue 16) pp:3147-3150
Publication Date(Web):15 August 2015
DOI:10.1016/j.bmcl.2015.06.006
Twenty-five novel imidazole N–H substituted Daclatasvir (BMS-790052, DCV) analogues (8a–8y) were designed and synthesized as potential prodrugs. Structure modifications were performed in order to improve potency and pharmacokinetic (PK) properties. All target compounds were evaluated in a hepatitis C virus (HCV) genotype 1b replicon, and the 2-oxoethyl acetate substituted compound 8t showed similar anti-HCV activity (EC50 = 0.08 nM) to that of the lead compound Daclatasvir. Moreover, the utility of prodrug 8t was demonstrated through similar exposure of the parent compound when the prodrugs were dosed in vivo. PK studies showed that prodrug 8t was an ideal candidate for a slower and sustained release form of Daclatasvir.A design for DCV prodrugs.
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