Effects of the aryl linker and the aromatic substituent on the anti-HCV activities of aryl diketoacid (ADK) analogues

…, SY Kang, SJ Lee, HS Park, DE Kim, Y Chong

Index: Kim, Jinyoung; Kim, Ki-Sun; Lee, Hyo Seon; Park, Kwang-Su; Park, Sun Young; Kang, Seock-Yong; Lee, Soo Jae; Park, Hyung Soon; Kim, Dong-Eun; Chong, Youhoon Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 16 p. 4661 - 4665

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Citation Number: 14

Abstract

Based on our pharmacophore model of the aryl diketoacids (ADKs), we designed and prepared a series of novel ADK analogues, which showed potent inhibitory activities against the NS5B polymerase in the submicromolar range. Pharmacophore-guided docking study revealed that the antiviral activities of the ADKs are highly dependent upon the aryl linker as well as the size and position of the aromatic substituent. It is of another importance that, ...