European Journal of Medicinal Chemistry p. 65 - 73 (2017)
Update date:2022-07-30
Topics:
Park, Dong-Sik
Jo, Eunji
Choi, Jihyun
Lee, MyungEun
Kim, Soohyun
Kim, Hee-Young
Nam, Jiyon
Ahn, Sujin
Hwang, Jong Yeon
Windisch, Marc Peter
Upon high-throughput screening of synthetic small molecule libraries with the infectious hepatitis C virus (HCV) cell culture system, we identified an iminodipyridinopyrimidine (IDPP) scaffold. IDPP did not inhibit HCV replication, but exhibited very potent inhibitory activity on early and late steps of HCV life cycle. Applying an intensive structure-activity relationship (SAR) study, a promising IDPP Lead compound (12c) with excellent potency (EC50 = 10 nM), high safety margin (SI > 2000), and an acceptable stability in human and rat liver microsomes (t1/2 >60 min) was identified. Overall, our results suggest that the IDPP scaffold could be used for the development of novel HCV interventions.
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