AI Article Synopsis
- Researchers discovered a chemical structure called iminodipyridinopyrimidine (IDPP) while screening compounds to fight the hepatitis C virus (HCV) in lab tests.
- Although IDPP didn't stop HCV from replicating, it was effective in blocking key early and late processes in the virus's life cycle.
- A specific version of IDPP, known as compound 12c, showed strong effectiveness (with an effective concentration of 10 nM), a high safety margin, and good stability in liver microsomes, suggesting it could lead to new treatments for HCV.
Article Abstract
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 (EC = 10 nM), high safety margin (SI > 2000), and an acceptable stability in human and rat liver microsomes (t >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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| http://dx.doi.org/10.1016/j.ejmech.2017.09.010 | DOI Listing |
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