What is it about?
Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pangenotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV genotypes (GT 1 to 6) of 10d is increased to some extent. Our findings in preclinical tests suggest that the silicon-containing compound 10d could be worthy of continued study as a potential drug candidate.
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Why is it important?
we have successfully applied the carbon/silicon switch strategy to discover new drug candidates. It further demonstrate that this is more than a “patent busting”activity , and it is a powerful tool to improve the overall properties of drugs.
Perspectives
The growing evidence supporting the lack of inherent toxicological issue with silicon, and increasing clinical experience with silicon-containing compounds are important facts that will lead to further investigatment in this innovative med chem tool in the drug-discovery process. It will attract the more attention of medicinal chemists.
Dr Yinsheng Zhang
Chia Tai Tianqing Pharmaceutical Group Co., LTD
Read the Original
This page is a summary of: Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity, European Journal of Medicinal Chemistry, March 2018, Elsevier,
DOI: 10.1016/j.ejmech.2018.02.025.
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