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Recently, in a program designed to improve the metabolic stability of the HCV inhibitor GSK5852, N-benzoxaborole benzofuran (GSK8175) emerged as a clinical candidate that not only retains the broad-spectrum activity… Click to show full abstract
Recently, in a program designed to improve the metabolic stability of the HCV inhibitor GSK5852, N-benzoxaborole benzofuran (GSK8175) emerged as a clinical candidate that not only retains the broad-spectrum activity against HCV subgenomic replicons but is free of the N-benzylboronic acid structure, which is a metabolic liability, and probably the cause of low in vivo clearance in preclinical species. This Viewpoint discusses some medicinal chemistry issues involved in the identification of GSK8175.
Keywords:
benzoxaborole benzofuran;
chemistry;
clinical candidate;
benzofuran gsk8175;
metabolic liability
Journal Title: Journal of medicinal chemistry
Year Published: 2019
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Journal Title: Journal of medicinal chemistry
Year Published: 2019
Link to full text (if available)
Share on Social Media: Sign Up to like & get
recommendations!