Article
Redesigning of the cap conformation and symmetry of the diphenylethyne core to yield highly potent pan-genotypic NS5A inhibitors with high potency and high resistance barrier.
European journal of medicinal chemistry - 5 Feb 2022
Abdallah Mennatallah, Hamed Mostafa M, Frakolaki Efseveia, Katsamakas Sotirios, Vassilaki Niki, Bartenschlager Ralf, Zoidis Grigoris, Hirsch Anna K H, Abdel-Halim Mohammad, Abadi Ashraf H
Abstract excerpt
Herein, we report the discovery of several NS5A inhibitors with potency against HCV genotype 1b in the picomolar range. Compounds (15, 33) were of extremely high potency against HCV genotype 1b (EC50 ≈ 1 pM), improved activity against genotype 3a (GT 3a) and good metabolic stability. We studied the impact of changing the cap conformation relative to the diphenylethyne core and/or compound symmetry on both potency...
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