Article
Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase.
Bioorganic & medicinal chemistry letters - 15 Apr 2008
Donner Pamela L, Xie Qinghua, Pratt John K, Maring Clarence J, Kati Warren, Jiang Wen, Liu Yaya, Koev Gennadiy, Masse Sherie, Montgomery Debra, Molla Akhter, Kempf Dale J
Abstract excerpt
In our program to discover non-nucleoside, small molecule inhibitors of genotype 1 HCV polymerase, we investigated a series of promising analogs based on a benzothiadiazine screening hit that contains an ABCD ring system. After demonstrating that a methylsulfonylamino D-ring substituent increased the enzyme potency into the low nanomolar range, we explored a minimum core required for activity by truncating to a...
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