Structure–activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors

[Display omitted] We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved and flattened resistance profiles.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-11, Vol.26 (21), p.5354-5360
Hauptverfasser:	Tong, Ling, Yu, Wensheng, Coburn, Craig A., Chen, Lei, Selyutin, Oleg, Zeng, Qingbei, Dwyer, Michael P., Nair, Anilkumar G., Shankar, Bandarpalle B., Kim, Seong Heon, Yang, De-Yi, Rosenblum, Stuart B., Ruck, Rebecca T., Davies, Ian W., Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Liu, Rong, Agrawal, Sony, Carr, Donna, Curry, Stephanie, McMonagle, Patricia, Bystol, Karin, Lahser, Frederick, Ingravallo, Paul, Chen, Shiying, Asante-Appiah, Ernest, Kozlowski, Joseph A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral Agents - chemistry Antiviral Agents - pharmacology Benzofurans - chemistry Benzofurans - pharmacology Direct-acting antiviral agents Elbasvir HCV infection treatment HCV NS5A inhibitor Imidazoles - chemistry Imidazoles - pharmacology Indole based tetracyclic core Indoles - chemistry MK-8742 Proline - chemistry Structure-Activity Relationship Viral Nonstructural Proteins - antagonists & inhibitors
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Zusammenfassung:	[Display omitted] We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved and flattened resistance profiles.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2016.08.097