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MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.
Nair, Anilkumar G; Zeng, Qingbei; Selyutin, Oleg; Rosenblum, Stuart B; Jiang, Yueheng; Yang, De-Yi; Keertikar, Kerry; Zhou, Guowei; Dwyer, Michael; Kim, Seong Heon; Shankar, Bandarpalle; Yu, Wensheng; Tong, Ling; Chen, Lei; Mazzola, Robert; Caldwell, John; Tang, Haiqun; Agrawal, Sony; Liu, Rong; Kong, Rong; Ingravallo, Paul; Xia, Ellen; Zhai, Ying; Nomeir, Amin; Asante-Appiah, Ernest; Kozlowski, Joseph A.
Afiliación
  • Nair AG; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: gopinadhan.anilkumar@merck.com.
  • Zeng Q; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Selyutin O; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Rosenblum SB; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Jiang Y; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Yang DY; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Keertikar K; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zhou G; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Dwyer M; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kim SH; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Shankar B; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Yu W; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Tong L; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Chen L; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Mazzola R; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Caldwell J; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Tang H; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Agrawal S; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Liu R; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kong R; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Ingravallo P; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Xia E; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zhai Y; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Nomeir A; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Asante-Appiah E; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Kozlowski JA; Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 28(10): 1954-1957, 2018 06 01.
Article en En | MEDLINE | ID: mdl-29653894
ABSTRACT
HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral fixed dose combination regimen. Herein, we describe the discovery and characterization of silyl proline-containing HCV NS5A inhibitor MK-8325 with good pan-genotype activity and acceptable pharmacokinetic properties.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Prolina / Proteínas no Estructurales Virales / Compuestos Heterocíclicos de 4 o más Anillos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Prolina / Proteínas no Estructurales Virales / Compuestos Heterocíclicos de 4 o más Anillos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article