Structural optimization of cyclic sulfonamide based novel HIV-1 protease inhibitors to picomolar affinities guided by X-ray crystallographic analysis

Autor: Ganguly, Ashit K., Alluri, Sesha S., Wang, Chih-Hung, Antropow, Alyssa, White, Alex, Caroccia, Danielle, Biswas, Dipshikha, Kang, Eunhee, Zhang, Li-Kang, Carroll, Steven S., Burlein, Christine, Fay, John, Orth, Peter, Strickland, Corey

Publikováno v: In Tetrahedron 6 May 2014 70(18):2894-2904

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Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.

Autor: Neelamkavil SF; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Agrawal S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Bara T; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Bennett C; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Bhat S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Biswas D; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Brockunier L; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Buist N; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Burnette D; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Cartwright M; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Chackalamannil S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Chase R; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Chelliah M; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Chen A; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Clasby M; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Colandrea VJ; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Davies IW; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Eagen K; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Guo Z; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Han Y; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Howe J; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Jayne C; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Josien H; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Kargman S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Marcantonio K; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Miao S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Miller R; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Nolting A; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Pinto P; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Rajagopalan M; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Ruck RT; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Shah U; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Soriano A; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Sperbeck D; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Velazquez F; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Wu J; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Xia Y; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States., Venkatraman S; Merck Research Laboratories , Kenilworth, New Jersey 07033, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Dec 22; Vol. 7 (1), pp. 111-6. Date of Electronic Publication: 2015 Dec 22 (Print Publication: 2016).