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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard, Christopher J; Williams, Peter D; Schulz, Jurgen; Wiscount, Catherine M; Holloway, M Katharine; Loughran, H Marie; Manikowski, Jesse J; Su, Hua-Poo; Bennett, David J; Chang, Lehua; Chu, Xin-Jie; Crespo, Alejandro; Dwyer, Michael P; Keertikar, Kartik; Morriello, Gregori J; Stamford, Andrew W; Waddell, Sherman T; Zhong, Bin; Hu, Bin; Ji, Tao; Diamond, Tracy L; Bahnck-Teets, Carolyn; Carroll, Steven S; Fay, John F; Min, Xu; Morris, William; Ballard, Jeanine E; Miller, Michael D; McCauley, John A.
  • Bungard CJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Williams PD; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Schulz J; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Wiscount CM; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Holloway MK; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Loughran HM; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Manikowski JJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Su HP; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Bennett DJ; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Chang L; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Chu XJ; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Crespo A; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Dwyer MP; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Keertikar K; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Morriello GJ; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Stamford AW; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Waddell ST; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Zhong B; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China.
  • Hu B; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China.
  • Ji T; WuXi AppTec, 288 Fute Zhong Road, Shanghai 200131, China.
  • Diamond TL; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Bahnck-Teets C; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Carroll SS; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Fay JF; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Min X; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Morris W; Merck & Co., Inc., 126 East Lincoln Avenue, Rahway, New Jersey 07065, United States.
  • Ballard JE; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • Miller MD; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
  • McCauley JA; Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
ACS Med Chem Lett ; 8(12): 1292-1297, 2017 Dec 14.
Article en En | MEDLINE | ID: mdl-29259750
ABSTRACT
Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core showed an 60-fold increase in enzyme binding affinity and a 10-fold increase in antiviral activity relative to MK-8718.
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2017 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2017 Tipo del documento: Article