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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors. 2017
Christopher J Bungard, and
Peter D Williams, and
Jurgen Schulz, and
Catherine M Wiscount, and
M Katharine Holloway, and
H Marie Loughran, and
Jesse J Manikowski, and
Hua-Poo Su, and
David J Bennett, and
Lehua Chang, and
Xin-Jie Chu, and
Alejandro Crespo, and
Michael P Dwyer, and
Kartik Keertikar, and
Gregori J Morriello, and
Andrew W Stamford, and
Sherman T Waddell, and
Bin Zhong, and
Bin Hu, and
Tao Ji, and
Tracy L Diamond, and
Carolyn Bahnck-Teets, and
Steven S Carroll, and
John F Fay, and
Xu Min, and
William Morris, and
Jeanine E Ballard, and
Michael D Miller, and
John A McCauley
Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, United States.
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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