Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors

[Image: see text] 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...

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Publicado no:ACS Med Chem Lett
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2017
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5733263/
https://ncbi.nlm.nih.gov/pubmed/29259750
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00386
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