Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group

[Image: see text] A novel HIV protease inhibitor was designed using a morpholine core as the aspartate binding group. Analysis of the crystal structure of the initial lead bound to HIV protease enabled optimization of enzyme potency and antiviral activity. This afforded a series of potent orally bio...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Bungard, Christopher J., Williams, Peter D., Ballard, Jeanine E., Bennett, David J., Beaulieu, Christian, Bahnck-Teets, Carolyn, Carroll, Steve S., Chang, Ronald K., Dubost, David C., Fay, John F., Diamond, Tracy L., Greshock, Thomas J., Hao, Li, Holloway, M. Katharine, Felock, Peter J., Gesell, Jennifer J., Su, Hua-Poo, Manikowski, Jesse J., McKay, Daniel J., Miller, Mike, Min, Xu, Molinaro, Carmela, Moradei, Oscar M., Nantermet, Philippe G., Nadeau, Christian, Sanchez, Rosa I., Satyanarayana, Tummanapalli, Shipe, William D., Singh, Sanjay K., Truong, Vouy Linh, Vijayasaradhi, Sivalenka, Wiscount, Catherine M., Vacca, Joseph P., Crane, Sheldon N., McCauley, John A.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4948015/
https://ncbi.nlm.nih.gov/pubmed/27437081
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00135
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