Výsledky vyhledávání - "Melnick, Michael J."

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Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series

Autor: Krzysztof Appelt, Melnick Michael J, B.‐W. Wu, L. Musick, Mary Ann M. Fuhry, Reich Siegfried Heinz, Mark J. Pino, Jay F. Davies, Anthony J. Trippe

Publikováno v: Journal of Medicinal Chemistry. 39:2781-2794

The design, synthesis, and crystallographic analysis of protein-inhibitor complexes is described for a novel series of nonpeptidic HIV protease (HIV Pr)inhibitors. Beginning with a cocrystal structure of a Phe-Pro peptidomimetic bound to the HIV Pr,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8fb4e29ab3ee5663fc2578cdd634cef
https://doi.org/10.1021/jm960093o

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ChemInform Abstract: Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series

Autor: B.‐W. Wu, Reich Siegfried Heinz, Melnick Michael J, Anthony J. Trippe, Jay F. Davies, L. Musick, Mary Ann M. Fuhry, Krzysztof Appelt, Mark J. Pino

Publikováno v: ChemInform. 27

The design, synthesis, and crystallographic analysis of protein−inhibitor complexes is described for a novel series of nonpeptidic HIV protease (HIV Pr) inhibitors. Beginning with a cocrystal structure of a Phe-Pro peptidomimetic bound to the HIV P

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2ca3482018cf683dac9bf7dcf617aac7
https://doi.org/10.1002/chin.199643072

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Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design

Autor: Heather Dawson, Mitchell Lennert J, Kathy K. Lewis, Stephanie Webber, Dominic Andrada, B.‐W. Wu, Krzysztof Appelt, Anthony J. Trippe, Dan K. Gehlhaar, Deborah Kahil, Dzuy T. Nguyen, Jay F. Davies, Bhasker V. Shetty, L. Musick, Reich Siegfried Heinz, Melnick Michael J, Maha Kosa

Publikováno v: Journal of medicinal chemistry. 39(14)

A series of potent nonpeptide inhibitors of the HIV protease have been identified. Using the structure of compound 3 bound to the HIV protease, bis tertiary amide inhibitor 9 was designed and prepared. Compound 9 was found to be about 17 times more p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1292b4b60ff4c638e6b25940f1f41a5
https://pubmed.ncbi.nlm.nih.gov/8709110

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Protein structure-based design of potent orally bioavailable, nonpeptide inhibitors of human immunodeficiency virus protease

Autor: Mary Ann M. Fuhry, K. K. Lewis, J F Davies nd, D Nguyen, Melnick Michael J, Anthony J. Trippe, Reich Siegfried Heinz, H. Dawson, Mark J. Pino, Krzysztof Appelt

A class of potent nonpeptidic inhibitors of human immunodeficiency virus protease has been designed by using the three-dimensional structure of the enzyme as a guide. By employing iterative protein cocrystal structure analysis, design, and synthesis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b05197d8c5be39f4cdf78cbb175ee46a
https://europepmc.org/articles/PMC42153/