Zobrazeno 1 - 10 of 54 pro vyhledávání: '"William A. Slusarchyk"'
1
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Autor: David P. Rotella, Robert Zahler, David J. Augeri, Timur Gungor, Aiying Wang, William S. Slusarchyk, Scott A. Bolton, James C. Sutton, Jeffrey A. Robl, Zulan Pi, Karnail S. Atwal, Ligaya M. Simpkins, Yajun Liu, Chet Kwon, Lawrence G. Hamann, Rex A. Parker, Guohua Zhao, Mark S. Kirby, Zhong Sun, David R. Magnin, Jovita Marcinkeviciene, James G. Robertson
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:6476-6480
The synthesis and structure–activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efc358df323e8065d6c640de03adf2c4
https://doi.org/10.1016/j.bmcl.2007.09.090
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2
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase
Autor: Wei Meng, Martin L. Ogletree, Robert Zahler, James C. Sutton, Guohua Zhao, Steven M. Seiler, G. A. Jacobs, Arvind Mathur, Zulan Pi, Treuner Uwe D, Karen S. Hartl, Gregory S. Bisacchi, William A. Slusarchyk, Scott A. Bolton
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:2227-2231
Azetidinones such as BMS-363131 (2) and BMS-363130 (3), which contain a guanidine group in the C-3 side chain were previously shown to be very potent inhibitors of human tryptase with high selectivity versus other serine proteases, including trypsin.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6aed84872ee718c1328d0681d89f4806
https://doi.org/10.1016/j.bmcl.2004.02.011
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3
A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors
Autor: David A. Gordon, Ligaya M. Simpkins, William A. Slusarchyk, David R. Magnin, Chongqing Sun, Prakash Taunk, Jamil Haris, Lori Kunselman, Ying Chen, Scott A. Biller, John R. Wetterau, Fergal Connolly, Jeffrey A. Robl, John K. Dickson, Talal Sabrah, Thomas Harrity, Shih-Jung Lan, Richard B. Sulsky, Tammy C. Wang
Publikováno v: Journal of Medicinal Chemistry. 44:851-856
A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in place of a piperidine group afforded potent inhibitors of MTP in vitro which were weakly activ
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be68a36dea52f3ff5c3ddb2e2c700e83
https://doi.org/10.1021/jm000494a
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5
BMS-200475, a novel carbocyclic 2′-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro
Autor: G. A. Jacobs, S. Innaimo, William A. Slusarchyk, O. Kocy, J.E. Sundeen, Robert Zahler, Alain Martel, M. G. Young, Sam T. Chao, Jean-Paul Daris, Gregory S. Bisacchi, Richard J. Colonno, C. Bachard, Philippe Lapointe, Z. Merchant
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:127-132
BMS-200475, a novel carbocyclic analog of 2′-deoxyguanosine, is a potent inhibitor of hepatitis B virus in vitro (ED50 = 3 nM) with relatively low cytotoxicity (CC50 = 21–120 μM). A practical 10-step asymmetric synthesis was developed affording
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4f254f1ed35e99aef5acd2c244ca770e
https://doi.org/10.1016/s0960-894x(96)00594-x
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6
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold
Autor: Karen S. Hartl, Steven M. Seiler, Guohua Zhao, William A. Slusarchyk, Eddie C.-K. Liu, Daniel L. Cheney, James Sutton, Robert Zahler, Rebecca A. Smirk, Scott A. Bolton, Steven Sheriff, Rushith Kumar Anumula, Zulan Pi, Jacobson Bruce L, Gregory S. Bisacchi, William A. Schumacher, Shung C. Wu, Treuner Uwe D, Sharon N. Bisaha, Anzhi Wei
Publikováno v: Bioorganicmedicinal chemistry letters. 23(18)
In this Letter, we describe the synthesis of several nonamidine analogs of biaryl acid factor VIIa inhibitor 1 containing weakly basic or nonbasic P1 groups. 2-Aminoisoquinoline was found to be an excellent surrogate for the benzamidine group (compou
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e308b8b54fe48668dfee00c12c8e60c5
https://pubmed.ncbi.nlm.nih.gov/23927973
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