Výsledky vyhledávání - "Mark P. Edelstein"

Rational Design of Potent Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase

Autor: Andrew J. Peat, Kurt Weaver, Liping Wang, Sebahar Paul Richard, Eugene L. Stewart, Amanda Mathis, Robert T. Nolte, Dulce Garrido, Robert G. Ferris, Mark P. Edelstein, Huichang Zhang, Pek Yoke Chong, Michael Youngman

Publikováno v: Journal of Medicinal Chemistry. 55:10601-10609

A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ddc8f9e72f78103aa7993201d354598
https://doi.org/10.1021/jm301294g

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Discovery of a novel series of cyclic urea as potent CCR5 antagonists

Autor: Pat Wheelan, Dan Todd, Rob Ferris, Matt Tallant, Zhiping Xiong, Jung Ho Jun, Wieslaw M. Kazmierski, Maosheng Duan, Mark P. Edelstein

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:6381-6385

A novel series of cyclic urea-based CCR5 antagonists was designed aiming to resolve instability issue in the fasted simulated intestinal fluid (FSIF) associated with the acyclic urea moiety in 1. This class of CCR5 compounds demonstrated high antivir

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04fa2166cbea9163ef4d6cea60e23b80
https://doi.org/10.1016/j.bmcl.2011.08.096

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Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1

Autor: Matthew David Tallant, Wieslaw M. Kazmierski, Pat Wheelan, Maosheng Duan, George Andrew Freeman, Mark P. Edelstein, Robert G. Ferris

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:1394-1398

We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat P

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68dbee409884703c0fdfed425864b7bb
https://doi.org/10.1016/j.bmcl.2011.01.030

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ChemInform Abstract: Discovery of a Novel Series of Cyclic Urea as Potent CCR5 Antagonists

Autor: Mark P. Edelstein, Pat Wheelan, Rob Ferris, Matt Tallant, Jung Ho Jun, Maosheng Duan, Wieslaw M. Kazmierski, Zhiping Xiong, Dan Todd

Publikováno v: ChemInform. 43

Design and practical syntheses of a novel class of cyclic urea-based CCR5-antagonists demonstrating high antiviral activities against HIV-1 infection in both HOS and PBL assays are described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1f9a0fb57b02781762ddefca6a5c8e28
https://doi.org/10.1002/chin.201209148

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Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats

Autor: Maosheng Duan, Pat Wheelan, Rena Nishizawa, Pek Yoke Chong, Mark P. Edelstein, Huichang Zhang, Felix Deanda, Rob Ferris, Jennifer Poole Peckham, Zhiping Xiong, Wieslaw M. Kazmierski, Yoshikazu Takaoka

Publikováno v: Bioorganicmedicinal chemistry letters. 21(21)

A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba862eb48e820d281c35bccce49ee148
https://pubmed.ncbi.nlm.nih.gov/21920742

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New inhibitors of sepiapterin reductase. Lack of an effect of intracellular tetrahydrobiopterin depletion upon in vitro proliferation of two human cell lines

Autor: Gary K. Smith, David S. Duch, Eric C. Bigham, Mark P. Edelstein

Publikováno v: Journal of Biological Chemistry. 267:5599-5607

N-Acetylserotonin (compound 1) and N-acetyldopamine (compound 7) inhibit bovine adrenal medullary sepiapterin reductase in a manner competitive with the pterin substrate and have Ki values of 0.12 and 0.4 microM, respectively. Molecular modeling sugg

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::078b7e033bc13c753109822be4792cd3
https://doi.org/10.1016/s0021-9258(18)42807-4

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Blockade of X4-Tropic HIV-1 Cellular Entry by GSK812397, a Potent Noncompetitive CXCR4 Receptor Antagonist▿

Autor: Stephen Jenkinson, Susan Danehower, Kristjan S. Gudmundsson, Michael Thomson, Mark P. Edelstein, Pat Wheelan, Andrew Spaltenstein, Wendell Lawrence, David C McCoy

GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays (e.g., in peripheral blood mononuclear cells [PBMCs] and a viral human osteosarcoma [HOS] assay, mean 50% inhibitory concentrati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::844ee8a56eb1f882e5fa33e712a97153
https://europepmc.org/articles/PMC2812144/

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