Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Robichaud Albert Jean"'
Autor:
Maria-Jesus Blanco, Quinn Coughlin, Dario Doller, Hopper Allen T, Robichaud Albert Jean, Vijaya Tirunagaru
Publikováno v:
Journal of medicinal chemistry. 62(13)
Medicinal chemists are accountable for embedding the appropriate drug target profile into the molecular architecture of a clinical candidate. An accurate characterization of the functional effects following binding of a drug to its biological target
Autor:
Erik Wagner, Jonathan A. Bard, Kristine Svenson, Guixan Jin, Rajiv Chopra, Mei-Chu Lo, Minakshi Jani, Eric S. Manas, Pawel Nowak, Derek C. Cole, John W. Ellingboe, Baihua Hu, Robichaud Albert Jean, Kristi Fan, Michael S. Malamas, Rani Narasimhan, Jim Turner, Ann Aulabaugh, Ping Zhou, Rebecca Cowling, Steve Jacobsen, Peter H. Reinhart, Joseph Raymond Stock, Joan Subrath
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:632-635
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine (1) was identified through HTS, as a weak (micromolar) inhibitor of BACE1. X-Ray crystallographic studies indicate the 2-aminoimidazole ring forms key H-bonding interactions with Asp32 an
Publikováno v:
ARKIVOC, Vol 2010, Iss 6, Pp 84-88 (2009)
An efficient method has been developed for the synthesis of 2-amino-4-(4-fluoro-3-(2- fluoropyridin-3-yl)phenyl)-4-(4-methoxy-3-methylphenyl)-1-methyl-1H-imidazol-5(4H)-one, a potent BACE1 inhibitor for the potential treatment of Alzheimer's Disease.
Autor:
Zhen Wang, Ronald B. Franklin, Paul E. Finke, Thomas A. Baillie, John R. Strauss, Su Er W Huskey, Shuet Hing L Chiu, William P. Feeney, Brian Dean, Bonnie Wang, Cornelis E. C. A. Hop, George A. Doss, Reza Anari, Minghua Zhang, Robichaud Albert Jean, P Cunningham
Publikováno v:
Drug Metabolism and Disposition. 32:246-258
The absorption, metabolism, and excretion of [14C]aprepitant, a potent and selective human substance P receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting, was evaluated in rats and dogs. Aprepitant was metabolized exten
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1591-1594
A simple and versatile synthetic scheme employing d -malic acid as the principal building block permits the ready preparation of acyclic mimics of the squalene synthase inhibitor zaragozic acid A (ZA-A). Several compounds which were synthesized accor
Publikováno v:
Tetrahedron Letters. 34:8403-8406
The asymmetric syntheses of the C-1 sidechains of zaragozic acid A and C are described. Aldol reaction defines the chirality at C-4′and C-5′in two independent routes. Multigram preparation as well as a route amenable to derivatization are highlig
Autor:
Zoe A. Hughes, Thomas A. Comery, Lo Jennifer Rebecca, Ronald C. Bernotas, Jean Y. Zhang, Kevin G. Liu, Dianne Kowal, Deborah L. Smith, Guo Ming Zhang, Lee E. Schechter, Christine Huselton, Meiyi Zhang, Yinfa Yan, Robichaud Albert Jean
Publikováno v:
Journal of medicinal chemistry. 53(21)
As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperaziny
Publikováno v:
ChemInform. 22
The first total syntheses of the structurally unusual pentacyclic Melodinus alkaloids (±)-meloscine (1) and (±)-epimeloscine (2) and the hexacyclic Aspidosperma alkaloid (±)-deoxoapodine (4) are reported. The syntheses proceed via a highly functio
Publikováno v:
ChemInform. 26
The recently discovered fungal metabolites known both as the squalestatins' and zaragozic acids2 have become attractive targets for synthesis3 as a consequence of their picomolar inhibition of the enzyme squalene synthase (EC 2.5.1.21), the first com
Publikováno v:
Journal of the American Chemical Society. 113:2598-2610
The first total syntheses of the structurally unusual pentacyclic Melodinus alkaloids (±)-meloscine (1) and (±)-epimeloscine (2) and the hexacyclic Aspidosperma alkaloid (±)-deoxoapodine (4) are reported. The syntheses proceed via a highly functio