Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Etzer Darout"'
Publikováno v:
Phosphodiesterases and Their Inhibitors
Publikováno v:
Synthesis. 45:2481-2484
A detailed investigation of the preparation of 1-methylcyclopropanol via the Kulinkovich reaction is presented. Reaction and workup parameters were optimized to provide a reproducible procedure for the synthesis of multigram quantities of 1-methylcyc
Autor:
Brian P. Rempel, Dona C. Love, Spencer Knapp, Paul R. Rablen, Stephen G. Withers, Mohannad Abdo, John A. Hanover, Etzer Darout, Eun Ju Kim
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:7058-7064
The title compound, which differs from the powerful O-GlcNAcase (OGA) inhibitor GlcNAc-thiazoline only at the chalcogen atom (Se for S), is a much weaker inhibitor in a direct OGA assay. In human cells, however, the selenazoline shows comparable abil
Autor:
Arindrajit Basak, Etzer Darout
Publikováno v:
Tetrahedron Letters. 51:2998-3001
An efficient approach to a oxa-azabicyclo[3.2.1] derivatives has been achieved via a double-Mannich reaction of N,N-bis(methoxymethyl)-1-phenylethanamine with symmetrical and unsymmetrical ketones.
Autor:
Spencer Knapp, Etzer Darout
Publikováno v:
Tetrahedron Letters. 43:6075-6078
Oxidation of GlcNAc thiazoline in the presence of an alcohol affords no glycosidation products, but rather the alkyl α-GlcNAc 1-C-sulfonate. E2 cleavage of the sulfonate ester and then O -deacetylation gives the α-GlcNAc 1-C-sulfonic acid, a new ty
Publikováno v:
Tetrahedron Letters. 52:1949-1951
The synthesis of two unprecedented regioisomeric oxospiropyrazole piperidine scaffolds is detailed. Their potential utility as templates for drug discovery is also exemplified. Chemical stability and solid state conformation were also evaluated.
Publikováno v:
ChemInform. 45
A carefully designed process for the scalable synthesis of 1-methylcyclopropanol (III) is developed as well as the optimized conversion to the mixed carbonate (V).
Publikováno v:
ChemInform. 43
Title compound (IV) is prepared as an unprecedented heterocyclic template for studies on the structure—activity relationship between the G-protein coupled receptor 119 (GPR119) and conformationally restricted ligands.
Autor:
William R. Roush, Peter Hodder, Joshua Roth, Gregg B. Fields, Dmitriy Minond, Janelle L. Lauer, Qin Liu, Etzer Darout
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(23)
Matrix metalloproteinase-13 (MMP-13) has been implicated as the protease responsible for collagen degradation in cartilage during osteoarthritis (OA). Compounds that inhibit the metalloproteinase at the Zn binding site typically lack specificity amon
Autor:
Michael P. DeNinno, Anthony R. Harris, Bruce Allen Lefker, Peter Cornelius, Etzer Darout, Daniel W. Kung, Lacey Samp, Paul D. Bonin, Sam Hornby, Kentaro Futatsugi, Bryan Li, E. D. Salter, Kim F. McClure, Jeffrey T. Kohrt, Ralph P. Robinson, Amit S. Kalgutkar, Ruduan Wang, Vincent Mascitti, Michael John Munchhof, Yue Chen, Cristiano Ruch Werneck Guimarães, Dianna E. Moore
Publikováno v:
Journal of medicinal chemistry. 54(6)
The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agoni