Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Thomas E. Christos"'
Publikováno v:
The Journal of Organic Chemistry. 66:5911-5914
Publikováno v:
The Journal of Organic Chemistry. 64:9673-9678
A general method for the cyclization of an unactivated 1,1-disubstituted alkene such as 1 to the corresponding cyclopentene 5 is described. Bromination followed by the addition of strong base in the same pot gave the vinyl bromide 3, which reacted fu
Autor:
Argyrios G. Arvanitis, Paul J. Gilligan, Robert J. Chorvat, Robert S. Cheeseman, Thomas E. Christos, Rajagopal Bakthavatchalam, James P. Beck, Anthony J. Cocuzza, Frank W. Hobbs, Richard G. Wilde, Charles Arnold, Dennis Chidester, Matthew Curry, Liqi He, Andrea Hollis, John Klaczkiewicz, Paul J. Krenitsky, Joseph P. Rescinito, Everett Scholfield, Steven Culp, Errol B. De Souza, Lawrence Fitzgerald, Dimitri Grigoriadis, S. William Tam, Y. Nancy Wong, Shiew-Mei Huang, Helen L. Shen
Publikováno v:
Journal of Medicinal Chemistry. 42:805-818
Screening of our chemical library using a rat corticotropin-releasing hormone (CRH) receptor assay led to the discovery that 2-anilinopyrimidine 15-1 weakly displaced [125I]-0-Tyr-oCRH from rat frontal cortex homogenates when compared to the known pe
Autor:
Paul Krenitsky, Strucely P, Robert Scott Cheeseman, Hodge Carl Nicholas, Thomas E. Christos, Zelda R. Wasserman, Paul J. Gilligan, Ciganek E, Nemeth Ga, Fernandez Ch, Everett Latham Scholfield, Argyrios G. Arvanitis, Aldrich Pe, Robert J. Chorvat
Publikováno v:
Journal of Medicinal Chemistry. 42:819-832
As described in the preceding paper (Arvanitis et al. J. Med. Chem. 1999, 42), anilinopyrimidines I were identified as potent antagonists of corticotropin-releasing hormone-1 receptor (CRH1-R, also referred to as corticotropin-releasing factor, CRF1-
Publikováno v:
Expert Opinion on Therapeutic Patents. 8:143-152
Corticotrophin-releasing factor (CRF) receptor antagonists have attracted considerable attention recently as potential therapeutics for a variety of neuropsychiatric disorders including anxiety, depression and anorexia nervosa. Preliminary results su
Autor:
Douglass F. Taber, Thomas E. Christos
Publikováno v:
Tetrahedron Letters. 38:4927-4930
The alkylidene carbene generated by chloromethylenation / α-elimination of 1 proceeds with a high degree of selectivity for methoxy CH insertion over methine insertion, to give 2. The carbene generated with trimethylsilydiazomethane results in an
Publikováno v:
Tetrahedron letters. 51(6)
The preparation of (Z)-1-fluoro-2-bromostyrenes provides a general route for the formation of (Z)-1-fluorostilbene derivatives as configurationally stable spacial linkers for the design of conformationally restricted peptidomimetics. Palladium-cataly
Publikováno v:
The Journal of Organic Chemistry. 61:2081-2084
A new procedure for cyclohexenone annelation has been developed. Thus, alkylation of 4-isopropylcyclohexanone with allyl bromide gives, over several steps, ketone 8. Exposure to (trimethylsilyl)diazomethane and MeLi smoothly cyclized 8 to the cyclope
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2347-2352
A series of novel cinnamyl and propargyl ether derivatives of alkyl piperidines which show high affinity for sigma and 5HT 2 receptors are described. The ligands exhibit high selectivities for these receptors over D 2 as well as good activity in vivo
Autor:
D. E. Grigoriadis, Paul J. Gilligan, Alexander L. Johnson, Gary A. Cain, S. William Tam, Charles J. Eyermann, Thomas E. Christos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:329-334
A series of novel conjugated aromatic 4-amino- and 4-amido-piperidines which are potent sigma receptor ligands are described. These ligands exhibited good to excellent selectivities for binding at sigma versus D2 and 5-HT2 receptors.