Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Tibur Schmidlin"'
Autor:
Dale Dhanoa, Pascal Rigollier, Tibur Schmidlin, Imadul Islam, Mary W. Walker, Walter Schilling, Heinrich Rueeger, Michele Chiesi, Steven Whitebread, Jack Zhang, Yasuchika Yamaguchi, Charles Gluchowski, Leoluca Criscione
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1175-1179
The design of a novel series of NPY-Y5 receptor antagonists is described. Key elements for the design were the identification of weak Y5 hits from a Y1 program, results from a combinatorial approach and database mining. This led to the discovery of t
Autor:
Marc Gerspacher, Steven Whitebread, Peter Buehlmayer, Tibur Schmidlin, Yasuchika Yamaguchi, Heinrich Rueeger, Leoluca Cricione, Hanspeter Nick, Pascal Rigollier, Barbara Nuesslein-Hildesheim
Publikováno v:
ChemInform. 35
Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)-piperidin-4-ylmethyl-am
Autor:
J. A. Salon, C. Hou, W. Cui, T A Branchek, Imadul Islam, Yasuchika Yamaguchi, H. Rueger, P. Du, N. Boyle, J. A. Tamm, Y. Shifman, P. J.-J. Vaysse, Daljit S. Dhanoa, Charles Gluchowski, R L Weinshank, Tibur Schmidlin, Mary W. Walker, B. Dowling, N Adham
Publikováno v:
Protein engineering. 10(2)
has been discovered (Figure 1b; Rudolf et al., 1994).Neuropeptide Y (NPY) receptors belong to the G-protein- To study the ligand–receptor interactions between the Y1coupled receptor (GPCR) superfamily and mediate several receptor and BIBP3226 Y1 as
Autor:
Tibur Schmidlin, Christoph Tamm
Publikováno v:
Helvetica Chimica Acta. 63:121-131
Several attempts to prepare 3-acetyl-5-benzyl-3-pyrrolin-2-one (7) from phenylalanine are described. This goal was only reached formally, because compound 7 exists in the tautomeric form of (Z)-5-benzyl-3-(1′-hydroxyethylidene)-4-pyrrolin-2-one (17
Publikováno v:
Helvetica Chimica Acta. 64:235-250
The total synthesis of the tetrahydroisoindolinone moiety corresponding to proxiphomin (1) is described, bearing functional groups for the attachment of the macrocyclic ring. Knoevenagel-Cope condensation of racemic 2-(benzyloxycarbonyl-amino)-3-phen
Autor:
Christoph Tamm, Tibur Schmidlin
Publikováno v:
Helvetica Chimica Acta. 61:2096-2099
The octahydroisoindolone moiety related to proxiphomin (1) has been synthesized by condensation of N-benzyloxycarbonyl-protected D, L-phenylalaninal (7) with methyl-(4-methyl-sorbyl)-malonate (11) to yield the branched ethylene derivative 12. Consecu
Publikováno v:
Helvetica Chimica Acta. 67:1989-1997
The synthesis of ethyl (2E, 4E, 8R)-8-methyl-10-[(2H-tetrahydropyran-2-yl)oxy]-2,4-decadienoate (11), methyl (2E, 8R)-8-methyl-10-[(2H-tetrahydropyran-2-yl)oxy]-2-decenoate (16), synthons for the construction of the macrocyclic moieties of the cytoch
Publikováno v:
Helvetica Chimica Acta. 67:1998-2008
The bicycle aldehyde 7 was prepared from the hydroxy ester 3 for the attachment of teh macrocyclic moiety of the cytochalasans. To protect the C(6),C(7)-double bond the intermediates 8, 9 and 13 were transformed into the epoxides 10, 11 and 14, respe
Publikováno v:
Helvetica Chimica Acta. 66:450-465
A general scheme for the synthesis of the tetrahydroisoindolinone moiety of naturally occurring cytochalasans and unnatural analogs was developed. The key-step consists of the intermolecular [2+4]cycloaddition of 4-methylsorbinol (7) to an alkylidene
Publikováno v:
Helvetica Chimica Acta. 66:1796-1805
The stereo- and regiochemical course in the [2+4]cycloaddition of the chiral alkylidene malonic ester 1 to selected derivatives of (2E, 4E)-4-methyl-2, 4-hexadien-l-ol (2) and (2E, 4E)-4-methyl-2, 4-hexadien-l-al (12) has been investigated. The resul