Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Arnold P. den Hartog"'
Autor:
Axel Stoit, Sjoerd van Schaik, Josephus H. M. Lange, Annemieke Rensink, Adri van den Hoogenband, Chris G. Kruse, Hein K. A. C. Coolen, Arnold P. den Hartog
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:459-465
The synthesis and SAR of a novel class of spirobenzofuranpiperidinyl-derived alkanoic acids 6-34 as sphingosine S1P5 receptor agonists are described. The target compounds generally elicit high S1P5 receptor agonistic potencies and in general are sele
Autor:
Josephus H. M. Lange, Remco Henzen, Natasja de Bruin, Jelle de Vries, Wouter I. Iwema Bakker, Wouter de Looff, Arnold P. den Hartog, Stefan Verhoog, Rob P. van de Woestijne, Chris G. Kruse, Arnold van Loevezijn, Jennifer Venhorst, Martina A.W. van der Neut
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1605-1611
The discovery of non-basic N'-(arylsulfonyl)pyrazoline-1-carboxamidines as 5-HT6 antagonists with unique structural features was recently disclosed. Here we describe how this structural class was further developed by addressing an unexplored interact
Autor:
Axel R, Stoit, Jos H M, Lange, Hein K A C, Coolen, Annemieke, Rensink, Adri, van den Hoogenband, Arnold P, den Hartog, Sjoerd, van Schaik, Chris G, Kruse
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(3)
The synthesis and SAR of a novel class of spirobenzofuranpiperidinyl-derived alkanoic acids 6-34 as sphingosine S1P
Autor:
Henri C. Wals, Arnold P. den Hartog, Herman H. van Stuivenberg, Vliet Bernard J Van, Martina A.W. van der Neut, Chris G. Kruse, Josephus H. M. Lange, Jan Hoogendoorn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1752-1757
The synthesis, structure–activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6–18 represent a novel class of potent and selective CB1 rec
Autor:
Arnold P. den Hartog, Dijksman Jessica A R, Koos Tipker, Hiskias G. Keizer, Hein K. A. C. Coolen, Henri C. Wals, Tiny J.P. Adolfs, Bob Stork, Peter C Verveer, Andrew C. McCreary, Josephus H. M. Lange, Natasja M J de Jong, Herman H. van Stuivenberg, Jan Hoogendoorn, Chris G. Kruse, Arnoud H.J. Herremans, Eric Ronken, Willem Veerman
Publikováno v:
Journal of Medicinal Chemistry. 47:627-643
A series of novel 3,4-diarylpyrazolines was synthesized and evaluated in cannabinoid (hCB(1) and hCB(2)) receptor assays. The 3,4-diarylpyrazolines elicited potent in vitro CB(1) antagonistic activities and in general exhibited high CB(1) vs CB(2) re
Autor:
Axel Stoit, Jos Hubertus Maria Lange, Dijksman Jessica A R, Koos Tipker, Herman H. van Stuivenberg, Chris G. Kruse, Henri C. Wals, Arnold P. den Hartog, Eric Ronken
Publikováno v:
Chemical and Pharmaceutical Bulletin. 50:1109-1113
The design, synthesis and biological activities of potent pyrazole-based tricyclic CB1 receptor antagonists (2) are described. The key synthetic step involves the ring closure of the lithiated alpha, gamma-keto ester adduct (4). The optimal nitroderi
Autor:
Vliet Bernard J Van, Josephus H. M. Lange, Arnold P. den Hartog, Henri C. Wals, Martina A.W. van der Neut, Jan Hoogendoorn, Herman H. van Stuivenberg, Chris G. Kruse
Publikováno v:
ChemInform. 41
The synthesis, structure–activity relationship (SAR) studies and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles are described. The target compounds 6–18 represent a novel class of potent and selective CB1 rec
Autor:
Henri C. Wals, Vliet Bernard J Van, Josephus H. M. Lange, Alice J.M. Borst, Hicham Zilaout, Gijs D. Kuil, Martina A.W. van der Neut, Herman H. van Stuivenberg, Arnold P. den Hartog, Arie T. Mulder, Wouter Goutier
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(3)
The synthesis and structure–activity relationship studies of imidazoles are described. The target compounds 6 – 20 represent a novel chemotype of potent and CB 2 /CB 1 selective cannabinoid CB 2 receptor antagonists/inverse agonists with very hig
Autor:
Arnold P. den Hartog, Tiny J.P. Adolfs, Sjoerd van Schaik, Jan H. Reinders, Hiskias G. Keizer, Nynke Barkhuijsen, Cees N. J. Stroomer, Hein K. A. C. Coolen, Chris G. Kruse, Axel Stoit, Martina A.W. van der Neut, Harry Mons
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(1)
We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor
Autor:
Hiskias G. Keizer, Chris G. Kruse, and Arnoud H. J. Herremans, Janpeter de Moes, Herman H. van Stuivenberg, Hein K. A. C. Coolen, Arnold P. den Hartog, Martin Tulp, Rolf van Hes, Leonarda C. Niemann, Andrew C. McCreary, Rob H. Plekkenpol, Mayke B. Hesselink, Cees N. J. Stroomer, Bob Stork, Pieter Smid
Publikováno v:
Journal of medicinal chemistry. 48(22)
A series of novel bicyclic 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines was synthesized and evaluated on binding to dopamine D(2) receptors and serotonin reuptake sites. This class of compounds proved to be potent in vitro dopamine D(2) rec