Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Hein K. A. C. Coolen"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bd3ebf6ed30fa1e94992ef7801db2807
https://doi.org/10.1016/j.bmcl.2017.12.018
https://doi.org/10.1016/j.bmcl.2017.12.018
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::76f53879546cda122e1a9dd857a94fb0
https://pubmed.ncbi.nlm.nih.gov/29254642
https://pubmed.ncbi.nlm.nih.gov/29254642
Autor:
Peter C Verveer, Bob Stork, Hein K. A. C. Coolen, Alice J.M. Borst, Josephus H. M. Lange, Martina A.W. van der Neut, Chris G. Kruse
Publikováno v:
Journal of Medicinal Chemistry. 53:1338-1346
Pyrazolines 7-10 were designed as novel CB(1) receptor antagonists, which exhibited improved turbidimetric aqueous solubilities. On the basis of their extended CB(1) antagonist pharmacophore, hybrid molecules exhibiting cannabinoid CB(1) receptor ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a17a640414c9826697d448ffeea4e10
https://doi.org/10.1021/jm901614b
https://doi.org/10.1021/jm901614b
Autor:
Peter C Verveer, Herman H. van Stuivenberg, Josephus H. M. Lange, Wouter de Looff, Alice J.M. Borst, Willem Veerman, Hiskias G. Keizer, Hein K. A. C. Coolen, Andrew C. McCreary, Henri C. Wals, Chris G. Kruse, Tiny J.P. Adolfs
Publikováno v:
Journal of Medicinal Chemistry. 48:1823-1838
Series of thiazoles, triazoles, and imidazoles were designed as bioisosteres, based on the 1,5-diarylpyrazole motif that is present in the potent CB(1) receptor antagonist rimonabant (SR141716A, 1). A number of target compounds was synthesized and ev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efcd4c8ade0a6c0b52c26817f2895e9e
https://doi.org/10.1021/jm040843r
https://doi.org/10.1021/jm040843r
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6bf7d3905b901be5418d4523216fb0d
https://doi.org/10.1021/jm031019q
https://doi.org/10.1021/jm031019q
Publikováno v:
Angewandte Chemie. 104:906-909
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5db3d1827842cb24508d93dc51eb7603
https://doi.org/10.1002/ange.19921040731
https://doi.org/10.1002/ange.19921040731
Autor:
Jeroen T.B.M. Tolboom, Hein K. A. C. Coolen, Jan-Hendrik Reinders, Jeffrey C. Glennon, Josephus H. M. Lange, Chris G. Kruse
Publikováno v:
Journal of medicinal chemistry. 50(21)
The receptor binding affinities of the three drug candidates 1 (SLV310), 2 (SLV313), and 3 (SLV314) were positioned against the results from nine (a)typical antipsychotic drugs. The receptor binding data from sixteen monoaminergic receptors served as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::587062993efd177560c2a16c0dec1194
https://pubmed.ncbi.nlm.nih.gov/17880057
https://pubmed.ncbi.nlm.nih.gov/17880057
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91661210ad122c794780ca9e60253d69
https://pubmed.ncbi.nlm.nih.gov/18006307
https://pubmed.ncbi.nlm.nih.gov/18006307
Autor:
Henri C. Wals, Herman H. van Stuivenberg, Josephus H. M. Lange, Bob Stork, Andrew C. McCreary, Hein K. A. C. Coolen, Willem Veerman, Tiny J.P. Adolfs, Chris G. Kruse
Publikováno v:
ChemInform. 37
Novel 3,4-diarylpyrazolines 1 as potent CB1 receptor antagonists with lipophilicity lower than that of SLV319 are described. The key change is the replacement of the arylsulfonyl group in the original series by a dialkylaminosulfonyl moiety. The abso
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1008e9f207f18e4e8bd539570cad349d
https://doi.org/10.1002/chin.200605111
https://doi.org/10.1002/chin.200605111
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f6dfd58fc02e458bbdfc217b38e9ce3
https://pubmed.ncbi.nlm.nih.gov/16250644
https://pubmed.ncbi.nlm.nih.gov/16250644