Výsledky vyhledávání - "Arnold P. den Hartog"

Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype

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

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Optimization of N ′-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT 6 antagonistic binding pocket

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9cf6abbf2099e90ec1e67445cecda377
https://doi.org/10.1016/j.bmcl.2016.02.001

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Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P

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

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Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB1 receptor antagonists

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2c90d51563f82391edda9612ecec016
https://doi.org/10.1016/j.bmcl.2010.01.049

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Synthesis, Biological Properties, and Molecular Modeling Investigations of Novel 3,4-Diarylpyrazolines as Potent and Selective CB1 Cannabinoid Receptor Antagonists

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

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Design, Synthesis and Biological Activity of Rigid Cannabinoid CB1 Receptor Antagonists

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::360b854c74fef10f0415fb89f07f0dee
https://doi.org/10.1248/cpb.50.1109

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ChemInform Abstract: Synthesis, SAR and Intramolecular Hydrogen Bonding Pattern of 1,3,5-Trisubstituted 4,5-Dihydropyrazoles as Potent Cannabinoid CB1 Receptor Antagonists

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8449671cf6ec8952e4dd6753e60a5351
https://doi.org/10.1002/chin.201030125

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Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d05bca00ba102b73cff12dc1d1f7d3f9
https://pubmed.ncbi.nlm.nih.gov/20031412

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Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition

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

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