Výsledky vyhledávání - "Martina A.W. van der Neut"

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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N′-(Arylsulfonyl)pyrazoline-1-carboxamidines as Novel, Neutral 5-Hydroxytryptamine 6 Receptor (5-HT6R) Antagonists with Unique Structural Features

Autor: Cor G de Korte, Stefan Verhoog, Martina A.W. van der Neut, Wouter I. Iwema Bakker, Alice J.M. Borst, Jennifer Venhorst, Chris G. Kruse, Natasja de Bruin, Rob P. van de Woestijne, Hiskias G. Keizer, Arnold van Loevezijn, Wouter de Looff, Jan-Willem van Wees, Maria J.P. van Dongen, Martijn van Hoeve

Publikováno v: Journal of Medicinal Chemistry. 54:7030-7054

The 5-HT(6) receptor (5-HT(6)R) has been in the spotlight for several years regarding CNS-related diseases. We set out to discover novel, neutral 5-HT(6)R antagonists to improve off-target selectivity compared to basic amine-containing scaffolds domi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::01b80e49fd141f75bc4e9afb4ff68b46
https://doi.org/10.1021/jm200466r

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Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity

Autor: Taco R. Werkman, Wytse J. Wadman, A.R. Blaazer, Femke S. den Boon, Chris G. Kruse, Josephus H. M. Lange, Martina A.W. van der Neut, Arie H. Mulder

Publikováno v: Journal of Medicinal Chemistry, 46, 5086-5098. American Chemical Society

The discovery, synthesis and structure-activity relationship (SAR) of a novel series of cannabinoid 1 (CB(1)) and cannabinoid 2 (CB(2)) receptor ligands are reported. Based on the aminoalkylindole class of cannabinoid receptor agonists, a biphenyl mo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9add9a1145563982df9aced0b673e8c
https://hdl.handle.net/11245/1.352856

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Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern

Autor: Vliet Bernard J Van, Josephus H. M. Lange, Herman H. van Stuivenberg, Chris G. Kruse, Alice J.M. Borst, Mahmut Selman Yildirim, Martina A.W. van der Neut

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:2770-2775

The cannabinoid CB(1)/CB(2) receptor subtype selectivity in the 1,2-diarylimidazole-4-carboxamide series was boosted by fine-tuning its 5-substitution pattern. The presence of the 5-methylsulfonyl group in 11 led to a greater than approximately 840-f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1132e90c911a5e665c358a7347df54f7
https://doi.org/10.1016/j.bmcl.2010.03.068

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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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Design, Synthesis, Biological Properties, and Molecular Modeling Investigations of Novel Tacrine Derivatives with a Combination of Acetylcholinesterase Inhibition and Cannabinoid CB1 Receptor Antagonism

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

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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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Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists

Autor: Hicham Zilaout, Hans van Aken, Henri C. Wals, Amos Attali, Arie H. Mulder, Martina A.W. van der Neut, Vliet Bernard J Van, Josephus H. M. Lange, Ate Duursma

Publikováno v: Bioorganicmedicinal chemistry letters. 20(17)

The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1-23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24-27 as two novel cannabinoid CB(1) receptor agonist classes were described. The target compounds elicited high aff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a6d7054709649e3b5815449cde19c3f
https://pubmed.ncbi.nlm.nih.gov/20688519

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Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia

Autor: Jean Zhang, Ping Zhou, Tikva Carrick, Albert J. Robichaud, Rolf Feenstra, Jan-Hendrik Reinders, Dianne Kowal, Chris G. Kruse, Martina A.W. van der Neut, Yinfa Yan, David P. Rotella, Mark H. Pausch, Margaret Lai, Karen L. Marquis

Publikováno v: Bioorganicmedicinal chemistry letters. 20(9)

A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5166982a958128acf3a0153c1b0e0b45
https://pubmed.ncbi.nlm.nih.gov/20347298

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