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Dive into the research topics where Axel Stoit is active.

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Featured researches published by Axel Stoit.


Bioorganic & Medicinal Chemistry Letters | 2017

Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P 5 receptor agonist chemotype

Axel 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

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 selective against both S1P1 and S1P3 receptor subtypes. The key compound 32 shows a high bioavailability of 73% and a CNS/plasma ratio of 0.8 after oral administration in rats.


Chemical & Pharmaceutical Bulletin | 2002

Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists

Axel Stoit; Jos H.M. Lange; Arnold P. den Hartog; Eric Ronken; Koos Tipker; Herman H. van Stuivenberg; Jessica A. R. Dijksman; Henri C. Wals; Chris G. Kruse


Tetrahedron Letters | 2010

A simple, base-free preparation of S-aryl thioacetates as surrogates for aryl thiols

Adri van den Hoogenband; Jos H.M. Lange; Raymond P.J. Bronger; Axel Stoit; Jan Willem Terpstra


Archive | 2005

Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition

Roelof W. Feenstra; Axel Stoit; Jan-Willem Terpstra; Maria L. Pras-Raves; Andrew C. McCreary; Bernard J. Van Vliet; Mayke B. Hesselink; Cornelis G. Kruse; Gustaaf J. M. Van Scharrenburg


Bioorganic & Medicinal Chemistry Letters | 2008

7-Azaindole derivatives as potential partial nicotinic agonists.

Axel Stoit; Arnold P. den Hartog; Harry Mons; Sjoerd van Schaik; Nynke Barkhuijsen; Cees Stroomer; Hein K. A. C. Coolen; Jan Hendrik Reinders; Tiny J.P. Adolfs; Martina A.W. van der Neut; Hiskias G. Keizer; Chris G. Kruse


Tetrahedron | 2013

Synthesis and differential functionalisation of pyrrolidine and piperidine based spirodiamine scaffolds

Kamil Weinberg; Axel Stoit; Chris G. Kruse; Mairi F. Haddow; Timothy Gallagher


Archive | 2009

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

Loevezijn Arnold Van; Bakker Wouter I. Iwema; Axel Stoit; Agatha A.M. Rensink; Jennifer Venhorst; Der Neut Martina A.W. Van; Haan Martin De; Cornelis G. Kruse


Archive | 2010

thio)morpholine derivatives as s1p modulators

Wouter I. Iwema Bakker; Hein K. A. C. Coolen; Axel Stoit; Harmen Mons; Eric Ronken; Elizabeth van der Kam; Jurjen Frankena; Adrian D. Hobson


Archive | 2008

N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS

Lechoslaw Turski; Axel Stoit; Cornelis G. Kruse; Sander Vader; Martinus T. M. Tulp


Archive | 2007

AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION

Axel Stoit; Hein K. A. C. Coolen; Martina A.W. van der Neut; Cornelis G. Kruse

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