32705-71-8Relevant academic research and scientific papers
Covalent inhibition of the histamine H3 receptor
Wágner, Gábor,Mocking, Tamara A.M.,Kooistra, Albert J.,Slynko, Inna,ábrányi-Balogh, Péter,Keser u, Gy?rgy M.,Wijtmans, Maikel,Vischer, Henry F.,de Esch, Iwan J.P.,Leurs, Rob
, (2019/12/25)
Covalent binding of G protein-coupled receptors by small molecules is a useful approach for better understanding of the structure and function of these proteins. We designed, synthesized and characterized a series of 6 potential covalent ligands for the histamine H3 receptor (H3R). Starting from a 2-amino-pyrimidine scaffold, optimization of anchor moiety and warhead followed by fine-tuning of the required reactivity via scaffold hopping resulted in the isothiocyanate H3R ligand 44. It shows high reactivity toward glutathione combined with appropriate stability in water and reacts selectively with the cysteine sidechain in a model nonapeptide equipped with nucleophilic residues. The covalent interaction of 44 with H3R was validated with washout experiments and leads to inverse agonism on H3R. Irreversible binder 44 (VUF15662) may serve as a useful tool compound to stabilize the inactive H3R conformation and to study the consequences of prolonged inhibition of the H3R.
2-Aminopyrimidine modulators of the histamine H4 receptor
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Page/Page column 16, (2008/12/07)
2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 /su
Synthesis and bioactivity of aripiprazole derivatives
Ge, Hai-Xia,Wang, Li-Chen,Jiang, Zhen-Zhou,Ni, Sheng-Liang
, p. 673 - 677 (2007/10/03)
Ten aripirazole (CAS 129722-12-9) derivatives were prepared and examined for dopamine receptor antagonist activity. The structures of these newly synthesized compounds were confirmed by their elemental analyses and by IR, 1H-NMR and mass spectra. It was demonstrated that all the new compounds have dopamine receptor antagonist activity to a certain extent. Three compounds showed more potent activity than aripiprazole. ECV · Editio Cantor Verlag.
Piperazinylalkylpyrimidines as hypoglycemic agents
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, (2008/06/13)
Novel hypoglycemic agents having the formula (I) are disclosed. STR1
Succinimide derivatives, and their production and use
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, (2008/06/13)
A succinimide derivative of the formula: STR1 wherein R is a pyridyl or pyrimidinyl group substituted with at least one member selected from the group consisting of halogen, lower alkyl, lower alkoxy, cyano, benzyloxy, hydroxyl and amino, and n is an integer of 1 or 2, or a pharmaceutically acceptable acid addition salt thereof. The succinimide derivatives are useful as an anti-anxiety drugs.
