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The major biogenic amine metabolites in mood disorders. [PDF]
Yang J, Yuan M, Zhang W.
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Novel imidazole-based histamine H3 antagonists
Bioorganic & Medicinal Chemistry Letters, 2009A novel series of imidazole containing histamine H(3) receptor ligands were investigated and found to be potent functional antagonists. After improving the stability of these molecules towards liver microsomes, these compounds were found to have no appreciable affinity for CYP P450s.
Jill A, Jablonowski +11 more
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Indole- and benzothiophene-based histamine H3 antagonists
Bioorganic & Medicinal Chemistry Letters, 2010Previous research on histamine H(3) antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the central phenyl core with heteroaromatic fragments resulted in the preparation of novel 3,5-, 3,6- and 3,7-substituted indole and 3,5 ...
Alejandro, Santillan +12 more
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Fluorinated non-imidazole histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2009Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (
K, Isensee +8 more
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Non-imidazole histamine NO-donor H3-antagonists
Il Farmaco, 2005Recently a series of H3-antagonists related to Imoproxifan was realised (I); in these products the oxime substructure of the lead was constrained in NO-donor furoxan systems and in the corresponding furazan derivatives. In this paper, a new series of compounds derived from I by substituting the imidazole ring with the ethoxycarbonylpiperazino moiety ...
TOSCO, Paolo +5 more
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Non-imidazole heterocyclic histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2003Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.
Wenying, Chai +10 more
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2-Aryloxymethylmorpholine histamine H3 antagonists
Bioorganic & Medicinal Chemistry Letters, 2008The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H(3) antagonists is described. The new compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain.
Michael A, Letavic +10 more
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