Acylated and alkylated histamine derivatives as new histamine H3-receptor antagonists
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Cited by (24)
Non-imidazole histamine H <inf>3</inf> ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H <inf>3</inf>-antagonists
2005, European Journal of Medicinal ChemistryCitation Excerpt :However, histamine H3-receptors antagonists have not been introduced into therapy yet, but potential therapeutic applications have been proposed, e.g. memory and learning deficits [10–12], epilepsy [13,14], Alzheimer’s disease [15,16], and attention-deficit hyperactivity disorder [17]. Since the discovery of thioperamide (Ki = 4.3 nM) [18] (Chart 1), the prototype of H3-antagonist, many potent ligands carrying an imidazole moiety have been described [19–24] among others, potent and selective antagonists with high in vitro and in vivo activity FUB 470 [25] and ciproxifan [26] (Chart 1). The most representative compound of this group is GT 2331 (Ki = 0.12 nM) [27] (Chart 1); the first histamine H3-antagonist to be taken into human clinical trials.
6 The Histamine H<inf>3</inf> Receptor and its Ligands
2001, Progress in Medicinal ChemistryQSAR Studies on acylated histamine derivatives
2001, Bioorganic and Medicinal ChemistryCitation Excerpt :They observed that these compounds possess moderate to pronounced H3-receptors antagonists activity. In addition, Stark et al.11 also observed that there is no difference in activity between the acetyl derivatives (compound 1, Table 1) and the phenylacetyl derivative (compound 2, Table 1). Also, that exchange of 1-methylene group by oxygen or sulfur has no advantage on H3-receptors activity (4–7).
4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: The design of potent histamine H<inf>3</inf> receptor antagonists
1999, Bioorganic and Medicinal Chemistry LettersDiphenylmethyl ethers: Synthesis and histamine H<inf>3</inf>-receptor antagonist in vitro and in vivo activity
1996, Bioorganic and Medicinal Chemistry LettersNew potent histamine H<inf>3</inf>-receptor antagonists of the amide type
1995, European Journal of Pharmaceutical Sciences