Literature DB >> 15139761

1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.

Florencio Zaragoza1, Henrik Stephensen, Sanne M Knudsen, Lone Pridal, Birgitte S Wulff, Karin Rimvall.   

Abstract

With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H(3) receptor. The most potent amides had antagonist potencies in the subnanomolar range.

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Year:  2004        PMID: 15139761     DOI: 10.1021/jm031028z

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.

Authors:  Michael A Letavic; Leah Aluisio; Richard Apodaca; Manoj Bajpai; Ann J Barbier; Anne Bonneville; Pascal Bonaventure; Nicholas I Carruthers; Christine Dugovic; Ian C Fraser; Michelle L Kramer; Brian Lord; Timothy W Lovenberg; Lilian Y Li; Kiev S Ly; Heather Mcallister; Neelakandha S Mani; Kirsten L Morton; Anthony Ndifor; S Diane Nepomuceno; Chennagiri R Pandit; Steven B Sands; Chandra R Shah; Jonathan E Shelton; Sandra S Snook; Devin M Swanson; Wei Xiao
Journal:  ACS Med Chem Lett       Date:  2015-03-13       Impact factor: 4.345

2.  Histamine H3-receptor agonists and imidazole-based H3-receptor antagonists can be thermodynamically discriminated.

Authors:  E A Harper; J W Black
Journal:  Br J Pharmacol       Date:  2007-04-02       Impact factor: 8.739

  2 in total

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