Literature DB >> 12657274

Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.

Ramin Faghih1, Wesley Dwight, Jia Bao Pan, Gerard B Fox, Kathy M Krueger, Timothy A Esbenshade, Jill M McVey, Kennan Marsh, Youssef L Bennani, Arthur A Hancock.   

Abstract

Novel 4'-[(NR1R2-1-yl)]-propoxy-biaryl-4-carboxamides were designed and synthesized. All compounds were tested for affinity at histamine H(3)receptors. Most compounds were highly potent and selective for human and rat H(3) receptors and selected examples such as A-349821 showed functional antagonism of H(3) receptors in vitro and in a mouse dipsogenia model.

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Year:  2003        PMID： 12657274     DOI： 10.1016/s0960-894x(03)00118-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand.

Authors:  David G Witte; Betty Bei Yao; Thomas R Miller; Tracy L Carr; Steven Cassar; Rahul Sharma; Ramin Faghih; Bruce W Surber; Timothy A Esbenshade; Arthur A Hancock; Kathleen M Krueger
Journal:  Br J Pharmacol       Date:  2006-05-22       Impact factor: 8.739

Review 2.  Roles of histamine and its receptors in allergic and inflammatory bowel diseases.

Authors:  Hua Xie; Shao-Heng He
Journal:  World J Gastroenterol       Date:  2005-05-21       Impact factor: 5.742

3.  Direct one-pot synthesis of primary 4-amino-2,3-diaryl-quinolines via Suzuki-Miyaura cross-coupling of 2-aryl-4-azido-3-iodoquinolines with arylboronic acids.

Authors:  Malose Jack Mphahlele; Mamasegare Mabel Mphahlele
Journal:  Molecules       Date:  2011-10-25       Impact factor: 4.411
  3 in total

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