Literature DB >> 16300945

Aplysamine-1 and related analogs as histamine H3 receptor antagonists.

Devin M Swanson1, Sandy J Wilson, Jamin D Boggs, Wei Xiao, Richard Apodaca, Ann J Barbier, Timothy W Lovenberg, Nicholas I Carruthers.   

Abstract

Aplysamine-1 (1), a marine natural product, was synthesized and screened for in vitro activity at the human and rat histamine H3 receptors. Aplysamine-1 (1) was found to possess a high binding affinity for the human H3 receptor (Ki = 30+/-4 nM). Synthetic analogs of 1, including des-bromoaplysamine-1 (10) and dimethyl-{2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-ethyl}-amine (13), were potent H3 antagonists.

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Year:  2005        PMID: 16300945     DOI: 10.1016/j.bmcl.2005.11.003

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


  6 in total

1.  Total Synthesis (+)-7-Bromotrypargine and Unnatural Analogs: Biological Evaluation Uncovers Activity at CNS Targets of Therapeutic Relevance.

Authors:  John T Brogan; Sydney L Stoops; Brenda C Crews; Lawrence J Marnett; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-11-16       Impact factor: 4.418

2.  Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets.

Authors:  John T Brogan; Sydney L Stoops; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2012-06-27       Impact factor: 4.418

3.  A short and efficient total synthesis of the bromotyrosine-derived alkaloid psammaplysene A.

Authors:  Jingjing Xu; Kai Wang; Jinlong Wu
Journal:  RSC Adv       Date:  2018-04-12       Impact factor: 4.036

Review 4.  Recent progress in neuroactive marine natural products.

Authors:  Ryuichi Sakai; Geoffrey T Swanson
Journal:  Nat Prod Rep       Date:  2014-01-17       Impact factor: 13.423

5.  Bioactive marine drugs and marine biomaterials for brain diseases.

Authors:  Clara Grosso; Patrícia Valentão; Federico Ferreres; Paula B Andrade
Journal:  Mar Drugs       Date:  2014-05-02       Impact factor: 5.118

6.  4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation.

Authors:  Beata Olszewska; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Int J Mol Sci       Date:  2018-04-19       Impact factor: 5.923

  6 in total

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