Literature DB >> 17498953

A new class of histamine H3 receptor antagonists derived from ligand based design.

Olivier Roche1, Rosa María Rodríguez Sarmiento.   

Abstract

Design and synthesis of highly potent and selective non-imidazole inverse agonists for the histamine H(3) receptor is described. The study validates a new pharmacophore model based on the merging of two previously described models. It also demonstrates that the removal of the basic center potentially interacting with ASP3.32 and common to both models leads to loss of activity, whereas the replacement of the second basic center by an acceptor retains the potency.

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Year:  2007        PMID: 17498953     DOI: 10.1016/j.bmcl.2007.04.056

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


  5 in total

Review 1.  Computational methods in drug discovery.

Authors:  Gregory Sliwoski; Sandeepkumar Kothiwale; Jens Meiler; Edward W Lowe
Journal:  Pharmacol Rev       Date:  2013-12-31       Impact factor: 25.468

2.  Synthesis, biological evaluation, and computational studies of Tri- and tetracyclic nitrogen-bridgehead compounds as potent dual-acting AChE inhibitors and hH3 receptor antagonists.

Authors:  Fouad H Darras; Steffen Pockes; Guozheng Huang; Sarah Wehle; Andrea Strasser; Hans-Joachim Wittmann; Martin Nimczick; Christoph A Sotriffer; Michael Decker
Journal:  ACS Chem Neurosci       Date:  2014-01-14       Impact factor: 4.418

3.  Automated design of ligands to polypharmacological profiles.

Authors:  Jérémy Besnard; Gian Filippo Ruda; Vincent Setola; Keren Abecassis; Ramona M Rodriguiz; Xi-Ping Huang; Suzanne Norval; Maria F Sassano; Antony I Shin; Lauren A Webster; Frederick R C Simeons; Laste Stojanovski; Annik Prat; Nabil G Seidah; Daniel B Constam; G Richard Bickerton; Kevin D Read; William C Wetsel; Ian H Gilbert; Bryan L Roth; Andrew L Hopkins
Journal:  Nature       Date:  2012-12-13       Impact factor: 49.962

4.  Accessing an azaborine building block: synthesis and substitution reactions of 2-chloromethyl-2,1-borazaronaphthalene.

Authors:  Gary A Molander; Steven R Wisniewski; Javad Amani
Journal:  Org Lett       Date:  2014-10-15       Impact factor: 6.005

5.  Synthesis and characterization of new bivalent agents as melatonin- and histamine H3-ligands.

Authors:  Daniele Pala; Laura Scalvini; Alessio Lodola; Marco Mor; Lisa Flammini; Elisabetta Barocelli; Valeria Lucini; Francesco Scaglione; Silvia Bartolucci; Annalida Bedini; Silvia Rivara; Gilberto Spadoni
Journal:  Int J Mol Sci       Date:  2014-09-12       Impact factor: 5.923

  5 in total

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