Literature DB >> 16990005

Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.

Alice Lee-Dutra1, Kristen L Arienti, Daniel J Buzard, Michael D Hack, Haripada Khatuya, Pragnya J Desai, Steven Nguyen, Robin L Thurmond, Lars Karlsson, James P Edwards, J Guy Breitenbucher.   

Abstract

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H(4) receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H(4) receptor.

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Year:  2006        PMID： 16990005     DOI： 10.1016/j.bmcl.2006.08.117

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


  6 in total

1.  Studies of H4R antagonists using 3D-QSAR, molecular docking and molecular dynamics.

Authors:  Jing Liu; Yan Li; Hui-Xiao Zhang; Shu-Wei Zhang; Ling Yang
Journal:  J Mol Model       Date:  2011-06-07       Impact factor: 1.810

Review 2.  International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Authors:  Pertti Panula; Paul L Chazot; Marlon Cowart; Ralf Gutzmer; Rob Leurs; Wai L S Liu; Holger Stark; Robin L Thurmond; Helmut L Haas
Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

3.  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

4.  DOGS: reaction-driven de novo design of bioactive compounds.

Authors:  Markus Hartenfeller; Heiko Zettl; Miriam Walter; Matthias Rupp; Felix Reisen; Ewgenij Proschak; Sascha Weggen; Holger Stark; Gisbert Schneider
Journal:  PLoS Comput Biol       Date:  2012-02-16       Impact factor: 4.475

5.  Synthesis and biological profile of substituted benzimidazoles.

Authors:  Neelam Vashist; Surinder Singh Sambi; Balasubramanian Narasimhan; Sanjiv Kumar; Siong Meng Lim; Syed Adnan Ali Shah; Kalavathy Ramasamy; Vasudevan Mani
Journal:  Chem Cent J       Date:  2018-12-01       Impact factor: 4.215

6.  Synthesis, DFT studies, molecular docking, antimicrobial screening and UV fluorescence studies on ct-DNA for novel Schiff bases of 2-(1-aminobenzyl) benzimidazole.

Authors:  Sugandha Singhal; Pankaj Khanna; Leena Khanna
Journal:  Heliyon       Date:  2019-10-11
  6 in total

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