Literature DB >> 15544557

Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists.

Holger Stark1, Markus Kathmann, Eberhard Schlicker, Walter Schunack, Birgit Schlegel, Wolfgang Sippl.   

Abstract

The first antagonists known for the histamine H3 receptor were mono-substituted imidazole-containing compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.

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Year:  2004        PMID： 15544557     DOI： 10.2174/1389557043403107

Source DB:  PubMed          Journal:  Mini Rev Med Chem        ISSN： 1389-5575            Impact factor:   3.862


  10 in total

1.  Search for novel, high affinity histamine H3 receptor ligands with fluorescent properties.

Authors:  K J Kuder; T Kottke; H Stark; X Ligneau; J-C Camelin; R Seifert; K Kieć-Kononowicz
Journal:  Inflamm Res       Date:  2010-03       Impact factor: 4.575

2.  Highly enantioselective dearomatizing formal [3+3] cycloaddition reactions of N-acyliminopyridinium ylides with electrophilic enol carbene intermediates.

Authors:  Xinfang Xu; Peter Y Zavalij; Michael P Doyle
Journal:  Angew Chem Int Ed Engl       Date:  2013-10-02       Impact factor: 15.336

Review 3.  Multiple Targeting Approaches on Histamine H3 Receptor Antagonists.

Authors:  Mohammad A Khanfar; Anna Affini; Kiril Lutsenko; Katarina Nikolic; Stefania Butini; Holger Stark
Journal:  Front Neurosci       Date:  2016-05-30       Impact factor: 4.677

4.  Structure-based prediction of subtype selectivity of histamine H3 receptor selective antagonists in clinical trials.

Authors:  Soo-Kyung Kim; Peter Fristrup; Ravinder Abrol; William A Goddard
Journal:  J Chem Inf Model       Date:  2011-11-16       Impact factor: 4.956

5.  Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.

Authors:  Ashwin U Rao; Ning Shao; Robert G Aslanian; Tin-Yau Chan; Sylvia J Degrado; Li Wang; Brian McKittrick; Mary Senior; Robert E West; Shirley M Williams; Ren-Long Wu; Joyce Hwa; Bhuneshwari Patel; Shuqin Zheng; Christopher Sondey; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2011-11-21       Impact factor: 4.345

6.  Generation of a homology model of the human histamine H(3) receptor for ligand docking and pharmacophore-based screening.

Authors:  Birgit Schlegel; Christian Laggner; Rene Meier; Thierry Langer; David Schnell; Roland Seifert; Holger Stark; Hans-Dieter Höltje; Wolfgang Sippl
Journal:  J Comput Aided Mol Des       Date:  2007-08-01       Impact factor: 3.686

7.  Design, synthesis, and in vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H3 receptor antagonists.

Authors:  Marek Staszewski; Anna Stasiak; Tadeusz Karcz; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Katarzyna Kieć-Kononowicz; Rob Leurs; Krzysztof Walczyński
Journal:  Medchemcomm       Date:  2019-01-11       Impact factor: 3.597

8.  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

9.  Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines.

Authors:  Roman Guryn; Marek Staszewski; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Molecules       Date:  2018-02-03       Impact factor: 4.411

10.  4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity.

Authors:  Gábor Wágner; Tamara A M Mocking; Marta Arimont; Gustavo Provensi; Barbara Rani; Bruna Silva-Marques; Gniewomir Latacz; Daniel Da Costa Pereira; Christina Karatzidou; Henry F Vischer; Maikel Wijtmans; Katarzyna Kieć-Kononowicz; Iwan J P de Esch; Rob Leurs
Journal:  J Med Chem       Date:  2019-11-20       Impact factor: 7.446
  10 in total

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