Literature DB >> 15896682

Keynote review: Medicinal chemistry strategies to CB1 cannabinoid receptor antagonists.

Jos H M Lange1, Chris G Kruse.   

Abstract

The proven clinical efficacy of the CB(1) cannabinoid receptor antagonist rimonabant in both obesity and smoking cessation and its therapeutic potential in other disorders has given a tremendous impetus to the discovery of novel CB(1) antagonists. The number of disclosed patents wherein novel chemical entities having CB(1) antagonistic or inverse agonistic properties have been claimed has exploded. Besides novel compound classes that were identified in screening, rational medicinal chemistry approaches such as conformational constraint and scaffold hopping have been successfully applied. CB(1) receptor modelling has provided insight into crucial receptor-ligand interaction points thereby leading to a general CB(1) inverse agonist pharmacophore model.

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Year:  2005        PMID： 15896682     DOI： 10.1016/S1359-6446(05)03427-6

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN： 1359-6446            Impact factor:   7.851


  18 in total

1.  Exploring the binding features of rimonabant analogues and acyclic CB1 antagonists: docking studies and QSAR analysis.

Authors:  Elena Cichero; Giulia Menozzi; Andrea Spallarossa; Luisa Mosti; Paola Fossa
Journal:  J Mol Model       Date:  2008-08-12       Impact factor: 1.810

2.  Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity.

Authors:  Hong Fan; Evangelia Kotsikorou; Alexander F Hoffman; Hayden T Ravert; Daniel Holt; Dow P Hurst; Carl R Lupica; Patricia H Reggio; Robert F Dannals; Andrew G Horti
Journal:  Eur J Med Chem       Date:  2008-04-18       Impact factor: 6.514

3.  N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.

Authors:  Sean R Donohue; Robert F Dannals; Christer Halldin; Victor W Pike
Journal:  J Med Chem       Date:  2011-03-23       Impact factor: 7.446

4.  Crystal Structure of the Human Cannabinoid Receptor CB1.

Authors:  Tian Hua; Kiran Vemuri; Mengchen Pu; Lu Qu; Gye Won Han; Yiran Wu; Suwen Zhao; Wenqing Shui; Shanshan Li; Anisha Korde; Robert B Laprairie; Edward L Stahl; Jo-Hao Ho; Nikolai Zvonok; Han Zhou; Irina Kufareva; Beili Wu; Qiang Zhao; Michael A Hanson; Laura M Bohn; Alexandros Makriyannis; Raymond C Stevens; Zhi-Jie Liu
Journal:  Cell       Date:  2016-10-20       Impact factor: 41.582

5.  (4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs.

Authors:  Mariam M Mahmoud; Teresa Olszewska; Hui Liu; Derek M Shore; Dow P Hurst; Patricia H Reggio; Dai Lu; Debra A Kendall
Journal:  Mol Pharmacol       Date:  2014-11-19       Impact factor: 4.436

6.  Conformational characteristics of the interaction of SR141716A with the CB1 cannabinoid receptor as determined through the use of conformationally constrained analogs.

Authors:  Brian F Thomas; Yanan Zhang; Marcus Brackeen; Kevin M Page; S Wayne Mascarella; Herbert H Seltzman
Journal:  AAPS J       Date:  2006-10-27       Impact factor: 4.009

7.  Drugs in the pipeline for the obesity market.

Authors:  David C Klonoff; Frank Greenway
Journal:  J Diabetes Sci Technol       Date:  2008-09

8.  Bivalent ligands that target μ opioid (MOP) and cannabinoid1 (CB1) receptors are potent analgesics devoid of tolerance.

Authors:  Morgan Le Naour; Eyup Akgün; Ajay Yekkirala; Mary M Lunzer; Mike D Powers; Alexander E Kalyuzhny; Philip S Portoghese
Journal:  J Med Chem       Date:  2013-06-20       Impact factor: 7.446

9.  Enhanced Functional Activity of the Cannabinoid Type-1 Receptor Mediates Adolescent Behavior.

Authors:  Miriam Schneider; Fernando Kasanetz; Diane L Lynch; Chris M Friemel; Olivier Lassalle; Dow P Hurst; Frauke Steindel; Krisztina Monory; Carola Schäfer; Isabelle Miederer; F Markus Leweke; Mathias Schreckenberger; Beat Lutz; Patricia H Reggio; Olivier J Manzoni; Rainer Spanagel
Journal:  J Neurosci       Date:  2015-10-14       Impact factor: 6.167

10.  Tricyclic Pyrazoles. Part 5. Novel 1,4-Dihydroindeno[1,2-c]pyrazole CB2 Ligands Using Molecular Hybridization Based on Scaffold Hopping.

Authors:  Gabriele Murineddu; Battistina Asproni; Stefania Ruiu; Francesco Deligia; Matteo Falzoi; Amedeo Pau; Brian F Thomas; Yanan Zhang; Gérard A Pinna; Luca Pani; Paolo Lazzari
Journal:  Open Med Chem J       Date:  2012-05-17
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