Literature DB >> 29419319

Synthesis and biological evaluation of ferrocene-based cannabinoid receptor 2 ligands.

Supojjanee Sansook1, Wei Tuo2, Mélanie Bollier2, Amélie Barczyk2, Xavier Dezitter2, Fredérique Klupsch2, Natascha Leleu-Chavain2, Amaury Farce2, Graham J Tizzard3, Simon J Coles3, John Spencer1, Régis Millet2.   

Abstract

Ferrocene analogs of known fatty acid amide hydrolase inhibitors and CB2 ligands have been synthesized and characterized spectroscopically and crystallographically. The resulting bio-organometallic isoxazoles were assayed for their effects on CB1 and CB2 receptors as well as on fatty acid amide hydrolase. None had any fatty acid amide hydrolase activity but compound 3, 5-(2-(pentyloxy)phenyl)-N-ferrocenylisoxazole-3-carboxamide, was found to be a potent CB2 ligand (Ki = 32.5 nM).

Entities:  

Keywords:  FAAH; cannabinoids; ferrocene; isoxazole

Mesh:

Substances:

Year:  2018        PMID: 29419319     DOI: 10.4155/fmc-2017-0200

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  1 in total

1.  Metallodrug Profiling against SARS-CoV-2 Target Proteins Identifies Highly Potent Inhibitors of the S/ACE2 interaction and the Papain-like Protease PLpro.

Authors:  Maria Gil-Moles; Sebastian Türck; Uttara Basu; Andrea Pettenuzzo; Saurav Bhattacharya; Ananthu Rajan; Xiang Ma; Rolf Büssing; Jessica Wölker; Hilke Burmeister; Henrik Hoffmeister; Pia Schneeberg; Andre Prause; Petra Lippmann; Josephine Kusi-Nimarko; Storm Hassell-Hart; Andrew McGown; Daniel Guest; Yan Lin; Anna Notaro; Robin Vinck; Johannes Karges; Kevin Cariou; Kun Peng; Xue Qin; Xing Wang; Joanna Skiba; Łukasz Szczupak; Konrad Kowalski; Ulrich Schatzschneider; Catherine Hemmert; Heinz Gornitzka; Elena R Milaeva; Alexey A Nazarov; Gilles Gasser; John Spencer; Luca Ronconi; Ulrich Kortz; Jindrich Cinatl; Denisa Bojkova; Ingo Ott
Journal:  Chemistry       Date:  2021-11-23       Impact factor: 5.020

  1 in total

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