1.
Bioorg Med Chem Lett
; 18(13): 3695-700, 2008 Jul 01.
Article
in English
| MEDLINE
| ID: mdl-18522867
ABSTRACT
The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.
Subject(s)
Benzimidazoles/chemistry , Receptor, Cannabinoid, CB2/chemistry , Benzimidazoles/chemical synthesis , Binding, Competitive , Cannabinoid Receptor Modulators/chemistry , Cannabinoids/chemistry , Chemistry, Pharmaceutical/methods , Drug Design , Humans , Models, Chemical , Receptor, Cannabinoid, CB1/chemistry , Receptors, Cannabinoid/chemistry , Structure-Activity Relationship , Technology, Pharmaceutical/methods
2.
Org Lett
; 7(4): 629-31, 2005 Feb 17.
Article
in English
| MEDLINE
| ID: mdl-15704911
ABSTRACT
The first Directed ortho Metalation (DoM) reaction of aryl O-carbamates on polystyrene-divinylbenzene (PS-DVB) resin using a trityl linker is described. Using low temperatures and short metalation times, a range of electrophiles have been introduced to give, after cleavage from support, substituted benzyl alcohols in high purity. [reaction: see text]
