Canna~Fangled Abstracts

Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.

By November 26, 2014 No Comments
2014 Nov 26. pii: S0960-894X(14)01224-4. doi: 10.1016/j.bmcl.2014.11.040. [Epub ahead of print]

pm1Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.

Abstract

The design and synthesis of novel 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamide CB2 selective ligands for the potential treatment of pain is described. Compound (R,R)-25 has good balance between CB2 agonist potency and selectivity over CB1, and possesses overall favorable pharmaceutical properties. It also demonstrated robust in vivo efficacy mediated via CB2 activation in the rodent models of inflammatory and osteoarthritis pain after oral administration.
Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

CB2 agonist; Cannabinoid 2 receptor; Pain

PMID:

 25488844
[PubMed – as supplied by publisher]twin memes II

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