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, 2014No 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.

Han S1, Thoresen L2, Zhu X2, Narayanan S2, Jung JK2, Strah-Pleynet S2, Decaire M2, Choi K2, Xiong Y2, Yue D2, Semple G2, Thatte J2, Solomon M2, Fu L2, Whelan K2, Al-Shamma H2, Gatlin J2, Chen R2, Dang H2, Pride C2, Gaidarov I2, Unett DJ2, Behan DP2, Sadeque A2, Usmani KA2, Chen C2, Edwards J2, Morgan M2, Jones RM2.

Author information 

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