2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs.

Abstract:

:Structure-activity relationships and efforts to optimize the pharmacokinetic profile of isosteric analogs of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among those examined, compound 25 showed potent affinity for cannabinoid receptor 1 (CB1) and receptor 2 (CB2). This compound displayed oral bioavailability and analgesic activity.

journal_name

Bioorg Med Chem Lett

authors

Kai H,Morioka Y,Koriyama Y,Okamoto K,Hasegawa Y,Hattori M,Koike K,Chiba H,Shinohara S,Iwamoto Y,Takahashi K,Tanimoto N

doi

10.1016/j.bmcl.2008.10.070

subject

Has Abstract

pub_date

2008-12-15 00:00:00

pages

6444-7

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01276-6

journal_volume

18

pub_type

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