Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.


Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good strategy for improving stability both in vitro and in vivo. This led to the discovery of 24, which had an… (More)
DOI: 10.1016/j.bmcl.2010.10.093


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