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Design, synthesis, and structure–activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists

✍ Scribed by Elizabeth M. Moir; Kazuya Yoshiizumi; Jim Cairns; Phillip Cowley; Morag Ferguson; Fiona Jeremiah; Takao Kiyoi; Richard Morphy; Jason Tierney; Grant Wishart; Mark York; James Baker; Jean E. Cottney; Andrea K. Houghton; Petula McPhail; Andrew Osprey; Glenn Walker; Julia M. Adam


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
311 KB
Volume
20
Category
Article
ISSN
0960-894X

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Design, synthesis, and structure–activit
✍ Angus J. Morrison; Julia M. Adam; James A. Baker; Robert A. Campbell; John K. Cl 📂 Article 📅 2011 🏛 Elsevier Science 🌐 English ⚖ 401 KB

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