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

✍ Scribed by Takao Kiyoi; Mark York; Stuart Francis; Darren Edwards; Glenn Walker; Andrea K. Houghton; Jean E. Cottney; James Baker; Julia M. Adam


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
998 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