𝔖 Bobbio Scriptorium
✦   LIBER   ✦

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

✍ Scribed by Angus J. Morrison; Julia M. Adam; James A. Baker; Robert A. Campbell; John K. Clark; Jean E. Cottney; Maureen Deehan; Anna-Marie Easson; Ruth Fields; Stuart Francis; Fiona Jeremiah; Neil Keddie; Takao Kiyoi; Duncan R. McArthur; Karsten Meyer; Paul D. Ratcliffe; Jurgen Schulz; Grant Wishart; Kazuya Yoshiizumi

Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
401 KB
Volume
21
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

✦ Synopsis

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 increased duration of action in the mouse tail flick test in comparison to the lead 1.

📜 SIMILAR VOLUMES

ChemInform Abstract: Novel Indole and Az
ChemInform Abstract: Novel Indole and Azaindole (Pyrrolopyridine) Cannabinoid (CB) Receptor Agonists: Design, Synthesis, Structure—Activity Relationships, Physicochemical Properties and Biological Activity.
✍ Antoni R. Blaazer; Jos H. M. Lange; Martina A. W. van der Neut; Arie Mulder; Fem 📂 Article 📅 2012 🏛 John Wiley and Sons ⚖ 38 KB 👁 1 views

## Abstract The discovery, synthesis, and SAR of a novel series of cannabinoid 1 (CB~1~) and cannabinoid 2 (CB~2~) receptor ligands are reported.