%0 Journal Article
%T Exploring 6-Azaindole and 7-Azaindole Rings for Developing Cannabinoid Receptor 1 Allosteric Modulators
%A Boqiao Fu
%A Dai Lu
%A Debra A. Kendall
%A Rachel Dopart
%A Sri Sujana Immadi
%A Zhixing Wu
%J Archive of "Cannabis and Cannabinoid Research".
%D 2018
%R 10.1089/can.2018.0046
%X Introduction and Objective: {"type":"entrez-protein","attrs":{"text":"Org27569","term_id":"1179174593","term_text":"ORG27569"}}Org27569 is a prototypical allosteric modulator of the cannabinoid receptor 1 (CB1). It belongs to the indole-2-carboxamide scaffold and has been intensively investigated in pharmacology and in structure¨Cactivity relationship (SAR) studies. Although azaindoles are rare in natural products and differ only by the presence of an extra ring nitrogen, they were demonstrated as valuable bioisosteres in many pharmacologically important molecules. To extend the SAR investigation of the indole-2-carboxamide class of CB1 allosteric modulators, azaindole (pyrrolopyridine) rings were used to replace the indole ring of {"type":"entrez-protein","attrs":{"text":"Org27569","term_id":"1179174593","term_text":"ORG27569"}}Org27569 analogs to explore the potential of azaindole-2-carboxamides as CB1 allosteric modulators. Using 6- and 7-azaindole in lieu of the indole moiety within this class of CB1 allosteric modulators indeed improved the aqueous solubility
%K allosteric modulators
%K azaindole
%K bioisostere
%K cannabinoid
%K CB1 receptor
%U https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6290480/