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Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved aqueous solubility

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Abstract

Previously we identified a series of amidoalkylindoles as potent and selective CB2 partial agonists. In the present study, we report our continuous effort to improve the aqueous solubility by introducing N atoms to the amidoalkylindole framework. Synthesis, characterization, and pharmacology evaluations were described. Bioisosteric replacements of the indole nucleus with an indazole, azaindole and benzimidazole were explored. Benzimidazole 43 (EC50,CB1 = NA, EC50,CB2 = 0.067 μM) and azaindole 24 (EC50,CB1 = NA, EC50,CB2 = 0.048 μM) were found to be potent and selective CB2 receptor partial agonists, both with improved aqueous solubility.

Graphical abstract: Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved aqueous solubility

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Publication details

The article was received on 23 Aug 2019, accepted on 25 Oct 2019 and first published on 18 Nov 2019


Article type: Research Article
DOI: 10.1039/C9MD00411D
Med. Chem. Commun., 2019, Advance Article

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    Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved aqueous solubility

    Y. Ji, Z. Wang, F. Pei, J. Shi, J. Li, H. Gunosewoyo, F. Yang, J. Tang, X. Xie and L. Yu, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00411D

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