Previously we identified a series of amidoalkylindoles as potent and selective CB 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 (EC = NA, EC = 0.067 μM) and azaindole (EC = NA, EC = 0.048 μM) were found to be potent and selective CB receptor partial agonists, both with improved aqueous solubility.
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| http://dx.doi.org/10.1039/c9md00411d | DOI Listing |
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