期刊
MEDCHEMCOMM
卷 10, 期 12, 页码 2131-2139出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9md00411d
关键词
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资金
- Innovation Program of Shanghai Municipal Education Commission [15ZZ027]
- National Natural Science Foundation of China [81425024, 81730099]
- State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences [SIMM1501KF-05]
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 mu M) and azaindole 24 (EC50,CB1 = NA, EC50,CB2 = 0.048 mu M) were found to be potent and selective CB2 receptor partial agonists, both with improved aqueous solubility.
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