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Design, synthesis and biological activity evaluation of adenosine analogues / 药学学报
Acta Pharmaceutica Sinica ; (12): 881-886, 2013.
Article in Chinese | WPRIM | ID: wpr-259536
ABSTRACT
N6-(2-Hydroxyethyl) adenosine, HEA (1), an active ingredient isolated from cultured mycelia of cordyceps species which is a famous traditional tonic in China, showed brain protective, sedative hypnotic activity in pharmacological tests. In order to explore novel non-benzodiazepine sedative-hypnotic agents, HEA was treated as the lead compound. Twenty three target compounds were designed and synthesized. Their chemical structures were characterized by 1H NMR, MS and elemental analysis. Pharmacological test in vivo showed that target compounds 8, 4, 13 were more active than HEA on locomotor and gasping activities of mice. Structure-activity relationships showed that the ribose moiety at N-9 position of adenine base was critical for activity.
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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Structure-Activity Relationship / Molecular Structure / Random Allocation / Adenosine / Chemistry / Hypnotics and Sedatives / Mice, Inbred ICR / Motor Activity Limits: Animals Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2013 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Structure-Activity Relationship / Molecular Structure / Random Allocation / Adenosine / Chemistry / Hypnotics and Sedatives / Mice, Inbred ICR / Motor Activity Limits: Animals Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2013 Type: Article