Design, synthesis and biological activity evaluation of adenosine analogues.
- Author:
Dong-Mei WANG
1
;
Xiao-Hui LIU
;
Hui GUO
;
Jun-Hua HUANG
;
Lin WANG
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Adenosine;
analogs & derivatives;
chemical synthesis;
chemistry;
pharmacology;
Animals;
Hypnotics and Sedatives;
chemical synthesis;
chemistry;
pharmacology;
Male;
Mice;
Mice, Inbred ICR;
Molecular Structure;
Motor Activity;
drug effects;
Random Allocation;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2013;48(6):881-886
- CountryChina
- Language:Chinese
-
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.
