Wang Dong-Mei, Liu Xiao-Hui, Guo Hui, Huang Jun-Hua, Wang Lin
Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2013 Jun;48(6):881-6.
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.
N6-(2-羟乙基)腺苷，即HEA（1），是从中国著名传统滋补品虫草属的培养菌丝体中分离出的一种活性成分，在药理试验中显示出脑保护、镇静催眠活性。为了探索新型非苯二氮䓬类镇静催眠药物，将HEA作为先导化合物。设计并合成了23个目标化合物。通过1H NMR、MS和元素分析对其化学结构进行了表征。体内药理试验表明，目标化合物8、4、13对小鼠的运动和喘息活动的活性比HEA更强。构效关系表明，腺嘌呤碱基N-9位的核糖部分对活性至关重要。
