摘要
甘氨酸转运体1(GlyT1)是研究抗精神分裂症药物的靶点。以化合物2,4-二氯-N-{[4-(环丙甲基)-1-(乙磺酰基)哌啶-4-基]甲基}苯甲酰胺(1a,IC50=92.2 nmol/L)为参考,设计并合成了未见文献报道的13个喹唑啉酮类化合物。初步药理活性实验结果表明,所合成的化合物除化合物7e外都具有一定程度的GlyT1抑制活性,其中化合物7j的活性最强,接近阳性对照药1a。
Glycine transporter-1（GlyT1） is an attractive therapeutic target for schizophrenia.A series of novel quinazolone derivatives were designed and synthesized as active GlyT1 inhibitors on the basis of compound 2,4-dichloro-N-{[4-（cyclopropylmethyl）-1-（ethylsulfonyl）piperidin-4-yl]methyl}benzamide（1a,IC50=92.2 nmol/L） developed by Merck ＆ Co Inc.Preliminary results showed that all the compounds except 7e possessed GlyT1 inhibitory activity to a different extent,and that compound 7j was the most potent one within this series of compounds,possessing almost the same potency as that of compound 1a.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2012年第3期199-203,共5页
Journal of China Pharmaceutical University
关键词
精神分裂症
甘氨酸转运体1
喹唑啉酮
设计
合成
schizophrenia syndrome
glycine transporter-1
quinazolone
design
synthesis
