新型半胱胺和胱胺衍生物的合成及其辐射防护活性

Synthesis and radioprotective activity of new cysteamine and cystamine derivatives.

作者信息

Oiry J, Pue J Y, Imbach J L, Fatome M, Sentenac-Roumanou H, Lion C

出版信息

J Med Chem. 1986 Nov;29(11):2217-25. doi: 10.1021/jm00161a015.

Abstract

A variety of N-(aminoalkanoyl)-S-acylcysteamine and N,N'-bis(aminoalkanoyl)cystamine salt derivatives were synthesized. Toxicity and radioprotective activity (as the dose reduction factor DRF) were determined in vivo on mice and compared to WR 2721 and S-acetylcysteamine hydrochloride. One of the most interesting compounds of this series was N-glycyl-S-acetylcysteamine trifluoroacetate (16, I 102). Structure-activity relationships are discussed.

摘要

合成了多种N-(氨基烷酰基)-S-酰基半胱胺和N,N'-双(氨基烷酰基)胱胺盐衍生物。在小鼠体内测定了它们的毒性和辐射防护活性（作为剂量减少因子DRF），并与WR 2721和盐酸S-乙酰半胱氨酸进行了比较。该系列中最有趣的化合物之一是N-甘氨酰-S-乙酰半胱胺三氟乙酸盐(16, I 102)。讨论了构效关系。