Synthesis Of Novel 2,2-Dimethylthiazolidine And L-Cysteine Derivatives & Biological Activities Of Radiation Protection

These years, with the rapid development of radiation therapy and intense situation of the worldwide nuclear security, radioprotective agents has caused wide concern again, especially after Fukushima nuclear accident. Radioprotective agents have been used to reduce morbidity or mortality caused by ionizing irradiation. The concept that biological systems can be protected from lethal doses of ionizing radiation by chemicals first became established in 1948. So far, the developments of chemical radioprotective agents mainly focused on aminothiols derivatives, heterocyclic compounds containing sulfur and metal complexing compounds. One of them is Amifostine which has come into the market as clinical medication in many countries since the late 20th century.In this paper, it studied that 2,2-Dimethylthiazolidine, L-cysteine and other lead compounds or pharmacophores combinate on the basis of combination principle. In order to find an anti-radiation drug of aminothiols derivatives which has high anti-radiation effect and low harmful side-effects, we decide to choice 2,2-dimethylthiazolidine and L-cysteine as leading compounds and transform the chemical structure of the compounds through method of synthesis. Eight compounds have been designed and synthesized. The chemical structures of the eight new derivatives were confirmed by MS, IR,1H-NMR.The pharmacological experiments of anti-radiation biological potency and 30 days survival rate of the eight new compounds have been done. The experimental results showed that eight derivatives increased bone marrow DNA, CFU-S, spleen index and thymus index, so that they recovered fuctions of hematopoietic and immune system on irradiated mice in certain degree. Therfore, to some extent, they possessed anti-radiation activity, and so it is very valuable to further study.