Zemliakov A E, Tsikalova V N, Azizova L R, Chirva V Ia, Mulik E L, Shkalev M V, Kaliuzhin O V, Kiselevskiĭ M V
Bioorg Khim. 2008 Mar-Apr;34(2):245-51.
Phenyl, p-tolyl, and p-tert-butylphenyl beta-1-thio-N-acetylglucosaminides were synthesized by the treatment of thiophenols with peracetate of alpha-D-glucosaminyl chloride in the presence of triethylamine or under the conditions of phase-transfer catalysis with quaternary ammonium salts. The compounds synthesized were used for obtaining of glycosides of 4,6-O-isopropylidene-N-acetylmuramic acid, which were coupled with L-Ala-D-Glu(NH2)-OBzl and then deprotected to obtain the target aryl beta-thioglycosides of N-acetylmuramyl-L-alanyl-D-isoglutamine (MDP). The aryl beta-thioglycosides of MDP were found to stimulate an antibacterial resistance toward Staphylococcus aureus in mice. The reliable induction of the spontaneous activity of natural killers in the population of blood mononuclear cells was observed only for phenyl beta-thio-MDP at a dose of 200 microg/ml. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2008, vol. 34, no. 2; see also http://www.maik.ru.
通过在三乙胺存在下或在季铵盐相转移催化条件下,用α-D-氨基葡萄糖酰氯的过乙酸盐处理硫酚,合成了苯基、对甲苯基和对叔丁基苯基β-1-硫代-N-乙酰氨基葡萄糖苷。合成的化合物用于制备4,6-O-异亚丙基-N-乙酰胞壁酸的糖苷,将其与L-Ala-D-Glu(NH2)-OBzl偶联,然后脱保护以获得目标N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺(MDP)的芳基β-硫代糖苷。发现MDP的芳基β-硫代糖苷可刺激小鼠对金黄色葡萄球菌的抗菌抗性。仅在剂量为200μg/ml的苯基β-硫代-MDP时,观察到血液单核细胞群体中自然杀伤细胞自发活性的可靠诱导。论文英文版:《俄罗斯生物有机化学杂志》,2008年,第34卷,第2期;另见http://www.maik.ru。