Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-06-14 , DOI: 10.1007/s11094-021-02402-3 L A Baltina 1 , R M Kondratenko 2 , L A Baltina 1 , O A Plyasunova 3
A new method for the synthesis of glycyrrhizic acid (GA) conjugates with S-benzyl-L-cysteine using 1-ethyl-3-(3-dimethylaminoproopyl)carbodiimide is proposed. It is established that 3-O-{2-O-[N-(β-D-glucopyranosyluronyl)-L-cysteine-S-benzyl]-N-(β-D-glucopyranosyluronyl)-L-cysteine-S-benzyl}-(3β,20β)-11-oxo-30-(N-carbonyl-L-cysteine-S-benzyl)-30-norolean-12-ene is superior to GA in inhibiting the accumulation of HIV-I virus-specific protein p24 (viral antigen) in MT-4 cell culture (IC50 3 μg/mL, SI 90) and is 50 – 55 times less toxic to cells than azidothymidine.
中文翻译:
甘草酸与S-苄基-L-半胱氨酸缀合物的合成及其抗病毒活性
提出了一种使用 1-乙基-3-(3-二甲氨基丙酰)碳二亚胺合成甘草酸 (GA) 与 S-苄基-L-半胱氨酸缀合物的新方法。确定3- O- {2- O- [ N- (β- D-吡喃葡萄糖醛酸基) -L-半胱氨酸-S-苄基] -N- (β- D-吡喃葡萄糖醛酸基) -L-半胱氨酸-S-苄基}-(3β,20β)-11-oxo-30-( N-羰基-L-半胱氨酸-S-苄基)-30-norolean-12-ene在抑制HIV-I病毒特异性积累方面优于GA MT-4 细胞培养物中的蛋白 p24(病毒抗原)(IC 50 3 μg/mL,SI 90),对细胞的毒性比叠氮胸苷低 50 – 55 倍。