Herranz R, Castro-Pichel J, García-López M T, Pérez C, Balzarini J, De Clercq E
Instituto de Química Médica, C.S.I.C., Madrid, Spain.
Arch Pharm (Weinheim). 1991 Aug;324(8):497-500. doi: 10.1002/ardp.2503240807.
5'-N-(alpha-Amino-beta-mercaptoacyl)amino-5'-deoxynucleosides have been synthesized by coupling of N-formylthiazolidines derived from D- and L-penicillamine, and D- and L-cysteine to 5'-amino-5'-deoxynucleosides using the DCC/HOSu method, followed by deprotection in N HCl in MeOH under argon. Although these compounds were designed as potential anti-HIV-1 agents, none of them showed anti-HIV-1 activity in MT-4 cells or antiviral effect against some other viruses, at concentrations below the cytotoxicity threshold.
通过使用二环己基碳二亚胺/ N-羟基琥珀酰亚胺(DCC/HOSu)方法,将源自D-和L-青霉胺以及D-和L-半胱氨酸的N-甲酰基噻唑烷与5'-氨基-5'-脱氧核苷偶联,然后在氩气保护下于甲醇中的盐酸中脱保护,合成了5'-N-(α-氨基-β-巯基酰基)氨基-5'-脱氧核苷。尽管这些化合物被设计为潜在的抗HIV-1药物,但在低于细胞毒性阈值的浓度下,它们在MT-4细胞中均未显示出抗HIV-1活性,对其他一些病毒也没有抗病毒作用。