Ladurée D, Sugeac E, Fossey C, Schmidt S, Laumond G, Aubertin A M
Centre d'Etudes et de Recherche sur le Médicament de Normandie U.F.R. des Sciences Pharmaceutiques, Caen, France.
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):873-5. doi: 10.1081/NCN-120022675.
Expected for the ability to inhibit HIV replication, we report the synthesis of two heterodimers of the general formula: [2NRTI]-C5-GLY-SUCCINYL-Npiperazinyl-[NNRTI] (18, 19) containing both a Nucleoside Reverse Transcriptase Inhibitor (10, 11) and a Non-Nucleoside Reverse Transcriptase Inhibitor (8) [Trovirdine Analogue belonging of the phenethyl thiazolyl thiourea class] connected through the "succinyl-glycine" spontaneously cleavable linker.
基于抑制HIV复制的能力，我们报道了通式为[2NRTI]-C5-甘氨酰-琥珀酰基-N-哌嗪基-[NNRTI]（18, 19）的两种异二聚体的合成，该异二聚体包含一个核苷类逆转录酶抑制剂（10, 11）和一个非核苷类逆转录酶抑制剂（8）[属于苯乙基噻唑基硫脲类的曲韦定类似物]，它们通过“琥珀酰-甘氨酸”可自发裂解的连接子相连。
