化学
人类免疫缺陷病毒(HIV)
立体化学
化学合成
逆转录酶
突变体
组合化学
生物活性
体外
生物化学
病毒学
核糖核酸
生物
基因
作者
Jérôme Guillemont,Abdellah Benjahad,Said Oumouch,Laurence Decrane,Patrice Palandjian,Daniel Vernier,Laurence Quéguiner,Koen Andries,Marie‐Pierre de Béthune,Kurt Hertogs,David S. Grierson,Chi Hung Nguyen
摘要
A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin-2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase inhibitory properties, for example, compounds 93 and 99 are active at 0.6−50 nM against wild type HIV-1 and a panel of major simple/double HIV mutant strains.
科研通智能强力驱动
Strongly Powered by AbleSci AI