Synthesis and Evaluation of N4-Arylsulfonylquinoxalinones as HIV-1 Reverse Transcriptase Inhibitors

• 作 者: Bailing Xu Jie zhou Haibo Zhou Ying Guo
• 机 构: Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beiji
• 出 处: 第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
• 发表日期: 2012年8期

　　At present,there are more than 20 anti-HIV drugs,which belonged to 6 different classes,approved since the first anti-HIV drug,azidothymidine (AZT)marketed in 1987.1 Among them,NNRTIs are still an important class of anti-HIV drugs due to their possessing high potency and low toxicity.2,3 Nevertheless,a primary drawback in the use of the approved NNRTIs is the rapid emergence of drug resistance.Therefore,a great challenge is continuously to develop new chemical entities that are effective against both the wild type and mutant forms of the reverse transcriptase.