Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains

…, Y Ouyang, Z Wang, Y Cao, X Liu, L Ran…

Index: Li, Amin; Ouyang, Yabo; Wang, Ziyun; Cao, Yuanyuan; Liu, Xiangyi; Ran, Li; Li, Chao; Li, Li; Zhang, Liang; Qiao, Kang; Xu, Weisi; Huang, Yang; Zhang, Zhili; Tian, Chao; Liu, Zhenming; Jiang, Shibo; Shao, Yiming; Du, Yansheng; Ma, Liying; Wang, Xiaowei; Liu, Junyi Journal of Medicinal Chemistry, 2013 , vol. 56, # 9 p. 3593 - 3608

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Citation Number: 17

Abstract

Novel 6-substituted-4-cycloalkyloxy-pyridin-2 (1 H)-ones were synthesized as non- nucleoside reverse transcriptase inhibitors (NNRTIs), and their biological activity was evaluated. Most of the compounds, especially 26 and 22, bearing a 3-isopropyl and 3-iodine group, respectively, exhibited highly potent activity against wild-type HIV-1 strains and those resistant to reverse transcriptase inhibitors (RTIs). The diastereoisomers of 26-trans and ...