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Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-08-27 , DOI: 10.1016/j.bmcl.2020.127516 Manoj Patel 1 , Christopher Cianci 2 , Christopher W Allard 3 , Dawn D Parker 1 , Jean Simmermacher 1 , Susan Jenkins 1 , Brian Mcauliffe 4 , Beatrice Minassian 2 , Linda Discotto 2 , Mark Krystal 4 , Nicholas A Meanwell 3 , B Narasimhulu Naidu 1
中文翻译：
设计，合成和SAR研究新型的C2-吡唑并嘧啶酰胺和作为变构整合酶抑制剂的酰胺异构体。
更新日期：2020-08-27
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-08-27 , DOI: 10.1016/j.bmcl.2020.127516 Manoj Patel 1 , Christopher Cianci 2 , Christopher W Allard 3 , Dawn D Parker 1 , Jean Simmermacher 1 , Susan Jenkins 1 , Brian Mcauliffe 4 , Beatrice Minassian 2 , Linda Discotto 2 , Mark Krystal 4 , Nicholas A Meanwell 3 , B Narasimhulu Naidu 1
Affiliation
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The design, synthesis and structure-activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of HIV-1 integrase (ALLINIs) are described. Structural modifications to these molecules were made in order to examine the effect on potency and, for select compounds, pharmacokinetic properties. We examined a variety of C2-substituted pyrazolopyrimidines and found that the C2-amide derivatives demonstrated the most potent antiviral activity of this class against HIV-1 infection in cell culture.
中文翻译：
设计，合成和SAR研究新型的C2-吡唑并嘧啶酰胺和作为变构整合酶抑制剂的酰胺异构体。
描述了与一系列作为HIV-1整合酶（ALLINIs）的有效变构抑制剂的C2取代的吡唑并嘧啶相关的设计，合成和构效关系。对这些分子进行结构修饰，以检查其对功效的影响，以及对于某些化合物而言，其药代动力学特性。我们检查了各种C2取代的吡唑并嘧啶，发现C2-酰胺衍生物在细胞培养中显示出最有效的抗HIV-1感染的抗病毒活性。
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