新型 C2-吡唑并嘧啶酰胺和酰胺类变构整合酶抑制剂的设计、合成及构效关系研究。
Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors.
机构信息
Departments of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA; ViiV Healthcare, 36 East Industrial Parkway, Branford, CT 06405, USA.
Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2020 Nov 1;30(21):127516. doi: 10.1016/j.bmcl.2020.127516. Epub 2020 Aug 27.
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.
本文描述了一系列 C2 取代的吡唑并嘧啶类化合物作为有效的 HIV-1 整合酶别构抑制剂（ALLINIs）的设计、合成和构效关系。对这些分子进行了结构修饰，以研究其对效力的影响，并且针对某些化合物，还研究了其药代动力学性质。我们研究了多种 C2 取代的吡唑并嘧啶类化合物，发现 C2-酰胺衍生物在细胞培养中对 HIV-1 感染具有最强的抗 HIV-1 活性。
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