新型二芳基嘧啶类似物的合成及其对1型人类免疫缺陷病毒的抗病毒活性。
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
作者信息
Guillemont Jerome, Pasquier Elisabeth, Palandjian Patrice, Vernier Daniel, Gaurrand Sandrine, Lewi Paul J, Heeres Jan, de Jonge Marc R, Koymans Lucien M H, Daeyaert Frits F D, Vinkers Maarten H, Arnold Eddy, Das Kalyan, Pauwels Rudi, Andries Koen, de Béthune Marie-Pierre, Bettens Eva, Hertogs Kurt, Wigerinck Piet, Timmerman Philip, Janssen Paul A J
机构信息
Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development, Campus de Maigremont BP615, Val de Reuil, France.
出版信息
J Med Chem. 2005 Mar 24;48(6):2072-9. doi: 10.1021/jm040838n.
This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further optimized to produce compounds displaying improved activity against a panel of eight clinically relevant single and double mutant strains of human immunodeficiency virus type 1 (HIV-1).
本文报道了新型二芳基嘧啶（DAPY）化合物作为非核苷类逆转录酶抑制剂（NNRTIs）的合成及其抗病毒特性。围绕这一新的DAPY系列的合成方案得到了进一步优化，以制备对一组8种临床相关的1型人类免疫缺陷病毒（HIV-1）单突变和双突变株具有更高活性的化合物。
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