新型呋喃香豆素类化合物作为潜在的 HIV-1 整合酶抑制剂。
Novel furocoumarins as potential HIV-1 integrase inhibitors.
机构信息
Department of Chemistry and Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Biomed, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
出版信息
Bioorg Chem. 2014 Dec;57:1-4. doi: 10.1016/j.bioorg.2014.07.008. Epub 2014 Jul 30.
A series of seven novel, rationally designed N-substituted 3-{3,5-dimethylfuro[3,2-g]coumarin-6-yl}propanamides have been prepared as potential HIV-1 integrase (IN) inhibitors via a five-step pathway commencing with resorcinol and diethyl 2-acetylglutarate, and the HIV-1 IN inhibition potential of these compounds has been examined relative to raltegravir, a known HIV-1 IN inhibitor.
已制备了一系列七个新型的、经合理设计的 N-取代的 3-{3,5-二甲基呋喃[3,2-g]色满-6-基}丙酰胺，它们可作为潜在的 HIV-1 整合酶（IN）抑制剂，通过起始于间苯二酚和二乙基 2-乙酰基戊二酸的五步法途径来制备，并且相对于已知的 HIV-1 IN 抑制剂拉替拉韦，对这些化合物的 HIV-1 IN 抑制潜力进行了检查。
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