新型氧化吲哚作为HIV-1非核苷逆转录酶抑制剂的设计、合成及生物学评价。第2部分。
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
作者信息
Jiang Tao, Kuhen Kelli L, Wolff Karen, Yin Hong, Bieza Kimberly, Caldwell Jeremy, Bursulaya Badry, Tuntland Tove, Zhang Kanyin, Karanewsky Donald, He Yun
机构信息
Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2109-12. doi: 10.1016/j.bmcl.2006.01.066. Epub 2006 Feb 7.
A series of heterocycle-containing oxindoles was synthesized and their HIV antiviral activities were assessed. Some of these analogs exhibited potent inhibitory activities against both wild-type virus and a number of drug-resistant mutant viruses. In addition, oxindole 9z also showed promising pharmacokinetics.
合成了一系列含杂环的氧化吲哚，并评估了它们的抗HIV活性。其中一些类似物对野生型病毒和多种耐药突变病毒均表现出强效抑制活性。此外，氧化吲哚9z还显示出良好的药代动力学特性。
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