Muraglia Ester, Kinzel Olaf D, Laufer Ralph, Miller Michael D, Moyer Gregory, Munshi Vandna, Orvieto Federica, Palumbi Maria Cecilia, Pescatore Giovanna, Rowley Michael, Williams Peter D, Summa Vincenzo
Department of Medicinal Chemistry, IRBM/MRL Rome, Via Pontina Km 30,600, 00040 Pomezia, Rome, Italy.
Bioorg Med Chem Lett. 2006 May 15;16(10):2748-52. doi: 10.1016/j.bmcl.2006.02.024. Epub 2006 Feb 28.
A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.
合成了一系列芳基四唑基乙酰苯胺，并作为HIV-1非核苷类逆转录酶抑制剂对野生型病毒和临床相关的K103N突变株进行了评估。广泛的构效关系研究得到了强效化合物，对K103N具有纳摩尔活性，且在大鼠体内具有口服生物利用度。
