联芳基酸：新型1型和2型HIV逆转录酶的非核苷抑制剂
Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.
作者信息
Milton J, Slater M J, Bird A J, Spinks D, Scott G, Price C E, Downing S, Green D V, Madar S, Bethell R, Stammers D K
机构信息
Department of Chemistry, GlaxoWellcome Medicines Research Center, Stevenage, Oxford.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2623-8. doi: 10.1016/s0960-894x(98)00214-5.
A series of biaryl acids has been found to show micromolar inhibition of the HIV reverse transcriptase (RT) from types 1 and 2 with IC50S in the micromolar range. The series was discovered by consideration of the polymerase active site and sub-structure searching of the company compound collection. Synthesis of analogues to investigate the SAR is described. Two of these compounds have shown inhibition of HIV-2 RT only.
已发现一系列联芳基酸对1型和2型HIV逆转录酶（RT）具有微摩尔级抑制作用，其半数抑制浓度（IC50）在微摩尔范围内。该系列是通过考虑聚合酶活性位点并对公司化合物库进行子结构搜索而发现的。文中描述了用于研究构效关系（SAR）的类似物的合成。其中两种化合物仅对HIV-2 RT有抑制作用。
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