环状脲类作为HIV蛋白酶抑制剂的合成与评价：P1/P1'残基的修饰
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
作者信息
Patel M, Bacheler L T, Rayner M M, Cordova B C, Klabe R M, Erickson-Viitanen S, Seitz S P
机构信息
Department of Chemical & Physical Sciences, DuPont Merck Pharmaceutical Company, Experimental Station, Wilmington, DE 19880-0500, USA.
出版信息
Bioorg Med Chem Lett. 1998 Apr 7;8(7):823-8. doi: 10.1016/s0960-894x(98)00119-x.
PMID:9871548
Abstract
Two series of cyclic ureas modified at the P1/P1' residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-methoxy analog) showed significant improvement in antiviral activity relative to lead compounds DMP323 and DMP 450.
摘要
制备了在P1/P1'残基处修饰的两系列环状脲，并对其进行了HIV蛋白酶抑制和全细胞抗病毒活性评估。与先导化合物DMP323和DMP 450相比，化合物8b、10（3-和4-吡啶基甲基类似物）和6b（4-甲氧基类似物）的抗病毒活性有显著提高。
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