Development of 2-tbutyl-N-methyl pyrimidones as potent inhibitors of HIV integrase

被引：17

作者：

Di Francesco, M. Emilia ^{[1
]}

Pace, Paola ^{[1
]}

Fiore, Fabrizio ^{[2
]}

Naimo, Francesca ^{[2
]}

Bonelli, Fabio ^{[2
]}

Rowley, Michael ^{[1
]}

Summa, Vincenzo ^{[1
]}

机构：

[1] IRBM, MRL, Dept Med Chem, I-00040 Pomezia, Italy

[2] IRBM, MRL, Dept Drug Metab, I-00040 Pomezia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 08期

关键词：

HIV integrase; N-methyl pyrimidones; dihydroxypyrimidines; imidines;

D O I：

10.1016/j.bmcl.2008.03.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-tbutyl-N-methyl pyrimidone HIV-1 integrase inhibitors have been identified. Optimization of the initial lead resulted in compounds such as 9d and 14a, which showed high levels of activity in cell culture inhibiting viral replication with CIC95 of 10 nM in the presence of 50% normal human serum. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2709 / 2713

页数：5

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