Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1

被引：114

作者：

Guillemont, J

Pasquier, E

Palandjian, P

Vernier, D

Gaurrand, S

Lewi, PJ

Heeres, J

de Jonge, MR

Koymans, LMH

Daeyaert, FFD

Vinkers, MH

Arnold, E

Das, K

Pauwels, R

Andries, K

de Béthune, MP

Bettens, E

Hertogs, K

Wigerinck, P

Timmerman, P

Janssen, PAJ

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Dept Med Chem, Val De Reuil, France

[2] Janssen Pharmaceut NV, Ctr Mol Design, Vosselaar, Belgium

[3] Tibotec, B-2800 Mechelen, Belgium

[4] Johnson & Johnson Pharmaceut Res & Dev, Dept Pharmacokinet, B-2340 Beerse, Belgium

[5] Rutgers State Univ, Dept Chem, Ctr Adv Biotechnol & Med, Piscataway, NJ 08854 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 06期

关键词：

D O I：

10.1021/jm040838n

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further optimized to produce compounds displaying improved activity against a panel of eight clinically relevant single and double mutant strains of human immunodeficiency virus type 1 (HIV-1).

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收藏

页码：2072 / 2079

页数：8

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