Piperazine-based CCR5 antagonists as HIV-1 inhibitors.: I:: 2(S)-methyl piperazine as a key pharmacophore element

被引：65

作者：

Tagat, JR

McCombie, SW

Steensma, RW

Lin, SI

Nazareno, DV

Baroudy, B

Vantuno, N

Xu, S

Liu, J

机构：

[1] Schering Plough Res Inst, Dept Chem Res, Kenilworth, NJ 07033 USA

[2] Schering Plough Res Inst, Dept Antiviral Therapy, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00381-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Optimization of the piperidino-piperazines 1 and 2 provided early leads 3 and 4, which showed good activity in the CCR5-RANTES binding assay and in antiviral assays. A systematic study around these structures showed that the 2(S)-methyl piperazine is essential for CCR5 affinity, which is further enhanced by forming the 2,6-dimethyl benzamide of the piperidine. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2143 / 2146

页数：4

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