Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and Pharmacokinetic profiles of symmetrical Heteroaryl Carboxamides

被引：55

作者：

McCombie, SW ^{[1
]}

Tagat, JR ^{[1
]}

Vice, SF ^{[1
]}

Lin, SI ^{[1
]}

Steensma, R ^{[1
]}

Palani, A ^{[1
]}

Neustadt, BR ^{[1
]}

Baroudy, BM ^{[1
]}

Strizki, JM ^{[1
]}

Endres, M ^{[1
]}

Cox, K ^{[1
]}

Dan, N ^{[1
]}

Chou, CC ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(02)00918-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The unsymmetrical nicotinamide-N-oxide moiety in compound I was replaced with symmetrical isonicotinamides as well as 4,6-dimethyl pyrimidine-5-carboxamides. Compound 16 from the latter set reduced the number of rotamers, improved potency of inhibiting UIV entry, slightly diminished the affinity for the muscarine receptors and showed very good oral absorption. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：567 / 571

页数：5

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