CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity

被引：17
作者：
Lynch, CL
Hale, JJ
Budhu, RJ
Gentry, AL
Finke, PE
Caldwell, CG
Mills, SG
MacCoss, M
Shen, DM
Chapman, KT
Malkowitz, L
Springer, MS
Gould, SL
DeMartino, JA
Siciliano, SJ
Cascieri, MA
Carella, A
Carver, G
Karen, H
Schleif, WA
Danzeisen, R
Hazuda, D
Kessler, J
Lineberger, J
Miller, M
Emini, E
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Antiviral Res, W Point, PA 19486 USA
来源：
ORGANIC LETTERS | 2003年 / 5卷 / 14期
关键词：
D O I：
10.1021/ol034707c
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
graphic A novel approach to alpha,alpha-disubstituted-beta-amino acids (beta(2,2)-amino acids) was employed in the synthesis of a series of 3-(pyrrolidin-1-yl)-propionic acids possessing high affinity for the CCR5 receptor and potent anti-HIV activity. The rat pharmacokinetics for these new analogues featured higher bioavailabilities and lower rates of clearance as compared to cyclopentane 1.
引用
收藏
页码：2473 / 2475
页数：3
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