A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC(95)=50 nM). Compound 4a also has improved PK properties relative to 1.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)00988-5 | DOI Listing |
Publication Analysis
Top Keywords
134 trisubstituted
8
trisubstituted pyrrolidine
8
pyrrolidine ccr5
8
ccr5 receptor
4
receptor antagonists
4
antagonists bearing
4
bearing 4-aminoheterocycle
4
4-aminoheterocycle substituted
4
substituted piperidine
4
piperidine side
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!