1.
Bioorg Med Chem Lett
; 21(5): 1414-8, 2011 Mar 01.
Article
in English
| MEDLINE
| ID: mdl-21295470
ABSTRACT
A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.
Subject(s)
Anti-HIV Agents/chemical synthesis , Drug Design , HIV-1/drug effects , Receptors, CXCR4/antagonists & inhibitors , Virus Replication/drug effects , Aminoquinolines , Animals , Anti-HIV Agents/chemistry , Anti-HIV Agents/pharmacokinetics , Benzimidazoles , Butylamines , DNA Replication/drug effects , Dogs , HIV-1/physiology , Heterocyclic Compounds, 1-Ring/chemistry , Molecular Structure , Rats
2.
Bioorg Med Chem Lett
; 21(1): 262-6, 2011 Jan 01.
Article
in English
| MEDLINE
| ID: mdl-21109432
ABSTRACT
An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog.