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Chem Biol Drug Des ; 67(4): 305-8, 2006 Apr.
Article in English | MEDLINE | ID: mdl-16629828

ABSTRACT

The development of compound 1, a piperidine-based CCR5 receptor antagonist with Type I CYP2D6 inhibition, into the tropane-derived analogue 5, is described. This compound, which is devoid of CYP2D6 liabilities, is a highly potent ligand for the CCR5 receptor and has broad-spectrum activity against a range of clinically relevant HIV isolates. The identification of human ether a-go-go-related gene channel inhibition within this series is described and the potential for QTc interval prolongation discussed. Furthermore, structure activity relationship (SAR) around the piperidine moiety is also described.


Subject(s)
Anti-HIV Agents/chemistry , CCR5 Receptor Antagonists , Tropanes/chemistry , Anti-HIV Agents/chemical synthesis , Anti-HIV Agents/pharmacology , Cytochrome P-450 CYP2D6 Inhibitors , HIV-1/drug effects , Humans , Models, Molecular , Piperidines/chemistry , Receptors, CCR5/metabolism , Structure-Activity Relationship , Tropanes/chemical synthesis , Tropanes/pharmacology
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