Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety

SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compounds with potency and PK properties comparable to raltegravir were identified. SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compou...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-04, Vol.19 (8), p.2263-2265
Main Authors: Jin, Haolun, Metobo, Sammy, Jabri, Salman, Mish, Michael, Lansdown, Rachael, Chen, Xiaowu, Tsiang, Manuel, Wright, Matthew, Kim, Choung U.
Format: Article
Language:English
Subjects:
AIDS
Animals
Anti-HIV Agents - chemistry
Anti-HIV Agents - metabolism
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Benzyl moiety
Binding, Competitive - physiology
Biological and medical sciences
Biological Availability
Cell Line
Dogs
Fluorobenzenes - chemistry
Fluorobenzenes - metabolism
Fluorobenzenes - pharmacology
HIV
HIV Integrase Inhibitors - administration & dosage
HIV Integrase Inhibitors - chemical synthesis
HIV Integrase Inhibitors - pharmacology
HIV-1 - drug effects
HIV-1 - metabolism
Human immunodeficiency virus
Humans
Integrase inhibitor
Medical sciences
Pharmacology. Drug treatments
Rats
Structure-Activity Relationship
Tricyclic
Tumor Cells, Cultured
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Summary:SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compounds with potency and PK properties comparable to raltegravir were identified. SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compounds with potency and PK properties comparable to raltegravir were identified.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.02.092