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

Haolun Jin; Sammy Metobo; Salman Jabri; Michael Mish; Rachael Lansdown; Xiaowu Chen; Manuel Tsiang; Matthew Wright; Choung U Kim

doi:10.1016/j.bmcl.2009.02.092

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

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2263-5. doi: 10.1016/j.bmcl.2009.02.092. Epub 2009 Feb 27.

Authors

Haolun Jin¹, Sammy Metobo, Salman Jabri, Michael Mish, Rachael Lansdown, Xiaowu Chen, Manuel Tsiang, Matthew Wright, Choung U Kim

Affiliation

¹ Gilead Sciences, Inc, Foster City, CA 94404, USA. hjin@gilead.com

PMID: 19285389
DOI: 10.1016/j.bmcl.2009.02.092

Abstract

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.

Publication types

Comparative Study

MeSH terms

Animals
Anti-HIV Agents / chemistry
Anti-HIV Agents / metabolism
Anti-HIV Agents / pharmacology
Binding, Competitive / physiology
Biological Availability
Cell Line
Dogs
Fluorobenzenes / chemistry*
Fluorobenzenes / metabolism
Fluorobenzenes / pharmacology
HIV Integrase Inhibitors / administration & dosage
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / pharmacology
HIV-1 / drug effects
HIV-1 / metabolism
Humans
Rats
Structure-Activity Relationship
Tumor Cells, Cultured

Substances

Anti-HIV Agents
Fluorobenzenes
HIV Integrase Inhibitors