Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs

Haolun Jin; Matthew Wright; Richard Pastor; Michael Mish; Sammy Metobo; Salman Jabri; Rachael Lansdown; Ruby Cai; Peter Pyun; Manuel Tsiang; Xiaowu Chen; Choung U Kim

doi:10.1016/j.bmcl.2008.01.018

Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1388-91. doi: 10.1016/j.bmcl.2008.01.018. Epub 2008 Jan 9.

Authors

Haolun Jin¹, Matthew Wright, Richard Pastor, Michael Mish, Sammy Metobo, Salman Jabri, Rachael Lansdown, Ruby Cai, Peter Pyun, Manuel Tsiang, Xiaowu Chen, Choung U Kim

Affiliation

¹ Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.

PMID: 18207398
DOI: 10.1016/j.bmcl.2008.01.018

Abstract

A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.

MeSH terms

Administration, Oral
Animals
Azacitidine / analogs & derivatives*
Azacitidine / chemistry
Azacitidine / pharmacology
Biological Availability
Crystallography, X-Ray
Dogs
HIV Integrase Inhibitors / chemical synthesis
HIV Integrase Inhibitors / chemistry
HIV Integrase Inhibitors / pharmacokinetics
HIV Integrase Inhibitors / pharmacology*
Humans
Organic Chemicals / chemistry
Organic Chemicals / pharmacokinetics
Organic Chemicals / pharmacology
Pyrrolidinones
Raltegravir Potassium
Rats

Substances

HIV Integrase Inhibitors
Organic Chemicals
Pyrrolidinones
Raltegravir Potassium
Azacitidine