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.
Haolun Jin  1 ,  Matthew Wright ,  Richard Pastor ,  Michael Mish ,  Sammy Metobo ,  Salman Jabri ,  Rachael Lansdown ,  Ruby Cai ,  Peter Pyun ,  Manuel Tsiang ,  Xiaowu Chen ,  Choung U Kim
Affiliations
  • 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.