From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.

  • Alessia Petrocchi
  • Uwe Koch-Gromus
  • Victor G Matassa
  • Barbara Pacini
  • Kara A Stillmock
  • Vincenzo Summa

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Abstract

4,5-Dihyroxypyrimidine carboxamides, which evolved from a related series of HCV NS5b polymerase inhibitors, have been optimized to provide selective HIV integrase strand transfer inhibitors. Extensive SAR around the benzylamide moiety led to the identification of the p-fluorobenzylamide as optimal in the enzymatic assay.

Bibliographical data

Original languageGerman
Article number2
ISSN0960-894X
Publication statusPublished - 2007
pubmed 17107799