959238-10-9Relevant articles and documents
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-iodopyridin-2(1H)-one type anti-HIV agents
Guillemont, Jér?me,Benjahad, Abdellah,Oumouch, Said,Decrane, Laurence,Palandjian, Patrice,Vernier, Daniel,Queguiner, Laurence,Andries, Koen,De Béthune, Marie-Pierre,Hertogs, Kurt,Grierson, David S.,Nguyen, Chi Hung
experimental part, p. 7473 - 7487 (2010/06/11)
A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin- 2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase inhibitory properties, for example, compounds 93 and 99 are active at 0.6-50 nM against wild type HIV-1 and a panel of major simple/double HIV mutant strains.
