651778-58-4Relevant articles and documents
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity
Benjahad, Abdellah,Oumouch, Said,Guillemont, Jerome,Pasquier, Elisabeth,Mabire, Dominique,Andries, Koen,Nguyen, Chi Hung,Grierson, David S.
, p. 712 - 716 (2007/10/03)
As part of a systematic SAR study on the 3-iodo-4-phenoxypyridinone 3 (IOPY) type non-nucleoside reverse transcriptase inhibitors, the analogues 4a-4z bearing different C-3 substituents were synthesized and evaluated for their anti-HIV activity against wild-type HIV-1 and four of the principal HIV mutant strains (K103N, Y181C, Y188L, and I100L). The results show that the 3-vinyl analogue 4j is the only compound which displays anti-HIV activity comparable to IOPY 3, and in this respect represents a possible back-up to this lead molecule.