A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors.
4-(Arylthio)-pyridin-2(1H)-ones variously substituted in their 3-, 5-, and 6-positions have been synthesized as a new series of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-pyridinone hybrid molecules. Biological studies revealed that some of them show potent HIV-1 specific reverse transcriptase inhibitory properties. Compounds 16 and 7c, the most active ones, inhibit the replication of HIV-1 at 3 and 6 nM, respectively.
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D054303:HIV Reverse Transcriptase; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology* / Q000502:physiology; D015498:HIV-2 / Q000201:enzymology; D007700:Kinetics; D015394:Molecular Structure; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology; D012194:RNA-Directed DNA Polymerase / Q000378:metabolism*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
C096773:3-amino-5-ethyl-6-methyl-4-((3',5'-dimethylphenyl)thio)pyridin-2(1H)-one; C096774:5-ethyl-6-methyl-3-nitro-4-((3',5'-dimethylphenyl)thio)pyridin-2(1H)-one; D000998:Antiviral Agents; D011728:Pyridones; D011994:Recombinant Proteins; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase; D012194:RNA-Directed DNA Polymerase