- Studies towards 4-C-alkylation of pyridin-2(1H)-one derivatives.
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In order to obtain 4-C-alkylated pyridin-2(1H)-ones, two strategies were studied: nucleophilic substitution of 4-chloro-3-nitropyridinone derivatives which essentially failed and lithiations of 2-methoxy-3-pivaloylaminopyridines which gave the expected products.
- Dolle, Valerie,Nguyen, Chi Hung,Bisagni, Emile
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p. 12505 - 12524
(2007/10/03)
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- Inhibitors of HIV reverse transcriptase
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Novel aminopyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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- Synergism of HIV reverse transcriptase inhibitors
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The combination of certain aminopyridones and anti-HIV nucleoside analogs has been found to synergistically inhibit HIV reverse transcriptase. This combination is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a combination of compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in further combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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- Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues
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A potent (IC50 = 30 nM), specific nonnucleoside HIV-1 reverse transcriptase (RT) inhibitor 3-[N-(phthalimidomethyl)amino]-5-ethyl-6- methylpyridin-2(1H)-one (1), was discovered through an in vitro screening program. This compound did not inhibi
- Hoffman,Wai,Thomas,Levin,O'Brien,Goldman
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p. 3784 - 3791
(2007/10/02)
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- Inhibitors of HIV reverse transcriptase
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Novel pyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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