- Tunable Heteroaromatic Sulfones Enhance in-Cell Cysteine Profiling
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Heteroaromatic sulfones react with cysteine via nucleophilic aromatic substitution, providing a mechanistically selective and irreversible scaffold for cysteine conjugation. Here we evaluate a library of heteroaromatic sulfides with different oxidation st
- Motiwala, Hashim F.,Kuo, Yu-Hsuan,Stinger, Brittany L.,Palfey, Bruce A.,Martin, Brent R.
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supporting information
p. 1801 - 1810
(2020/02/04)
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- Synthesis and anti-viral activity of azolo-adamantanes against influenza A virus
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Chemotherapy and chemoprophylaxis of influenza is one of the most important directions of health protection activity. Due to the high rate of drug-resistant strains of influenza virus, there is a need for the search and further development of new potent antivirals against influenza with a broad spectrum of activity. In the present study, a set of di-, tri- and tetrazole derivatives of adamantane was efficiently prepared and their anti-influenza activities evaluated against rimantadine-resistant strain A/Puerto Rico/8/34. In general, derivatives of tetrazole possessed the highest virus-inhibiting activity. We demonstrated that several compounds of this set exhibited much higher activity than the currently used antiviral rimantadine, a compound of related structure. Moreover, we showed that these azolo-adamantanes were significantly less toxic. This study demonstrates that influenza viruses can be inhibited by adamantyl-azoles and thus have potential for developing antiviral agents with an alternate mechanism of action.
- Zarubaev, Vladimir V.,Golod, Efim L.,Anfimov, Pavel M.,Shtro, Anna A.,Saraev, Victor V.,Gavrilov, Alexey S.,Logvinov, Alexander V.,Kiselev, Oleg I.
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experimental part
p. 839 - 848
(2010/04/29)
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