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Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity

…, A Kilonda, GJ Hoornaert, F Compernolle…

文献索引:Heeres, Jan; De Jonge, Marc R.; Koymans, Lucien M. H.; Daeyaert, Frits F. D.; Vinkers, Maarten; Van Aken, Koen J. A.; Arnold, Eddy; Das, Kalyan; Kilonda, Amuri; Hoornaert, Georges J.; Compernolle, Frans; Cegla, Marek; Azzam, Rasha A.; Andries, Koen; De Bethune, Marie-Pierre; Azijn, Hilde; Pauwels, Rudi; Lewi, Paul J.; Janssen, Paul A. J. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1910 - 1918

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被引用次数: 55

摘要

Reverse transcriptase (RT), being essential in the replication process of human immunodeficiency virus (HIV), can still be considered as one of the most attractive targets for the development of new antiretroviral drugs. Currently three non-nucleoside reverse transcriptase inhibitors (NNRTIs) have been approved by the FDA for clinical use, namely, nevirapine, delavirdine, and efavirenz. ... Different chemical classes have been reported to inhibit RT, such as the ...