Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase—Structure–activity relationships and crystallographic analysis

TA Kirschberg, M Balakrishnan, W Huang…

Index: Kirschberg, Thorsten A.; Balakrishnan, Mini; Huang, Wei; Hluhanich, Rebecca; Kutty, Nilima; Liclican, Albert C.; McColl, Damian J.; Squires, Neil H.; Lansdon, Eric B. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1131 - 1134

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Citation Number: 28

Abstract

Despite their longstanding use in the context of highly active anti-retroviral therapy (HAART) for the treatment of HIV infections, non-nucleoside reverse-transcriptase inhibitors (NNRTIs) continue to be the focus of much pharmaceutical research. 1 Three NNRTIs are currently approved for clinical use: Efavirenz, Nevirapine, and Delavirdine (Fig. 1). Other compounds, such as TMC-125 and TMC-278, have entered late stage clinical trials. 2 Mode of action studies ...