1452219-05-4Relevant academic research and scientific papers
Extension into the entrance channel of HIV-1 reverse transcriptase - Crystallography and enhanced solubility
Bollini, Mariela,Frey, Kathleen M.,Cisneros, José A.,Spasov, Krasimir A.,Das, Kalyan,Bauman, Joseph D.,Arnold, Eddy,Anderson, Karen S.,Jorgensen, William L.
, p. 5209 - 5212 (2013/09/12)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the parent anilinylpyrimidine 1 and the morpholinoethoxy analog 2j with HIV-RT have received crystallographic characterization confirming the designs. Measurement of aqueous solubilities of 2j, 2k, the parent triazene 2a, and other NNRTIs demonstrate profound benefits for addition of the morpholinyl substituent.
