1452006-62-0Relevant articles and documents
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
Bollini, Mariela,Cisneros, José A.,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
, p. 5213 - 5216 (2013/09/12)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.