Synthetic chemistry-led creation of a difluorinated biaryl ether non-nucleoside reverse transcriptase inhibitor.
In the process of developing a series of novel, fluorinated biaryl ether NNRTIs, we fortuitously discovered derivative 20, which possesses excellent potency against both wild-type and clinically relevant mutations of the reverse transcriptase enzyme.
Jones
Lyn H
LH
Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, UK CT13 9NJ. lyn.jones@pfizer.com
Randall
Amy
A
Barba
Oscar
O
Selby
Matthew D
MD
D002626:Chemistry, Pharmaceutical; D004987:Ethers / Q000737:chemistry* / Q000494:pharmacology*; D005461:Fluorine / Q000737:chemistry*; D015394:Molecular Structure; D009154:Mutation; D009705:Nucleosides / Q000737:chemistry; D012194:RNA-Directed DNA Polymerase / Q000737:chemistry* / Q000187:drug effects / Q000235:genetics; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry
D004987:Ethers; D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors; D005461:Fluorine; D012194:RNA-Directed DNA Polymerase