2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, is highly potent against all human immunodeficiency viruses type 1 and has low toxicity.
An idea to use 4'-C-substituted-2'-deoxynucleoside derivatives was proposed based on a working hypothesis to solve the problems of existing acquired immune deficiency syndrome chemotherapy (highly active antiretroviral therapy). Subsequent studies have successfully proved the validity of the idea and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, which is highly potent to all human immunodeficiency viruses type 1 (HIV-1s) including multidrug-resistant HIV-1 and has a low toxicity.
Ohrui
Hiroshi
H
Yokohama College of Pharmacy, 601 Matanocho, Tozukaku, Yokohama 245-0066, Japan. dhhdb500@ybb.ne.jp
D000818:Animals; D003839:Deoxyadenosines / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D024882:Drug Resistance, Viral; D015497:HIV-1 / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D013329:Structure-Activity Relationship; D023382:Toxicity Tests, Acute
C520539:2'-deoxy-4'-C-ethynyl-2-fluoroadenosine; D003839:Deoxyadenosines; D018894:Reverse Transcriptase Inhibitors