2'-deoxy-4'-C-ethynyl-2-fluoroadenosine: a nucleoside reverse transcriptase inhibitor with highly potent activity against wide spectrum of HIV-1 strains, favorable toxic profiles, and stability in plasma.
Working hypotheses to solve the critical problems of the existing highly active anti-retroviral therapy were proposed. The study based on the hypotheses proved the validity of the hypotheses and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, with highly potent activity against all HIV-1, very favorable toxic profiles, and stability in plasma. The nucleoside will prevent or delay the emergence of drug-resistant HIV-1 variants and be an ideal therapeutic agent for both HIV-1 and HBV infections.
Ohrui
Hiroshi
H
Yokomama College of Pharmacy, 601 Matano-cho, Totsuka, Yokohama, Japan. h.ohrui@hamayaku.ac.jp
Kohgo
Satoru
S
Hayakawa
Hiroyuki
H
Kodama
Eiichi
E
Matsuoka
Masao
M
Nakata
Tomohiro
T
Mitsuya
Hiroaki
H
D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D003839:Deoxyadenosines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D051379:Mice; D013329:Structure-Activity Relationship
C520539:2'-deoxy-4'-C-ethynyl-2-fluoroadenosine; D019380:Anti-HIV Agents; D003839:Deoxyadenosines; D054303:HIV Reverse Transcriptase