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

Abstract

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.

Keywords:

• 2′-Deoxy-4′-C-ethynyl nucleoside
• 2,′3′-dideoxynucleoside
• nucleoside reverse transcriptase inhibitors
• drug resistant HIV
• HAART