29836-02-0Relevant articles and documents
Synthesis and primary evaluation of novel HIV-1 inhibitors
Safadi, Yazan El,Marquet, Roland,Aubertin, Anne-Marie,Vivet-Boudou, Valerie
, p. 1161 - 1165 (2007)
The overcoming of antiviral drug resistance is an important challenge in the treatment of HIV-1 infection. According to the theory of viral error catastrophe, slightly increasing the mutation rate could exceed the error threshold for viability of a viral population and kill it. Investigation of this mechanism could lead to the discovery of new antiviral agents capable of bypassing viral resistance. To this aim, we designed several modified nucleosides. We describe here the synthesis and partial evaluation of 8-amido-2′-deoxyadenosine. The supplementary amide group on the base should allow base-pairing with several natural nucleosides, thus creating supplementary mutations that would kill the virus. Copyright Taylor & Francis Group, LLC.
Hydrolysis of 2'-Deoxypurine Nucleosides. The Effect of Substitution at the C-8 Position.
Laayoun, Ali,Decout, Jean-Luc,Lhomme, Jean
, p. 4989 - 4990 (2007/10/02)
The hydrolytic stability of 2'-deoxypurine nucleosides is decreased by introduction of electronwithdrawing substituents at the C-8 position in the series of compounds 2-8, 10-14.The sulfone group causes a 2.9 x 104 rate acceleration for glycosidic, bond cleavage in compound 14.