Author: el Kouni, M.H.

Source: Current Pharmaceutical Design, Volume 8, Number 8, 1 April 2002 , pp. 581-593(13)

Publisher: Bentham Science Publishers

Abstract:

Human HIV infection remains incurable although several anti-HIV drugs have been identified and developed. Among these the nucleoside analogues were and remain in the forefront of anti-HIV chemotherapeutic regimens. Most of these nucleoside analogues are modified mainly in the sugar moiety. In general, they lack a free hydroxy group at the 3'-position. Consequently, they cannot participate in the formation of a 3',5'-phosphodiester linkage, which renders the nucleoside 5'-triphosphates of such nucleoside analogues effective anti-HIV agents. Preventing the formation of 3',5'- phosphodiester linkages leads to inhibition of the viral DNA strand elongation and ultimately chain termination. The phosphorylation of nucleoside analogues is a key factor in their efficacy as anti-HIV agents. Efficient phosphorylation depends largely on the structure of the nucleoside. Therefore, modification of the structure of nucleoside analogues are sought to enhance their phosphorylation and ultimately, effective inhibition of the HIV reverse transcriptase. This review is concerned with the trends in the design of nucleoside analogues as anti-HIV agents.

Keywords: Nucleoside analogues; Anti-hiv drugs; azido-3-deoxythymidine; didehydro-3-deoxythymidine; Diaminopurine dioxolane(dapd); dioxolane guanosine (dxg); Diaminopurine dioxolane(dapd); thiocytidine(bch-01652,dotc); dideoxyinosine (ddl); dideoxycytidine(ddc)

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612024607171

Publication date: 2002-04-01

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• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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