| Literature DB >> 2033590 |
J T Huang1, L C Chen, L B Wang, M H Kim, J A Warshaw, D Armstrong, Q Y Zhu, T C Chou, K A Watanabe, J Matulic-Adamic.
Abstract
In order to obtain agents with therapeutic indices superior to those of AZT, FLT, or D4T, several analogues of anti-HIV-1 nucleosides were synthesized. These include 2',3'-dideoxy-2',3' -difluoro-5-methyluridine (13), its arabino analogue 19, arabino-5-methylcytosine analogue 21, 3'-deoxy-2',3'-didehydro-2' -fluorothymidine (25), 3'-azido-2',3'-dideoxy-2'-fluoro-5-methyluridine (29), 2'-azido-3'-fluoro-2',3'-dideoxy-5-methyluridine (31), and 2'3'-dideoxy-2' -fluoro-5-methyluridine (37). These new nucleosides were screened for their activity against HIV and feline TLV in vitro. None of the compounds showed significant activity. It is interesting to note that such a small modification in the sugar moiety of active anti-HIV nucleosides (i.e., displacement of hydrogen by fluorine) almost completely inactivate the agents.Entities:
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Year: 1991 PMID： 2033590 DOI： 10.1021/jm00109a017
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446