New Emivirine (MKC-442) Analogues Containing a Tetrahydronaphthalene at C-6 and their Anti-HIV Activity |
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Authors: | Frans Therkelsen Per T Jørgensen Claus Nielsen Erik B Pedersen |
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Institution: | (1) Nucleic Acid Center, Department of Chemistry, University of Southern Denmark, Odense M, Denmark;(2) Retrovirus Laboratory, Department of Virology, State Serum Institute, Copenhagen, Denmark |
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Abstract: | Summary. An 5-ethyl-2-thiouracil derivative with a 6-(tetrahydronaphthalen-1-yl)methyl substituent was synthesized by condensation
of thiourea with an adequate β-ketoester which in turn was synthesized in a single step from (tetrahydronaphthalen-1-yl)acetonitrile.
The latter starting material was also used to synthesize an analogously substituted tetrahydronaphthalen-1-yl substituted
uracil with a locked conformation. Only the non-nucleoside derivatives prepared from the desulfurized substituted 2-thiouracil
showed moderate activity against HIV whereas a corresponding non-nucleoside derivative was devoid of activity against HIV. |
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