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- W1984975543 abstract "Novel analogues of MKC442 (6-benzyl-1-(ethoxymethyl)-5-isopropylpyrimidine-2,4(1H,3H)-dione) were synthesized by reaction of 6-[(3,5-dimethylphenyl)fluoromethyl]-5-ethyluracil (5) with ethoxymethyl chloride and formaldehyde acetals. The Sonogashira reaction was carried out on the N1-(p-iodobenzyl)oxy]methyl derivative of compound 5 using propagyl alcohol to afford compound 12 (YML220). The latter compound was selected for further studies since it showed the most potent and selective activity in vitro against wild-type HIV-1 and non-nucleoside reverse transcriptase inhibitor-, nucleoside reverse transcriptase inhibitor-, and protease inhibitor-resistant mutants and a wide range of HIV-1 clinical isolates. 12 also showed microbicidal activity in long-term assays with heavily infected MT-4 cells." @default.
- W1984975543 created "2016-06-24" @default.
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- W1984975543 date "2014-06-03" @default.
- W1984975543 modified "2023-10-12" @default.
- W1984975543 title "Synthesis of Novel Fluoro Analogues of MKC442 as Microbicides" @default.
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- W1984975543 doi "https://doi.org/10.1021/jm500139a" @default.
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