92860-41-8Relevant academic research and scientific papers
Synthesis of novel MKC-442 analogues with potent activities against HIV-1
El-Brollosy, Nasser R.,Pedersen, Erik B.,Nielsen, Claus
, p. 236 - 241 (2003)
Bis(alken-1-yloxy)methanes 2 were synthesized by reacting 2-cyclohexenol, 3-cyclohexenylmethanol, cinnamyl alcohol and its α-methyl analogue with dibromomethane. Condensation of 2 with 5,6-disubstituted uracil derivatives 1 resulted in the desired MKC-442 analogues 3-6. The most active compounds, N-1 cinnamyloxymethyl- and N-1 2-methyl-3-phenylallyloxymethyl substituted 5-ethyl-6-(3,5-dimethylbenzyl)uracils (5b and 6b), showed activity against wild-type HIV-1 in the nanomolar range, and against Y181C and Y181C+K103N, mutant strains known to be resistant to MKC-442, in the micromolar range.
Synthesis and antimicrobial evaluation of 6-azauracil non-nucleosides
El-Brollosy, Nasser R.
scheme or table, p. 1483 - 1490 (2009/12/26)
The present study describes synthesis and antimicrobial evaluation of a series of novel 6-azauracil non-nucleosides. Reaction of silylated 6-azauracils with the appropriate chloroethers gave the corresponding non-nucleosides. 1-(Allyloxymethy)-6-azauracils and non-nucleosides bearing indanyl, cyclohexenyl, and cyclohexyl moieties were obtained via silylation of 6-azauracils followed by treatment with the appropriate acetals. Selected compounds were tested for their in vitro antimicrobial activity against a panel of standard strains of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Four compounds showed marked inhibitory activity particularly against the tested Gram-positive bacteria.
Synthesis of new quinazoline-2,4(1H,3H)-dione non-nucleoside analogues of the reverse transcriptase inhibitor TNK-651
El-Brollosy, Nasser R.
, p. 358 - 361 (2008/02/11)
The synthesis is described of a series of new non-nucleoside analogues of the reverse transcriptase inhibitor TNK-651 from quinazoline-2,4(1H,3H)-diones. Compounds 2a-c were silylated and treated with benzyl chloromethyl ether in the presence of CsI to give 1-benzyloxymethylquinazoline derivatives 3a-c. Treatment of the silylated quinazolinediones 2a-c with the appropriate acetals 5a-e in the presence of TMS triflate afforded the corresponding TNK-651 analogues 6-10.
