171048-68-3Relevant academic research and scientific papers
6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase
Tang, Jing,Maddali, Kasthuraiah,Dreis, Christine D.,Sham, Yuk Y.,Vince, Robert,Pommier, Yves,Wang, Zhengqiang
, p. 2400 - 2402 (2011/05/15)
N-3-Hydroxylation of pyrimidine-2,4-diones was recently found to yield inhibitors of both HIV-1 reverse transcriptase (RT) and integrase (IN). An extended series of analogues featuring a benzoyl group at the C-6 position of the pyrimidine ring was synthesized. Through biochemical studies it was found that these new analogues are dually active against both RT and IN in low micromolar range. Antiviral assays confirmed that these new inhibitors are active against HIV-1 in cell culture at nanomolar to low micromolar range, further validating 3-hydroxypyrimidine-2,4-diones as a viable scaffold for antiviral development.
Novel synthetic route for 5-substituted 6-arylmethylluracils from 2,4,6-trichloropyrimidines
Loksha, Yasser M.
experimental part, p. 1296 - 1301 (2010/03/23)
(Chemical Equation Presented) Treatment of 2,4,6-trichloropyrimidines (1a,b) with the sodium salt of benzyl cyanide derivatives (2a,b) afforded 5-substituted 4-aryl(cyanomethyl)-2,6-dichloropyrimidines (3a-f). Compounds 3a,b were alkylated with methyl iod
Synthesis of 6-arylvinyl analogues of the HIV drugs SJ-3366 and Emivirine
Wamberg, Michael,Pedersen, Erik B.,El-Brollosy, Nasser R.,Nielsen, Claus
, p. 1141 - 1149 (2007/10/03)
This paper reports the synthesis and the antiviral activities of a series of 6-arylvinyl substituted analogues of SJ-3366, a highly potent agent against HIV. The objective was to investigate whether substitution of the 6-arylketone with a 6-arylvinyl grou
