944826-07-7Relevant academic research and scientific papers
Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors
Wang, Yue-Ping,Chen, Fen-Er,De Clercq, Erik,Balzarini, Jan,Pannecouque, Christophe
experimental part, p. 1016 - 1023 (2009/09/29)
A series of new 5-alkyl-2-benzylsulfanylpyrimidin-4(3H)-ones (5a-y) bearing different substituted arylmethyl moieties at the C-6 position of the pyrimidine core have been synthesized and evaluated for their in vitro activities against HIV-1 and HIV-2 in MT-4 cell cultures. The majority of the title compounds showed moderate to good activities against HIV-1 with an IC50 range from 6.67 μM to 0.12 μM. Among them, 6-(3,5-dimethylbenzyl) analogue 5q exhibited the most potent anti-HIV-1 activity (IC50 = 0.12 μM, SI > 2642), which was about 40-fold more active than the reference compounds 1-[(2-hydroxyethoxy)methyl]-6-(phenylsulfanyl)thymine (HEPT) and 2′,3′-dideoxyinosine (DDI). The structure-activity relationships (SARs) of these new congeners were further discussed.
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Wang, Yue-Ping,Chen, Fen-Er,De Clercq, Erik,Balzarini, Jan,Pannecouque, Christophe
, p. 3887 - 3894 (2008/12/20)
A novel series of 2-arylcarbonylmethylthio-6-arylmethylpyrimidin-4(3H)-ones have been synthesized and evaluated for in vitro anti-HIV activities in MT-4 cells. Most of these new compounds showed moderate to potent activities against wild-type HIV-1 with a
Synthesis and anti-HIV-1 activity of new MKC-442 analogues with an alkynyl-substituted 6-benzyl group
Aly, Youssef L.,Pedersen, Erik B.,La Colla, Paolo,Loddo, Roberta
, p. 225 - 235 (2008/02/09)
Synthesis and antiviral activities are reported of a series of 6-(3-alkynyl benzyl)-substituted analogues of MKC-442 (6-benzyl-1-(ethoxymethyl)-5- isopropyluracil), a highly potent agent against HIV. The 3-alkynyl group is assumed to give a better stackin
