Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase
A series of substituted acyl(thio)urea and 2H-1,2,4-thiadiazolo [2,3-a] pyrimidine derivatives were prepared and both of their cell culture and enzymatic activity toward influenza virus were tested. Their in vitro neuraminidase inhibitory activities were in good agreement with the corresponding activities in cultured cells and they were evaluated as potent neuraminidase inhibitors. Of the analogues that demonstrated IC50s 0.1 μM, 16 and 60 were further investigated as candidates with the most potential for future development. The molecular docking work of the representative compound was described to provide more insight into their mechanism of action and further rationalize the observations of this new series herein, which represents a novel class of highly potent and selective inhibitors of influenza virus.
Synthesis of azinylthioureas and their heterocyclization using α-chloroacetoacetic ester
Treatment of aminopyrimidines with a mixture of PhCOCl and NH 4SCN and subsequent debenzoylation of the N-benzoyl-N′-(4,6- substituted pyrimidin-2-yl)thioureas obtained gave pyrimidinyl-2-thioureas. The heterocyclization of the azinyl-2-thioure
Dovlatyan,Eliazyan,Ghazaryan,Yengoyan
p. 389 - 391
(2008/02/03)
The Synthesis of Some Pyrimidinyl and Thiazolyl Ureas and Thioureas and Some Related Compounds
Some pyrimidin-2- and pyrimidin-4-amines were treated with isocyanates and isothiocyanates to give the corresponding disubstituted ureas or thioureas.A pyrimidin-2-amine is more reactive than a pyrimidin-4-amine in these reactions. 2-Aminothiazoles and th
Hurst, Derek T.,Stacey, Anthony D.,Nethercleft, Mark,Rahim, Amjad,Harnden, Michael R.
p. 1221 - 1229
(2007/10/02)
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