4319-73-7Relevant academic research and scientific papers
Novel peptidomimetic hepatitis C virus NS3/4A protease inhibitors spanning the P2-P1′ region
Lampa, Anna K.,Bergman, Sara M.,Gustafsson, Sofia S.,Alogheli, Hiba,Akerblom, Eva B.,Lindeberg, Gunnar G.,Svensson, Richard M.,Artursson, Per,Danielson, U. Helena,Karlen, Anders,Sandstroem, Anja
supporting information, p. 249 - 254 (2014/04/03)
Herein, novel hepatitis C virus NS3/4A protease inhibitors based on a P2 pyrimidinyloxyphenylglycine in combination with various regioisomers of an aryl acyl sulfonamide functionality in P1 are presented. The P1′ 4-(trifluoromethyl)phenyl side chain was shown to be particularly beneficial in terms of inhibitory potency. Several inhibitors with Ki-values in the nanomolar range were developed and included identification of promising P3-truncated inhibitors spanning from P2-P1′. Of several different P2 capping groups that were evaluated, a preference for the sterically congested Boc group was revealed. The inhibitors were found to retain inhibitory potencies for A156T, D168V, and R155K variants of the protease. Furthermore, in vitro pharmacokinetic profiling showed several beneficial effects on metabolic stability as well as on apparent intestinal permeability from both P3 truncation and the use of the P1′ 4-(trifluoromethyl)phenyl side chain.
CYCLIZATION OF THE PRODUCTS OF THE ADDITION OF CYANOMETHYLENETRIPHENYLPHOSPHORANE TO ACYL ISOTHIOCYANATES AS A CONVENIENT ROUTE TO FUNCTIONALLY SUBSTITUTED PYRIMIDINE DERIVATIVES
Smolii, O. B.,Panchishin, S. Ya.,Drach, B. S.
, p. 1390 - 1393 (2007/10/02)
The products of the addition of a readily accessible ylide Ph3-HCN to acyl isothiocyanates undergo an easy cyclization under the action of hydrogen chloride to give 2-alkyl(aryl)-6-mercapto-4-oxo-3,4-dihydropyrimidin-5-yltriphenylphosphonium chlorid
