69764-09-6Relevant academic research and scientific papers
Benzoic acid derivative as well as preparation method and medicinal application thereof
-
Paragraph 0048; 0059-0061; 0098-0100, (2021/09/21)
The invention discloses a benzoic acid derivative as well as a preparation method and a pharmaceutical application thereof, and belongs to the technical field of medicines. The invention specifically discloses a benzoic acid derivative represented by a co
Pd(OAc)2-catalyzed one-pot preparation of anthranilates from acyclic unsaturated β-enamino esters
Kishimoto, Ryo,Mikami, Shunya,Okada, Sho,Takabatake, Tetsuhiko,Toyota, Masahiro
, (2020/02/22)
A one-pot synthesis of anthranilates from acyclic unsaturated β-enamino esters with a catalytic amount of Pd(OAc)2 was achieved for the first time. The substrates for the key catalytic reaction were easily prepared from acetoacetate esters and amines, and functionalized anthranilates were obtained in moderate to good chemical yields. A simple assembly of a 13C-labeled anthranilate was demonstrated by applying this protocol. In addition, bioactive NNI-5 was synthesized using this catalytic process.
Identification of anthranilic acid derivatives as a novel class of allosteric inhibitors of hepatitis C NS5B polymerase
Nittoli, Thomas,Curran, Kevin,Insaf, Shabana,DiGrandi, Martin,Orlowski, Mark,Chopra, Rajiv,Agarwal, Atul,Howe, Anita Y. M.,Prashad, Amar,Floyd, M. Brawner,Johnson, Bernard,Sutherland, Alan,Wheless, Karen,Feld, Boris,O'Connell, John,Mansour, Tarek S.,Bloom, Jonathan
, p. 2108 - 2116 (2008/02/06)
A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography of the enzyme-inhibitor complex. Guided by both molecular modeling and traditional SAR, the enzyme activity of the initial hit was improved by approximately 100-fold, yielding a series of potent and selective NS5B inhibitors with IC50 values as low as 10 nM. These compounds were also inhibitors of the HCV replicon in cultured HUH7 cells.
