80819-65-4Relevant academic research and scientific papers
Fragment-Based Drug Design Facilitated by Protein-Templated Click Chemistry: Fragment Linking and Optimization of Inhibitors of the Aspartic Protease Endothiapepsin
Mondal, Milon,Unver, M. Yagiz,Pal, Asish,Bakker, Matthijs,Berrier, Stephan P.,Hirsch, Anna K. H.
, p. 14826 - 14830 (2016/10/11)
There is an urgent need for the development of efficient methodologies that accelerate drug discovery. We demonstrate that the strategic combination of fragment linking/optimization and protein-templated click chemistry is an efficient and powerful method that accelerates the hit-identification process for the aspartic protease endothiapepsin. The best binder, which inhibits endothiapepsin with an IC50value of 43 μm, represents the first example of triazole-based inhibitors of endothiapepsin. Our strategy could find application on a whole range of drug targets.
PROCESS FOR PREPARATION OF 1,2,3-TRIAZOLE-4 CARBOXAMIDES
-
Paragraph 0064; 0070, (2014/06/23)
The invention relates to the preparation of 1,2,3-triazole-4-carboxamide of general Formula I: wherein R1 and R2 may be the same or different and are selected from H, F, Cl, Br, I, OR, C(O)R, NH2, NHR or NR2. R can be a linear or branched alkyl group, for example a C1-C4 alkyl group. In exemplary embodiments, R1 and R2 are independently selected from H, F, Cl, Br, and I. The compound of Formula I can be Rufinamide.
Copper(I)-catalyzed aerobic oxidative azide-alkene cyclo-addition: An efficient synthesis of substituted 1,2,3-triazoles
Janreddy, Donala,Kavala, Veerababurao,Kuo, Chun-Wei,Chen, Wen-Chang,Ramesh, Chintakunta,Kotipalli, Trimurtulu,Kuo, Ting-Shen,Chen, Mei-Ling,He, Chiu-Hui,Yao, Ching-Fa
, p. 2918 - 2927 (2014/03/21)
A novel, copper(I)-promoted azide-alkene aerobic oxidative cycloaddition protocol was devel-oped for the regioselective synthesis of 1,4-disubsti-tuted/ 1,4,5-trisubstituted 1,2,3-triazoles by using azides and electron-deficient olefins under an oxygen atmosphere.
An abnormal N-heterocyclic carbene-copper(I) complex in click chemistry
Sau, Samaresh Chandra,Roy, Sudipta Raha,Sen, Tamal K.,Mullangi, Dinesh,Mandal, Swadhin K.
, p. 2982 - 2991 (2014/03/21)
Herein we report the synthesis of a copper(I) chloro complex using an abnormal N-heterocyclic carbene (aNHC) salt, 1,3-bis(2,6-diisopropylphenyl)-2,4- diphenylimidazolium. The Cu(aNHC) complex efficiently catalyzed Huisgen 1,3-dipolar cycloaddition reacti
