1049809-51-9Relevant articles and documents
Practical synthesis of a cathepsin S Inhibitor: Route identification, purification strategies, and serendipitous discovery of a crystalline salt form
Deng, Xiaoliu,Liang, Jimmy T.,Peterson, Matthew,Rynberg, Raymond,Cheung, Eugene,Mani, Neelakandha S.
experimental part, p. 1940 - 1947 (2010/05/18)
Chemical Equation Presented A redox economical strategy resulted in a concise, modular synthesis of compound 1, a potent Cathepsin S inhibitor. Starting from three building blocks, crude drug substance was prepared, in a two-step sequence in high yield. Efficient purification of the crude drug substance was accomplished via the formation of an unusual monoethyl oxalate salt.
Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements
Ameriks, Michael K.,Axe, Frank U.,Bembenek, Scott D.,Edwards, James P.,Gu, Yin,Karlsson, Lars,Randal, Mike,Sun, Siquan,Thurmond, Robin L.,Zhu, Jian
scheme or table, p. 6131 - 6134 (2010/06/13)
A crystal structure of 1 bound to a Cys25Ser mutant of cathepsin S helped to elucidate the binding mode of a previously disclosed series of pyrazole-based CatS inhibitors and facilitated the design of a new class of arylalkyne analogs. Optimization of the