149246-82-2Relevant articles and documents
Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors
Petek, Nejc,?tefane, Bogdan,Novinec, Marko,Svete, Jurij
, p. 226 - 238 (2019)
A series of novel 7-aminoalkyl substituted pyrazolo[1,5-a]pyrimidine derivatives were synthesized and tested for inhibition of cathepsin K. The synthetic methodology comprises cyclization of 5-aminopyrazoles with N-Boc-α-amino acid-derived ynones followed by transformation of the ester and the Boc-amino functions. It allows for easy diversification of the pyrazolo[1,5-a]pyrimidine scaffold at various positions. Molecular docking studies with pyrazolo[1,5-a]pyrimidine derivatives were also performed to elucidate the binding mode in the active site of cathepsin K. The synthesized compounds exhibited moderate inhibition activity (Ki ≥ 77 μM).
Pyrazolotriazines as inhibitors of nucleases
-
Paragraph 0122; 0123; 0124; 0125; 0126; 0127; 0164-0169, (2016/01/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
A convenient synthesis of 3- and 5-amino-1 H -pyrazoles via 3(5)-amino-4-(ethylsulfi nyl)-1 H -pyrazole desulfi nylation
Lassagne, Frederic,Snegaroff, Katia,Roisnel, Thierry,Nassar, Ekhlass,Mongin, Florence
, p. 139 - 145 (2011/12/01)
Syntheses of 5-amino-3-aryl- and 3-amino-5-aryl-1 H -pyrazoles from β -bromo- α -(ethylsulfanyl)cinnamonitrile are described. The β -bromo- α -(ethylsulfanyl)cinnamonitriles were oxidized with H2O 2 to the corresponding β -bromo- α -