Vicentini, C. B. published the artcilePotential of pyrazolooxadiazinone derivatives as serine protease inhibitors, Recommanded Product: Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, the publication is Journal of Enzyme Inhibition (2001), 16(1), 15-34, database is CAplus and MEDLINE.
As a part of an investigation on mol. hybrids as new serine protease inhibitors, the pyrazolo [4,3-c][1,2,5]oxadiazin-3(5H)-one ring system was selected as a model of potential mechanism-based inhibitors. Due to the inherent reactivity of this system an optimal balance between susceptibility to nucleophilic attack and stability in solvents was sought prior to development as therapeutic agents. Substitutions on N5 and C7 of the supporting pyrazole ring with either aliphatic or aromatic groups and the replacement of the carbonyl oxygen on the reactive oxadiazinone ring with sulfur were explored. Two members of this class of inhibitors displayed time-dependent inhibition of human leukocyte elastase (HLE) suggesting mechanism-based inhibition. The observation that HLE generated a product(s) which displayed an identical UV-Visible spectrum to that observed during non-enzymic hydrolysis further supports this proposal. FlexX-based docking of these compounds into a model of HLE active site produced a mol. model of the inhibitor-enzyme interaction.
Journal of Enzyme Inhibition published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C11H13N3, Recommanded Product: Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics