Application of 73874-95-0, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 73874-95-0, Name is tert-Butyl piperidin-4-ylcarbamate, molecular formula is C10H20N2O2. In a Article£¬once mentioned of 73874-95-0
Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y12 receptor
The present paper describes the development of a new series of P2Y 12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 muM, aq solubility <0.1 muM, microsomal CLint (HLM) ?300 muM/min/mg). By replacement of the urea functionality with a sulfonylurea group we observed increased affinity along with improved stability and solubility as exemplified by 47 (IC 50 binding affinity = 0.042 muM, aq solubility = 90 muM, microsomal CLint (HLM) = 70 muM/min/mg). Further improvements in affinity and metabolic stability were achieved by replacing the central piperazine ring with a 3-aminoazetidine as exemplified by 3 (IC50 binding affinity = 0.0062 muM, aq solubility = 83 muM, microsomal CLint (HLM) = 28 muM/min/mg). The improved affinity observed in the in vitro binding assay also translated to the potency observed in the WPA aggregation assay (47: 19 nM and 3: 9.5 nM) and the observed in vitro ADME properties translates to the in vivo PK properties observed in rat. In addition, we found that the chemical stability of the sulfonylureas during prolonged storage in solution was related to the sulfonyl urea linker and depended on the type of solvent and the substitution pattern of the sulfonyl urea functionality. Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application of 73874-95-0, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 73874-95-0, in my other articles.
Reference£º
Piperidine – Wikipedia,
Piperidine | C5H13727N – PubChem