One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Recommanded Product: Methyl piperidine-4-carboxylate, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2971-79-1
Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2971-79-1, molcular formula is C7H13NO2, introducing its new discovery. Recommanded Product: Methyl piperidine-4-carboxylate
Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy
Lead compounds 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-benzamide (1), tetrahydro-pyran-4-carboxylic acid [((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-amide (2), and 3,5-dimethyl-isoxazole-4-carboxylic acid [((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-amide (3) discovered in our laboratory, displayed high histamine H3 receptor (H3R) affinity, good selectivity and weak human Ether–go-go-Related Gene (hERG) channel affinity with desirable overall physico-chemical and pharmacokinetic (PK) profiles. Herein, we describe the design and synthesis of a novel series of H3R antagonists utilizing a scaffold hopping strategy. Further structure-activity relationship (SAR) studies of the series culminated in the identification of ((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-naphthalene-2-carboxylic acid (tetrahydro-pyran-4-yl)-amide (4c) and -[4-((2S,3?S)-2-methyl-[1,3?]bipyrrolidinyl-1?-yl)-phenyl]-N-(tetrahydro-pyran-4-yl)-acetamide (4d), which exhibited good H3R affinity in vitro, good selectivity, and desirable PK properties. Compounds 4c and 4d were also assessed in cardiac safety experiments. In particular, the effects of the compounds on action potentials recorded from ventricular myocytes isolated from guinea pigs were used to screen compounds that not only displayed a low affinity towards hERG channel, but also had lower interference with other cardiac ion channels. Compound 4c did not alter the major parameters in this model system at ?10 muM, and no significant induction of any major haemodynamic effect when intravenously administered at 3 mg/kg dose to anaesthetized mongrel dogs. Compound 4c is a new promising lead as orally potent and selective H3R antagonist belonging to a distinct structural class.
One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Recommanded Product: Methyl piperidine-4-carboxylate, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2971-79-1
Reference£º
Piperidine – Wikipedia,
Piperidine | C5H8057N – PubChem