Chemistry is an experimental science, category: piperidines, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 27578-60-5, Name is N-(2-Aminoethyl)piperidine
A short, efficient, and highly stereoselective synthesis of a series of (3R,6R,7R)-2,5-diketopiperazine oxytocin antagonists and their pharmacokinetics in rat and dog is described. Prediction of the estimated human oral absorption (EHOA) using measured lipophilicity (CHI log D) and calculated size (cMR) has allowed us to rank various 2,5-diketopiperazine templates and enabled us to focus effort on those templates with the greatest chance of high bioavailability in humans. This rapidly led to the 2?,4?-difluorophenyl- dimethylamide 25 and the benzofuran 4 with high levels of potency (pK i) and good bioavailability in the rat and dog. Dimethylamide 25 is more potent (>20-fold) than 4 in vivo and has a high degree of selectivity toward the vasopressyi receptors, > 10000 for hV1a/hV1b and ?500 for hV2. It has a good Cyp450 profile with no time dependent inhibition and was negative in the genotoxicity screens with a satisfactory oral safety profile in rats.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. category: piperidines, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 27578-60-5, in my other articles.
Reference：
Piperidine – Wikipedia,
Piperidine | C5H4699N – PubChem