Mueller, Stephan G. published the artcileDesign, synthesis and evaluation of MCH receptor 1 antagonists-Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414, HPLC of Formula: 39546-32-2, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(16), 3264-3269, database is CAplus and MEDLINE.
Despite recent approvals of antiobesity drugs there is still a high therapeutic need for alternative options with higher efficacy in humans. As part of the MCH-R1 antagonist program for the treatment of obesity, a series of biphenylacetamide HTS hits was evaluated. Several issues of the initial lead structures had to be resolved, such as potency, selectivity over related GPCRs and P-gp efflux limiting brain exposure in this series. The authors could demonstrate that all parameters can be significantly improved by structural modifications resulting in I as a potent and orally available MCH-R1 antagonist tool compound with acceptable in vivo efficacy in an animal model of obesity.
Bioorganic & Medicinal Chemistry Letters published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, HPLC of Formula: 39546-32-2.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem