Conformation of gem-disubstituted alkylarylpiperidines and their implication in design and synthesis of a conformationally-rigidified NK1 antagonist

Autor:	Cheng Wang, Alexei V. Buevich, Dong Xiao, Robert G. Aslanian, Anandan Palani, Hon-Chung Tsui
Rok vydání:	2013
Předmět:	Chemistry Stereochemistry In vivo Organic Chemistry Drug Discovery Antagonist Context (language use) NK1 receptor antagonist Biochemistry Combinatorial chemistry
Zdroj:	Tetrahedron Letters. 54:6199-6203
ISSN:	0040-4039
DOI:	10.1016/j.tetlet.2013.08.131
Popis:	Piperidines are ubiquitous in pharmaceuticals and bioactive natural products. Understanding the structural and functional properties of piperidines plays a key role in drug design and development. This Letter reported studies of conformation of a set of gem -disubstituted methylphenylpiperidines in the context of discovery of NK 1 antagonists. The findings led to re-design and an efficient synthesis of a potent NK 1 antagonist with excellent in vivo activity and rodent and monkey pharmacokinetic profiles.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::bb48bc49a2cc24a35bc22cdfe75c76dc https://doi.org/10.1016/j.tetlet.2013.08.131 Zobrazit plný text záznamu Full Text from ScienceDirect