Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT(1A) receptor and the serotonin transporter

Autor:	Zhongqi Shen, Geoffrey Hornby, Boyd L. Harrison, Nicole T. Hatzenbuhler, P. Siva Ramamoorthy, Deborah L. Smith, Wayne E. Childers, Kelly Sullivan, Michael Chlenov, Terrance H. Andree, Deborah Ann Evrard, Lee E. Schechter
Rok vydání:	2009
Předmět:	Tertiary amine Lactams Stereochemistry Clinical Biochemistry Pharmaceutical Science Serotonin 5-HT1 Receptor Antagonists Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Drug Discovery polycyclic compounds Cyclic AMP Structure–activity relationship Chromans Molecular Biology Serotonin transporter 5-HT receptor Serotonin Plasma Membrane Transport Proteins biology Organic Chemistry Transporter chemistry Drug Design Receptor Serotonin 5-HT1A biology.protein Lactam Molecular Medicine 5-HT1A receptor Selective Serotonin Reuptake Inhibitors
Zdroj:	Bioorganicmedicinal chemistry letters. 20(1)
ISSN:	1464-3405
Popis:	The structure–activity relationship (SAR) for three series of lactam-fused chroman derivatives possessing 3-amino substituents was evaluated. Many compounds exhibited affinities for both the 5-HT1A receptor and the 5-HT transporter. Compounds 45 and 53 demonstrated 5-HT1A antagonist activities in the in vitro cAMP turnover model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ffa3584c6f3a796ecb00de280080731 https://pubmed.ncbi.nlm.nih.gov/19932965 Zobrazit plný text záznamu Full Text from ScienceDirect