Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Antidepressive Agents, Tricyclic
/ chemical synthesis
Crystallography, X-Ray
Dose-Response Relationship, Drug
Humans
Lactams
/ chemical synthesis
Models, Molecular
Molecular Structure
Receptors, Dopamine
/ metabolism
Receptors, Histamine
/ metabolism
Receptors, Serotonin
/ metabolism
Structure-Activity Relationship
5 HT receptors
D(2) receptor
Dibenzepine
H(1) receptor
SERT inhibitors
Tricyclic drugs
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 11 2020
01 11 2020
Historique:
received:
03
06
2020
revised:
23
07
2020
accepted:
09
08
2020
pubmed:
18
8
2020
medline:
23
6
2021
entrez:
18
8
2020
Statut:
ppublish
Résumé
A series of fourteen novel, eight-membered lactam- and dilactam-based analogues of tricyclic drugs were obtained in a simple one-pot procedure. Crystal structures of two compounds were determined by single-crystal X-ray diffraction analysis and their selected structural features were discussed and compared with those of imipramine and dibenzepine. Affinity of developed molecules for histamine receptor H
Identifiants
pubmed: 32798652
pii: S0960-894X(20)30604-1
doi: 10.1016/j.bmcl.2020.127493
pii:
doi:
Substances chimiques
Antidepressive Agents, Tricyclic
0
Lactams
0
Receptors, Dopamine
0
Receptors, Histamine
0
Receptors, Serotonin
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
127493Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.