Structure-Activity Relationship Studies on 6-Chloro-1-phenylbenzazepines Leads to the Identification of a New Dopamine D1 Receptor Antagonist.


Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
11 Aug 2023
Historique:
received: 19 07 2023
revised: 30 07 2023
accepted: 31 07 2023
medline: 28 8 2023
pubmed: 26 8 2023
entrez: 26 8 2023
Statut: epublish

Résumé

The 1-phenylbenzazepine template has yielded a number of D1R-like ligands, which, though useful as pharmacological tools, have significant drawbacks in terms of selectivity versus D5R as well as pharmacokinetic behavior. A number of 1-phenylbenzazepines contain a 6-chloro functional group, but extensive SAR studies around the 6-chloro-1-phenylbenzazepine framework have not been reported in the literature. To further understand the tolerance of the 6-chloro-1-phenylbenzazepine template for various substituent groups towards affinity and selectivity at D1R, we synthesized two series of analogs with structural variations at the C-7, C-8,

Identifiants

pubmed: 37630262
pii: molecules28166010
doi: 10.3390/molecules28166010
pmc: PMC10458514
pii:
doi:

Substances chimiques

1-phenylbenzazepine 0
Receptors, Dopamine D1 0
Amides 0
Benzazepines 0
Dopamine Antagonists 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : National Institute of Health
ID : 1SC1DA049961

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Auteurs

Rajan Giri (R)

Department of Chemistry, Hunter College, City University of New York, 695 Park Avenue, New York, NY 10065, USA.
Program in Chemistry, CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.

Hari K Namballa (HK)

Department of Chemistry, Hunter College, City University of New York, 695 Park Avenue, New York, NY 10065, USA.

Vishwashiv Emogaje (V)

Department of Chemistry, Hunter College, City University of New York, 695 Park Avenue, New York, NY 10065, USA.

Wayne W Harding (WW)

Department of Chemistry, Hunter College, City University of New York, 695 Park Avenue, New York, NY 10065, USA.
Program in Chemistry, CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.
Program in Biochemistry, CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.

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Classifications MeSH