Next Article in Journal / Special Issue
Biaryl Product Formation from Cross-coupling in Palladiumcatalyzed Borylation of a Boc Protected Aminobromoquinoline Compound
Previous Article in Journal / Special Issue
Phenoxydifluoromethyl Substituted Nitrogen Heterocycles. Synthesis and Heterocyclization Reactions of Ethyl 4,4-Difluoro- 4-phenoxyacetoacetate
Molecules 2004, 9(3), 170-177; doi:10.3390/90300170
Article

New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry

* , , ,  and
Department of Medicinal Chemistry, Institute of Pharmacology of the Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland
* Author to whom correspondence should be addressed.
Received: 14 January 2004 / Accepted: 19 January 2004 / Published: 28 February 2004
(This article belongs to the Special Issue Biologically Relevant Heterocyclic Compounds)
View Full-Text   |   Download PDF [211 KB, uploaded 18 June 2014]   |  

Abstract

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moietiesderived from NAN190, were synthesized and evaluated in vitro for their ability to bind tothe serotonin 5-HT1A and 5-HT2A receptors. All new derivatives from series a demonstratedhigh 5-HT1A affinities, whereas THIQ analogues were much less active. With respect to5-HT2A receptors, three MPP derivatives presented moderate activity but the rest of theinvestigated compounds were practically inactive. The influence of changes in terminusgeometry on 5-HT1A receptor affinity was analyzed in regard to model compounds NAN190and MM199.
Keywords: 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives. 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives.
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
SciFeed

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
RIS
MDPI and ACS Style

Bojarski, A.J.; Mokrosz, M.J.; Duszyńska, B.; Kozioł, A.; Bugno, R. New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry. Molecules 2004, 9, 170-177.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert