Literature DB >> 11844685

A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: binding activity at D2 and D3 receptors.

Aloke K Dutta1, Xiang-Shu Fei, Maarten E A Reith.   

Abstract

A series of 7-hydroxy-2-[N-alkyl-(N-(4-phenylpiperazine)-alkyl)amino]tetralins was developed based on a novel hybrid approach that combined 2-aminotetralin and arylpiperazine pharmacophoric moieties. Our preliminary study revealed that a four-methylene butyl linker produced very potent compounds for both the D2 and D3 receptors. Further structure-activity studies led to a novel template showing 50- to 100-fold selectivity for the D3 receptor.

Entities:  

Mesh：

Substances：

Year:  2002        PMID： 11844685     DOI： 10.1016/s0960-894x(01)00820-4

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

Review 1.  Advances and challenges in the search for D2 and D3 dopamine receptor-selective compounds.

Authors:  Amy E Moritz; R Benjamin Free; David R Sibley
Journal:  Cell Signal       Date:  2017-07-14       Impact factor: 4.315

2.  Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.

Authors:  Dennis A Brown; Manoj Mishra; Suhong Zhang; Swati Biswas; Ingrid Parrington; Tamara Antonio; Maarten E A Reith; Aloke K Dutta
Journal:  Bioorg Med Chem       Date:  2009-04-19       Impact factor: 3.641

3.  Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding characterization at D2/D3 receptors and elucidation of a pharmacophore model.

Authors:  Dennis A Brown; Prashant S Kharkar; Ingrid Parrington; Maarten E A Reith; Aloke K Dutta
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

4.  Interaction of novel hybrid compounds with the D3 dopamine receptor: Site-directed mutagenesis and homology modeling studies.

Authors:  Sandhya Kortagere; Shu-Yuan Cheng; Tamara Antonio; Juan Zhen; Maarten E A Reith; Aloke K Dutta
Journal:  Biochem Pharmacol       Date:  2010-09-15       Impact factor: 5.858

5.  Concentration of receptor and ligand revisited in a modified receptor binding protocol for high-affinity radioligands: [3H]Spiperone binding to D2 and D3 dopamine receptors.

Authors:  Juan Zhen; Tamara Antonio; Aloke K Dutta; Maarten E A Reith
Journal:  J Neurosci Methods       Date:  2010-02-01       Impact factor: 2.390

6.  Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.

Authors:  Banibrata Das; Seenuvasan Vedachalam; Dan Luo; Tamara Antonio; Maarten E A Reith; Aloke K Dutta
Journal:  J Med Chem       Date:  2015-11-30       Impact factor: 7.446

7.  Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.

Authors:  Balaram Ghosh; Tamara Antonio; Juan Zhen; Prashant Kharkar; Maarten E A Reith; Aloke K Dutta
Journal:  J Med Chem       Date:  2010-02-11       Impact factor: 7.446

8.  (E)-2-Cyano-N'-(1,2,3,4-tetra-hydro-naphthalen-1-yl-idene)acetohydrazide.

Authors:  Mohamed A Al-Omar; Nagy M Khalifa; Hazem A Ghabbour; Tze Shyang Chia; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-05-16
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.