Literature DB >> 18007421

New imide 5-HT1A receptor ligands - modification of terminal fragment geometry.

Andrzej J Bojarski1, Maria J Mokrosz, Beata Duszyńska, Aneta Kozioł, Ryszard Bugno.   

Abstract

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT(1A) and 5-HT(2A) receptors. All new derivatives from series a demonstrated high 5-HT(1A) affinities, whereas THIQ analogues were much less active. With respect to 5-HT(2A) receptors, three MPP derivatives presented moderate activity but the rest of the investigated compounds were practically inactive. The influence of changes in terminus geometry on 5-HT(1A) receptor affinity was analyzed in regard to model compounds NAN190and MM199.

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Year:  2004        PMID： 18007421      PMCID： PMC6147342          DOI： 10.3390/90300170

Source DB:  PubMed          Journal:  Molecules        ISSN： 1420-3049            Impact factor:   4.411


  16 in total

1.  1,2,3,4-tetrahydroisoquinoline derivatives: a new class of 5-HT1A receptor ligands.

Authors:  M J Mokrosz; A J Bojarski; B Duszyńska; E Tatarczyńska; A Kłodzińska; A Dereń-Wesołek; S Charakchieva-Minol; E Chojnacka-Wójcik
Journal:  Bioorg Med Chem       Date:  1999-02       Impact factor: 3.641

2.  On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT(1A) receptor antagonists.

Authors:  M H Paluchowska; M J Mokrosz; A Bojarski; A Wesołowska; J Borycz; S Charakchieva-Minol; E Chojnacka-Wójcik
Journal:  J Med Chem       Date:  1999-12-02       Impact factor: 7.446

3.  Structure-activity relationship studies of CNS agents. Part 16: A lower limit of a distance between crucial pharmacophores of 5-HT1A ligands.

Authors:  J L Mokrosz; M J Mokrosz; A J Bojarski; S Charakchieva-Minol
Journal:  Pharmazie       Date:  1994-10       Impact factor: 1.267

4.  8-[4-[2-(1,2,3,4-Tetrahydroisoquinolinyl]butyl-8-azaspiro[4.5]decane-7,9-dione: a new 5-HT1A receptor ligand with the same activity profile as buspirone.

Authors:  J L Mokrosz; A Dereń-Wesołek; E Tatarczyńska; B Duszyńska; A J Bojarski; M J Mokrosz; E Chojnacka-Wójcik
Journal:  J Med Chem       Date:  1996-03-01       Impact factor: 7.446

5.  Active conformation of some arylpiperazine postsynaptic 5-HT(1A) receptor antagonists.

Authors:  Maria Halina Paluchowska; Andrzej Jacek Bojarski; Sijka Charakchieva-Minol; Anna Wesołowska
Journal:  Eur J Med Chem       Date:  2002-04       Impact factor: 6.514

6.  N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.

Authors:  Anneke Hackling; Robin Ghosh; Sylvie Perachon; André Mann; Hans-Dieter Höltje; Camille G Wermuth; Jean-Charles Schwartz; Wolfgang Sippl; Pierre Sokoloff; Holger Stark
Journal:  J Med Chem       Date:  2003-08-28       Impact factor: 7.446

7.  Structure-activity relationship studies of CNS agents. Part 9: 5-HT1A and 5-HT2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines.

Authors:  A J Bojarski; M T Cegła; S Charakchieva-Minol; M J Mokrosz; M Maćkowiak; S Misztal; J L Mokrosz
Journal:  Pharmazie       Date:  1993-04       Impact factor: 1.267

8.  N-(phthalimidoalkyl) derivatives of serotonergic agents: a common interaction at 5-HT1A serotonin binding sites?

Authors:  R A Glennon; N A Naiman; M E Pierson; J D Smith; A M Ismaiel; M Titeler; R A Lyon
Journal:  J Med Chem       Date:  1989-08       Impact factor: 7.446

Review 9.  Buspirone. A preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic.

Authors:  K L Goa; A Ward
Journal:  Drugs       Date:  1986-08       Impact factor: 9.546

10.  NAN-190: an arylpiperazine analog that antagonizes the stimulus effects of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT).

Authors:  R A Glennon; N A Naiman; M E Pierson; M Titeler; R A Lyon; E Weisberg
Journal:  Eur J Pharmacol       Date:  1988-09-23       Impact factor: 4.432
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  3 in total

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Authors:  M Gertrude Gutierrez; Farzad Jalali-Yazdi; Justin Peruzzi; Carson T Riche; Richard W Roberts; Noah Malmstadt
Journal:  Small       Date:  2016-08-16       Impact factor: 13.281

2.  Synthesis and Biological Evaluation of New 3-Phenyl-1-[(4-arylpiperazin-1-yl)alkyl]-piperidine-2,6-diones.

Authors:  Anna Bielenica; Jerzy Kossakowski; Marta Struga; Izabela Dybała; Roberta Loddo; Cristina Ibba; Paolo La Colla
Journal:  Sci Pharm       Date:  2011-02-12

3.  Synthesis of new azo compounds based on N-(4-hydroxypheneyl)maleimide and N-(4-methylpheneyl)maleimide.

Authors:  Issam Ahmed Mohammed; Asniza Mustapha
Journal:  Molecules       Date:  2010-10-25       Impact factor: 4.411
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