Literature DB >> 16087333

8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity.

Jamie M Singer1, Bridget M Barr, Linda L Coughenour, Tracy F Gregory, Michael A Walters.   

Abstract

Several new, potent dopamine subtype 2 (DA D(2)) active compounds with serotonin subtype 2A (5-HT(2A)) pharmacology are presented. 8-Substituted 3,4-dihydroquinolinones, tetrahydroquinolines, and N-acyl tetrahydroquinolines were evaluated in primary assays. Subtle changes on this novel scaffold translated to large changes in potency and selectivity in vitro. These compounds show promise as novel atypical antipsychotics for the treatment of schizophrenia.

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Year:  2005        PMID： 16087333     DOI： 10.1016/j.bmcl.2005.06.097

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


  4 in total

1.  Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.

Authors:  Jailall Ramnauth; Joanne Speed; Shawn P Maddaford; Peter Dove; Subhash C Annedi; Paul Renton; Suman Rakhit; John Andrews; Sarah Silverman; Gabriela Mladenova; Salvatore Zinghini; Sheela Nair; Concettina Catalano; David K H Lee; Milena De Felice; Frank Porreca
Journal:  J Med Chem       Date:  2011-07-08       Impact factor: 7.446

2.  Crystal structure of 1-benzyl-sulfonyl-1,2,3,4-tetra-hydro-quinoline.

Authors:  S Jeyaseelan; B R Sowmya; G Venkateshappa; P Raghavendra Kumar; B S Palakshamurthy
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-03-21

3.  α-Lithiation and electrophilic substitution of 1,4,4-trimethyl-3,4-dihydroquinolin-2-one.

Authors:  Bouclé Sébastien; Guillard Jérôme; Viaud-Massuard Marie-Claude
Journal:  Molecules       Date:  2010-10-29       Impact factor: 4.411

4.  Crystal structure of 1-tosyl-1,2,3,4-tetra-hydro-quinoline.

Authors:  S Jeyaseelan; K V Asha; G Venkateshappa; P Raghavendrakumar; B S Palakshamurthy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-10-24
  4 in total

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