Literature DB >> 24262377

Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-yl]-ω-[3,4-dihydroisoquinolin-2(1H)-yl]alkanamides.

Alla Zablotskaya1, Izolda Segal, Athina Geronikaki, Tatiana Eremkina, Sergey Belyakov, Marina Petrova, Irina Shestakova, Liga Zvejniece, Vizma Nikolajeva.   

Abstract

A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)-yl]ethan/propanamide derivatives was synthesized and characterized by (1)H, (13)C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N-(1,3-benzothiazol-2-yl)-2-[3,4-dihydroisoquinolin-2(1H)-yl]ethanamide is reported to determine its conformational feature. The investigated compounds were found to be active in psychotropic in vivo, anti-inflammatory in vivo and cytotoxicity in vitro screening. They possess marked sedative action, reveal high anti-inflammatory activity, have selective cytotoxic effects and NO-induction ability concerning tumour cell lines. Some of the compounds synthesized demonstrate antimicrobial action. An attempt was made to correlate the biological results with their structural characteristics and physicochemical parameters. Some specific combinations of types of activities for the synthesized compounds have been revealed.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-inflammatory activity; Antimicrobial activity; Cytotoxicity; Psychotropic activity; Tetrahydroisoquinoline; Thiazole

Mesh:

Substances:

Year:  2013        PMID: 24262377     DOI: 10.1016/j.ejmech.2013.10.008

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Chitosan-MgO Nanocomposite: One Pot Preparation and Its Utility as an Ecofriendly Biocatalyst in the Synthesis of Thiazoles and [1,3,4]thiadiazoles.

Authors:  Sayed M Riyadh; Khaled D Khalil; Ateyatallah Aljuhani
Journal:  Nanomaterials (Basel)       Date:  2018-11-08       Impact factor: 5.076

2.  Synthesis, characterization and biological evaluation of Pd(ii), Cu(ii), Re(i) and 99mTc(i) thiazole-based complexes.

Authors:  Jelena M Mašković; Antonios Hatzidimitriou; Ana Damjanović; Tatjana P Stanojković; Srećko R Trifunović; Athina A Geronikaki; Dionysia Papagiannopoulou
Journal:  Medchemcomm       Date:  2018-04-13       Impact factor: 3.597

  2 in total

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