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.

6533b835fe1ef96bd129ec20

RESEARCH PRODUCT

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.

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

subject

Models Molecular Antifungal Agents Stereochemistry medicine.drug_class Infrared spectroscopy Antineoplastic Agents Microbial Sensitivity Tests Carrageenan Crystallography X-Ray Anti-inflammatory chemistry.chemical_compound Mice Structure-Activity Relationship Seizures Cell Line Tumor Drug Discovery medicine Animals Edema Humans Benzothiazoles Thiazole Cytotoxicity Hypoxia Psychomotor Agitation Cell Proliferation Pharmacology Psychotropic Drugs Bacteria Dose-Response Relationship Drug Molecular Structure Tetrahydroisoquinoline Chemistry Physical Organic Chemistry Anti-Inflammatory Agents Non-Steroidal Fungi General Medicine Carbon-13 NMR Antimicrobial Isoquinolines Propanamide Anti-Bacterial Agents chemistry NIH 3T3 Cells Drug Screening Assays Antitumor Anesthesia Inhalation

description

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 1H, 13C 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.

year	journal	country	edition	language
2012-12-28	European journal of medicinal chemistry

10.1016/j.ejmech.2013.10.008 https://pubmed.ncbi.nlm.nih.gov/24262377