Repozytorium
Wyszukaj
Kolekcje
Inne
Synthesis, analgesic activity and computational study of new isothiazolopyridines of Mannich base type.
Autorzy
Rok wydania
2005
Czasopismo
Numer woluminu
60
Strony
961-968
DOI
10.1016/j.farmac.2005.08.005
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
A series of new 4-arylpiperazine derivatives of isothiazolopyridine of Mannich base type and their non-4-arylpiperazine analogues (3 and 4) were synthesized and assayed as potential analgesic agents. Pharmacological assay demonstrated that all the compounds prepared, without exception, displayed significant activity in the mouse writhing assay. The analgesic action, expressed as ED50, was found to be 2-10 times more potent than that of acetylsalicylic acid and 1.5-10 times weaker than that of morphine, these being used as standards. The toxicities (LD50) of the investigated derivatives varied and ranged from 250 to 2000 mg/kg. Additionally, the computational investigations were performed in order to find correlation between molecular structure and biological effects (toxicity, analgesic action) of discussed compounds. Useful model was found for toxicity assessment.
Adres publiczny
http://dx.doi.org/10.1016/j.farmac.2005.08.005
Strona internetowa wydawcy
Podobne publikacje
New chiral Mannich adducts of di-tert-butylphenols and a bicyclic imine : synthesis and antiproliferative activity.
Iwanejko Jakub, Wojaczyńska Elżbieta, Trynda Justyna, Maciejewska Magdalena, Wietrzyk Joanna, Kochel Andrzej, Wojaczyński Jacek
Dimerization and solvent-assisted proton dislocation in the low-barrier hydrogen bond of a Mannich base: a low-temperature NMR study.
Rospenk Maria, Sobczyk Lucjan, Schah-Mohammedi P., Limbach Hans-Heinrich, Golubev N. S., Melikova S. M.
The ligand-to-metal energy transfer and the role of Lewis base ligands and silver plasmons in emission of new type of lanthanide phosphors.
Gawryszewska Paula, Amirkhanov Vladimir M., Trush Victor A., Kulesza Dagmara, Legendziewicz Janina
