Pharmacological and Structure-Activity Relationship Evaluation of 4-aryl-1-Diphenylacetyl(thio)semicarbazides
Brak miniatury
Data
2014
Tytuł czasopisma
ISSN czasopisma
Tytuł tomu
Wydawca
Abstrakt
This article describes the synthesis of six 4-aryl-(thio)semicarbazides (series a and b) linked with diphenylacetyl moiety along with their pharmacological evaluation on the central nervous system in mice and computational studies, including conformational
analysis and electrostatic properties. All thiosemicarbazides (series b) were found to
exhibit strong antinociceptive activity in the behavioural model. Among them, compound
1-diphenylacetyl-4-(4-methylphenyl)thiosemicarbazide 1b was found to be the most potentan algesic agent, whose activity is connected with the opioid system. For compounds from series a significant anti-serotonergic effect, especially for compound 1-diphenylacetyl-4- (4-methoxyphenyl)semicarbazide 2b was observed. The computational studies strongly support the obtained results.
Opis
Słowa kluczowe
(thio)semicarbazides, conformational analysis, electrostatic properties, CNS activity, analgesic activity, serotonergic activity
Cytowanie
Molecules, Vol. 19, Issue 4, pages 4745-4759