Abstract
ABSTRACT . A group of trisubstituted pyrazoles containing thiophen, 2-alkyloxypyridine and thieno[2,3- d ]pyrimidine heterocycles were synthesized in a study for possible analgesic agents. The desired products were obtained by reaction of 2-((1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1 H -pyrazol-4-yl)methylene)malononitrile with sulfur in presence of TEA, followed by treatment with different reagents. Newer products were examined for their analgesic properties, among them, analog 7 showed significant analgesic effects in comparison with reference medicines activity. KEY WORDS : Trisubstituted pyrazoles, Thiophene, Alkyloxypyridine, Fused pyrimidine, Analgesic activities Bull. Chem. Soc. Ethiop. 2019 , 33(3), 505-515. DOI: https://dx.doi.org/10.4314/bcse.v33i3.11
Highlights
Pyrazole compounds have an interesting therapeutic effect
In the continuing work on synthesis of biologically active heterocycles based pyrazoles [25-29], we focused in this study on designing of new molecules carrying pyrazole substituents as hybrids with various heterocycles aiming to get potent candidates with analgesic properties
The starting ylidenemalononitrile 1 treated in basic conditions with sulfur to provide 2-aminothiophene-3carbonitrile derivative 2
Summary
Pyrazole compounds have an interesting therapeutic effect. Due to the large amount of drugs including this heterocyclic compound, the pharmaceutical properties of the ring were the topic of medicinal studies. Acetic acid writhing test was achieved on mice and aspirin was used as a reference control. Synthesis of pyrazole-containing thiophene, 2-alkyloxy-pyridine and one more mg/kg) were used orally for treatment of mice of 1st group (control) and 2nd group (reference).
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