Synthesis and Antinociceptive Activities of Some Pyrazoline Derivatives
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In the present study, some pyrazoline derivatives were synthesized to investigate their potential antinociceptive activities. 1-[(Benzoxazole/benzimidazole-2-yl)thioacetyl]pyrazoline derivatives were obtained by reacting 3,5-diaryl-1-(2-chloroacetyl)pyrazolines with 2-marcaptobenzoxazole/benzimidazole. The chemical structures of the compounds were elucidated by IR, (1)H NMR and FAB(+)-MS spectral data and Elemental Analyses. All of the compounds (100 mg/kg) exhibited significant antinociceptive activities in both hot plate and acetic acid-induced writhing tests. Naloxone (5 mg/kg) pre-treatment reversed the antinociceptive activities suggesting the involvement of opioid system in the analgesic actions. None of the compounds impaired motor coordination of animals when assessed in the Rota-Rod model. These results support the previous papers reporting the opioid sensitive antinociceptive activities of various benzoxazole/benzimidazole-pyrazoline derivative compounds.
Diverse Pharmacological Potential of different Substituted Pyrazole Derivatives.
Asif M, Almehmadi M, Alsaiari A, Allahyani M Curr Org Synth. 2023; 21(7):858-888.
PMID: 37861007 DOI: 10.2174/0115701794260444230925095804.
Dhonnar S, Jagdale B, Adole V, Sadgir N Mol Divers. 2022; 27(6):2441-2452.
PMID: 36367640 DOI: 10.1007/s11030-022-10562-x.
Yucel N, Osmaniye D, Kandemir U, Evren A, Can O, Ozkay U Molecules. 2021; 26(11).
PMID: 34199486 PMC: 8199615. DOI: 10.3390/molecules26113350.
Khanh L, Hanh Trinh Thi M, Quynh Bui Thi T, Vu Quoc T, Nguyen Thien V, Meervelt L Acta Crystallogr E Crystallogr Commun. 2019; 75(Pt 11):1590-1594.
PMID: 31709074 PMC: 6829711. DOI: 10.1107/S2056989019013379.
Higgs J, Wasowski C, Marcos A, Jukic M, Pavan C, Gobec S Heliyon. 2019; 5(3):e01376.
PMID: 30949609 PMC: 6430037. DOI: 10.1016/j.heliyon.2019.e01376.