SYNTHESIS, CHARACTERIZATION AND ANTI-INFLAMMATORY ACTIVITY OF NOVEL PYRAZOLE DERIVATIVES
Objectives: To synthesize novel pyrazole derivatives and their evaluation for anti-inflammatory activity.
Methods: The synthesis of chalcone (1) was carried out by using Claisen-Schmidt condensation. which on further cyclization with thiosemicarbazide
gives the substituted 3, 5-diphenyl-4, 5-dihydro-pyrazole-1-carbothoic acid amide (2), further reaction with different aldehydes yield title compounds
(3). Using this scheme 8 compounds were synthesized which further have been evaluated for anti-inflammatory activity by egg-albumin induced paw
Results: All the synthesized compounds have been supported by spectral analysis. The anti-inflammatory activity of synthesized compounds was
compared with standard anti-inflammatory agent Diclofenac sodium.
Conclusion: Compound-8, compound-2 and compound-3 showed greater anti-inflammatory activity due to the presence of alkene and electron
withdrawing groups (Cl and NO
Keywords: Chalcone, Thiosemicarbazide, Pyrazole derivatives, Anti-inflammatory activity.
2. Abdel-Rahman, et al., â€œSynthesis and antimicrobial of some chalcones and their derived pyrazoles, pyrazolines, isoxzolines and 5, 6-dihydropyrimidine-2-(1H)-thionesâ€, Monatsh. Chem., vol-138, 2007, pp 889â€“897.
3. Sharshira, et al., â€œSynthesis and in vitro antimicrobial activity of some pyrazolyl-1- carboxamide derivativesâ€, Molecules, vol-16, 2011, pp7736â€“7745.
4. Rashad, et al., â€œSynthesis of some biologically active pyrazoles and C-nucleosidesâ€, Acta Chim. Slov., vol-52, 2005, pp 429â€“434.
5. Rashad, et al., â€œSynthesis and antiviral evaluation of some new pyrazole and fused pyrazolopyrimidine derivativesâ€, Bioorganic Medicinal Chemistry, vol-16, 2008, pp 7102â€“7106.
6. Bhat, et al., â€œSynthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agentâ€, Journal of Medicinal Chemistry, vol-15, 2005, pp 3177â€“3180.
7. Michael, et al., â€œA new class of antimitotic agentsâ€, Journal of Medicinal Chemistry, vol-33, 1990, pp 1948â€“1954.
8. Vibhute, et al., â€œSynthesis and activities of a new series of chalcones as antibacterial agentsâ€, Indian Journal of Chemistry, Vol-42(B), 2003, pp202â€“205.
9. Clinton, et al., â€œSteroidal [3,2-c] pyrazoles, Journal of American Chemical Society, Vol-81, 1959, pp 1513â€“1514.
10. Kalirajan, et al., â€œSynthesis and biological evaluation of some heterocyclic derivatives chalconesâ€, Int. J. Chem. Sci., Vol-5, 2007, pp 73â€“80.
11. Urmila, et al., â€œSynthesis and antifungal activity of new fluorine containing 4-(substituted phenylazo) pyrazoles and isoxazolesâ€, Indian Journal of Heterocyclic Chemistry, Vol-14, 2005, pp 265â€“266.
12. Donald J., Ecobichon, The basic toxicology testing, CRC press, New York, 2nd edition, 1997, pp 43-86.
13. Roll R., et al., New Perspectives in Acute Toxicity Testing of Chemicals, Toxicol. Lett., Suppl., Vol-31, 1986, pp 86.
14. Trelle et al., "Cardiovascular safety of non-steroidal anti-inflammatory drugs: network meta-analysis", British Medical Journal (Clinical research ed.) 342, 11 January 2011.
15. "Anti-Inflammatory Foods to Choose from for Natural Healing", The Natural Anti-Inflammatory Remedies, December 20, 2012.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.