| Literature DB >> 26186150 |
Shivapura Viveka1, Prasanna Shama2, Gundibasappa Karikannar Nagaraja3, Shuvankar Ballav4, Savita Kerkar4.
Abstract
In the present study, an efficient synthesis of some new substituted pyrazoline derivatives linked to a substituted pyrazole scaffold was performed by a multistep reaction sequences and compounds were screened for their anti-inflammatory, analgesic and antibacterial activities. The preliminary results revealed that the N-acylated (5e, 5h) and nitro substituted N-phenyl (6f) pyrazolyl-pyrazolines derivatives exhibited a very promising anti-inflammatory activity whereas 5h, 6f were interesting analgesic agents. The compounds with halo substituted phenyl group at C-3 of the pyrazoline ring (4a, 5g, 5h, 6a and 6b) were found to be active against clinical bacterial pathogens with MIC in the range of 0.2-0.4 mg/mL. Compound containing N-propionyl pyrazolyl-pyrazoline (5h) could be identified as the most active member within this study with a dual anti-inflammatory and antibacterial profile. Taken together, this study has led to the development of promising compounds.Entities:
Keywords: Anti-inflammatory activity; Antibacterial activity; Drug design; Pyrazolyl-pyrazolines
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Year: 2015 PMID: 26186150 DOI: 10.1016/j.ejmech.2015.07.002
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514