title: Design and synthesis of some new pyrazolyl-pyrazolines as potential anti-inflammatory, analgesic and antibacterial agents.
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.
authors.affiliation: Department of Studies in Chemistry, Mangalore University, Mangalagangotri 574199, Karnataka, India.
authors.forename: Shivapura
authors.initials: S
authors.lastname: Viveka
authors.affiliation: Department of Studies in Chemistry, Mangalore University, Mangalagangotri 574199, Karnataka, India.
authors.lastname: Dinesha
authors.affiliation: Department of Pharmacology, N.G.S.M. Institute of Pharmaceutical Sciences, Paneer Deralakatte 574160, Karnataka, India.
authors.forename: Prasanna
authors.initials: P
authors.lastname: Shama
authors.affiliation: Department of Studies in Chemistry, Mangalore University, Mangalagangotri 574199, Karnataka, India. Electronic address: nagarajagk@gmail.com.
authors.forename: Gundibasappa Karikannar
authors.initials: GK
authors.lastname: Nagaraja
authors.affiliation: Department of Biotechnology, Goa University, Goa 403206, India.
authors.forename: Shuvankar
authors.initials: S
authors.lastname: Ballav
authors.affiliation: Department of Biotechnology, Goa University, Goa 403206, India.
authors.forename: Savita
authors.initials: S
authors.lastname: Kerkar
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002351:Carrageenan; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D011720:Pyrazoles; C031280:pyrazole; D002351:Carrageenan
keywords: Anti-inflammatory activity; Antibacterial activity; Drug design; Pyrazolyl-pyrazolines