title: Synthesis of novel coumarin appended bis(formylpyrazole) derivatives: Studies on their antimicrobial and antioxidant activities.
abstract: A series of novel coumarin pyrazole hybrids of biological interest were synthesized from the hydrazones, carbazones and thiocarbazones via Vilsmeier Haack formylation reaction. These intermediates and formyl pyrazoles were evaluated for antimicrobial and antioxidant activities. Among the series, compounds 6g and 6h showed excellent antimicrobial activity against different bacterial and fungal strains and compounds 7g, 7h were found to be potent antioxidant agents in both DPPH and hydroxyl radical scavenging assays. Further, detailed quantitative structure-activity relationship (QSAR) analysis indicated the molecular parameters that contribute to increased potency of inhibition. The above findings would further encourage our understanding in employing coumarin pyrazole hybrids as potential antibiotic agents for treating infections caused by pathogenic microbes and fungi. Further, it also paves the way for exploration of these compounds as potential therapeutic agents to treat conditions arising because of excessive oxidative damage.
authors.affiliation: Department of Chemistry, Yuvaraja College, University of Mysore, Mysore, India.
authors.forename: Renuka
authors.initials: R
authors.lastname: Nagamallu
authors.affiliation: Center for the Study of Systems Biology, School of Biology, Georgia Institute of Technology, 950, Atlantic Drive, Atlanta, GA 30332, USA.
authors.forename: Bharath
authors.initials: B
authors.lastname: Srinivasan
authors.affiliation: Transplant Surgery Section, Rangos Research Center, University of Pittsburgh, PA 15201, USA.
authors.forename: Mylarappa B
authors.initials: MB
authors.lastname: Ningappa
authors.affiliation: Department of Chemistry, Yuvaraja College, University of Mysore, Mysore, India.
authors.forename: Ajay Kumar
authors.initials: AK
authors.lastname: Kariyappa
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D009181:Mycoses / Q000188:drug therapy; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D000975:Antioxidants; D003374:Coumarins; D011720:Pyrazoles; C030123:coumarin
keywords: Antimicrobial; Antioxidant; Coumarin; DPPH; Hydroxyl radical; MIC; Pyrazole