title: Copper(II) triflate promoted multicomponent catalytic clubbing of piperazinyl-thiazoloquinolines and thiazolocoumarins as antimicrobials.
abstract: Step economical, multicomponent construction of two series based on quinoline and coumarin ring systems was carried out. Annulation towards the 2-piperazinylthiazole system was established in satisfactory yields, using copper(II) triflate. These multicomponent reaction products were examined for their potential inhibitory effect against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus), three Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae) and two fungal species (Aspergillus niger and Candida albicans). In vitro pharmacological screening data demonstrated that the majority of the compounds were found to possess a significant broad-spectrum antimicrobial (25-50 µg/mL of MIC) potential and the results were comparable to control drugs. The structural assignments of final products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy, and elemental analysis. The structure-activity relationship (SAR) was explored to facilitate further development of this class of compounds.
authors: Department of Applied Chemistry, S. V. National Institute of Technology, Surat, Gujarat, India. rahul.svnit11@gmail.com
authors: Rahul V
authors: RV
authors: Patel
authors: Jigar K
authors: JK
authors: Patel
authors: Shivraj H
authors: SH
authors: Nile
authors: Se Won
authors: SW
authors: Park
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001234:Aspergillus niger / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D002384:Catalysis; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008698:Mesylates / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D003374:Coumarins; D008698:Mesylates; D010879:Piperazines; D011804:Quinolines; D013844:Thiazoles; C548824:copper(I) triflate