title: Synthesis and antibacterial activity of a novel series of 2,3-diaryl-substituted-imidazo(2,1-b)-benzothiazole derivatives.
abstract: Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1-b)-benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti-inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3-diaryl-substituted imidazo(2,1-b)-benzothiazoles 13a-o have been synthesized by reaction of substituted 2-aminobenzothiazoles 1-8 and an appropriately substituted alpha-bromo-1-(4''-substituted)-phenyl-2-(4'-substituted)-phenyl-1-ethanones 9-12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, (1)H-NMR, and Mass) data. All the synthesized compounds were screened for their in-vitro antibacterial activity against Gram-positive, Gram-negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d, 13h, and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials.
authors.affiliation: Department of Pharmaceutical Chemistry, K L E University's College of Pharmacy, Vidyanagar, Hubli, Karnataka, India. bpmahesh1@gmail.com
authors.forename: Mahesh
authors.initials: M
authors.lastname: Palkar
authors.forename: Malleshappa
authors.initials: M
authors.lastname: Noolvi
authors.forename: Ramappa
authors.initials: R
authors.lastname: Sankangoud
authors.forename: Veeresh
authors.initials: V
authors.lastname: Maddi
authors.forename: Andanappa
authors.initials: A
authors.lastname: Gadad
authors.forename: Laxmi Venkat G
authors.initials: LV
authors.lastname: Nargund
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure
chemical_list: D000900:Anti-Bacterial Agents; D052160:Benzothiazoles; D007093:Imidazoles