title: Design, synthesis and in vitro antimicrobial evaluation of novel Imidazo[1,2-a]pyridine and imidazo[2,1-b][1,3]benzothiazole motifs.
abstract: New antimicrobial agents, imidazo[1,2-a]pyridine and imidazo[2,1-b][1,3]benzothiazole, have been synthesized. Their antimicrobial activities were conducted against various Gram-positive, Gram-negative bacteria and fungi. Compounds 6c, 7a, 10b, 11a, 12b, 14a, 14b, 15a and 15b, exerted strong inhibition of the investigated bacterial and fungal strains compared to control antibiotics amoxicillin and cefixime and the antifungal agent fluconazole. Results from this study showed that the nature of the substituents on the armed aryl groups determines the extent of the activity of the fused imidazopyridine and/or imidazobenzothiazole derivatives. Preliminary structure-activity observations revealed that bromo-fluoro substituents enhanced the antimicrobial activity significantly compared to other substituents.
authors.affiliation: College of Pharmacy, University of Sharjah, P.O. Box 27272, Sharjah, United Arab Emirates. taltal@sharjah.ac.ae
authors.forename: Taleb H
authors.initials: TH
authors.lastname: Al-Tel
authors.forename: Raed A
authors.initials: RA
authors.lastname: Al-Qawasmeh
authors.forename: Rania
authors.initials: R
authors.lastname: Zaarour
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005658:Fungi / Q000187:drug effects*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D052160:Benzothiazoles; D007093:Imidazoles; D011725:Pyridines; C559797:imidazo(2,1-b)(1,3)benzothiazole; C001439:imidazo(1,2-a)pyridine