2023
DOI: 10.3390/ijms24020954
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Synthesis and Antibacterial Evaluation of Ciprofloxacin Congeners with Spirocyclic Amine Periphery

Abstract: The synthesis of novel fluoroquinolones, congeners of ciprofloxacin, which was inspired by earlier work on spirocyclic ciprofloxacin, is described. An antibacterial evaluation of the 11 fluoroquinolone compounds synthesized against the ESKAPE panel of pathogens in comparison with ciprofloxacin revealed that the more compact spirocycles in the fluoroquinolone periphery resulted in active compounds, while larger congeners gave compounds that displayed no activity at all. In the active cohort, the level of potenc… Show more

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Cited by 4 publications
(3 citation statements)
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“…Ciprofloxacin has 12 FDA-approved human uses and other veterinary uses, but it is often used for unapproved uses (off-label). Ciprofloxacin interacts with other drugs, herbal and natural supplements, and thyroid medications (Lukin et al, 2023). Ciprofloxacin is a broad-spectrum antibiotic active against both Gram-positive and Gram-negative bacteria.…”
Section: Discussionmentioning
confidence: 99%
“…Ciprofloxacin has 12 FDA-approved human uses and other veterinary uses, but it is often used for unapproved uses (off-label). Ciprofloxacin interacts with other drugs, herbal and natural supplements, and thyroid medications (Lukin et al, 2023). Ciprofloxacin is a broad-spectrum antibiotic active against both Gram-positive and Gram-negative bacteria.…”
Section: Discussionmentioning
confidence: 99%
“…Ciprofloxacin has 12 FDA-approved human uses and other veterinary uses, but it is often used for unapproved uses (off-label). Ciprofloxacin interacts with other drugs, herbal and natural supplements, and thyroid medications (Lukin et al, 2023).…”
Section: Advances Inmentioning
confidence: 99%
“…On the other hand, thiazole and thiadiazole derivatives constitute crucial frameworks in the realm of medicinal chemistry. An exploration of the literature highlights their significant role encompassing a diverse array of biological effects [44][45][46][47][48], notably including antimicrobial properties [49][50][51][52][53].…”
Section: Introductionmentioning
confidence: 99%