Tags

Type your tag names separated by a space and hit enter

In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives.
Chemotherapy. 2017; 62(3):194-198.C

Abstract

BACKGROUND

Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains.

METHODS

The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL.

RESULTS

MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones.

CONCLUSION

Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound.

Authors+Show Affiliations

Facultad de Ciencias Químicas, Universidad Autónoma de San Luis Potosí, San Luis Potosí, Mexico.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28334702

Citation

Leyva-Ramos, Socorro, et al. "In Vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives." Chemotherapy, vol. 62, no. 3, 2017, pp. 194-198.
Leyva-Ramos S, de Loera D, Cardoso-Ortiz J. In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives. Chemotherapy. 2017;62(3):194-198.
Leyva-Ramos, S., de Loera, D., & Cardoso-Ortiz, J. (2017). In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives. Chemotherapy, 62(3), 194-198. https://doi.org/10.1159/000456533
Leyva-Ramos S, de Loera D, Cardoso-Ortiz J. In Vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives. Chemotherapy. 2017;62(3):194-198. PubMed PMID: 28334702.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro Antibacterial Activity of 7-Substituted-6-Fluoroquinolone and 7-Substituted-6,8-Difluoroquinolone Derivatives. AU - Leyva-Ramos,Socorro, AU - de Loera,Denisse, AU - Cardoso-Ortiz,Jaime, Y1 - 2017/03/24/ PY - 2016/10/10/received PY - 2017/01/15/accepted PY - 2017/3/24/pubmed PY - 2017/6/1/medline PY - 2017/3/24/entrez SP - 194 EP - 198 JF - Chemotherapy JO - Chemotherapy VL - 62 IS - 3 N2 - BACKGROUND: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. METHODS: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. RESULTS: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. CONCLUSION: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound. SN - 1421-9794 UR - https://www.unboundmedicine.com/medline/citation/28334702/In_vitro_Antibacterial_Activity_of_7_Substituted_6_Fluoroquinolone_and_7_Substituted_68_Difluoroquinolone_Derivatives_ L2 - https://www.karger.com?DOI=10.1159/000456533 DB - PRIME DP - Unbound Medicine ER -