Gatifloxacinacid
Gatifloxacinacid Basic information
- Product Name:
- Gatifloxacinacid
- Synonyms:
-
- Gatifloxacinacid
- 3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-, Monohydrochloride (9CI)
- 3-Quinolinecarboxylicacid,1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-,hydrochloride (1:1)
- BMS 206584-01 hydrochloride
- Gatifloxacin hydrochloride (AM 1155 hydrochloride
- PD 135432 hydrochloride)
- AM 1155 hydrochloride
- AM 1155 HYDROCHLORIDE;BMS 206584-01 HYDROCHLORIDE;PD 135432 HYDROCHLORIDE
- CAS:
- 121577-32-0
- MF:
- C19H22FN3O4.ClH
- MW:
- 411.859
- Mol File:
- 121577-32-0.mol
Gatifloxacinacid Chemical Properties
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- Soluble in DMSO
- form
- Powder
- color
- White to off-white
Gatifloxacinacid Usage And Synthesis
Uses
Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml)[1]. Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
Biological Activity
Gatifloxacin hydrochloride (AM-1155 hydrochloride) is a potent fluoroquinolone antibiotic with broad-spectrum antimicrobial activity.
in vivo
Gatifloxacin hydrochloride (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis .
< p>| Animal Model: | Female BALB/c mice with Nocardia brasiliensis in the right hind footpad |
| Dosage: | 100 mg/kg |
| Administration: | Subcutaneous injection; 3 times a day; 30 days |
| Result: | Reduced the production of lesions in mice. |
target
| Topoisomerase II 36.7 μM () |
IC 50
Quinolone; Topoisomerase II: 36.7 μM ()
References
[1] Takei M, et al. Inhibitory activities of Gatifloxacin hydrochloride (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.Antimicrob Agents Chemother.?1998 Oct;42(10):2678-81. DOI:10.1128/AAC.42.10.2678
[2] Fukuda H, et al. Antibacterial activity of Gatifloxacin hydrochloride (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother.?1998 Aug;42(8):1917-22. DOI:10.1128/AAC.42.8.1917
[3] Yamada C, et al. Gatifloxacin hydrochloride?acutely?stimulates?insulin?secretion?and?chronically?suppresses?insulin?biosynthesis. Eur J Pharmacol.?2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28. DOI:10.1016/j.ejphar.2006.09.043
[4] Daw-Garza A, et al. In?vivo?therapeutic?effect?of?Gatifloxacin mesylate?on?BALB/c?mice?infected?with?Nocardia?brasiliensis.Antimicrob Agents Chemother.?2008 Apr;52(4):1549-50. DOI:10.1128/AAC.00148-08
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