scholarly journals Protein binding of quinolonecarboxylic acids. II. Spectral changes on the interaction of cinoxacin, nalidixic acid and pipemidic acid with human and rat albumins.

1989 ◽  
Vol 37 (3) ◽  
pp. 746-752 ◽  
Author(s):  
Taro IZUMI ◽  
Takako NAGAYAMA ◽  
Takayasu KITAGAWA
Keyword(s):  
Protein Binding ◽  
Nalidixic Acid ◽  
Pipemidic Acid ◽  
Spectral Changes

scholarly journals Mycobacterium tuberculosis DNA Gyrase: Interaction with Quinolones and Correlation with Antimycobacterial Drug Activity

2004 ◽  
Vol 48 (4) ◽  
pp. 1281-1288 ◽  
Author(s):  
Alexandra Aubry ◽  
Xiao-Su Pan ◽  
L. Mark Fisher ◽  
Vincent Jarlier ◽  
Emmanuelle Cambau
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Nalidixic Acid ◽  
Dna Gyrase ◽  
Dna Supercoiling ◽  
Structural Features ◽  
Pipemidic Acid ◽  
Structure Activity ◽  
Nickel Chelate ◽  
Pbr322 Dna ◽  
Cleavage Complex

ABSTRACT Genome studies suggest that DNA gyrase is the sole type II topoisomerase and likely the unique target of quinolones in Mycobacterium tuberculosis. Despite the emerging importance of quinolones in the treatment of mycobacterial disease, the slow growth and high pathogenicity of M. tuberculosis have precluded direct purification of its gyrase and detailed analysis of quinolone action. To address these issues, we separately overexpressed the M. tuberculosis DNA gyrase GyrA and GyrB subunits as His-tagged proteins in Escherichia coli from pET plasmids carrying gyrA and gyrB genes. The soluble 97-kDa GyrA and 72-kDa GyrB subunits were purified by nickel chelate chromatography and shown to reconstitute an ATP-dependent DNA supercoiling activity. The drug concentration that inhibited DNA supercoiling by 50% (IC50) was measured for 22 different quinolones, and values ranged from 2 to 3 μg/ml (sparfloxacin, sitafloxacin, clinafloxacin, and gatifloxacin) to >1,000 μg/ml (pipemidic acid and nalidixic acid). By comparison, MICs measured against M. tuberculosis ranged from 0.12 μg/ml (for gatifloxacin) to 128 μg/ml (both pipemidic acid and nalidixic acid) and correlated well with the gyrase IC50s (R 2 = 0.9). Quinolones promoted gyrase-mediated cleavage of plasmid pBR322 DNA due to stabilization of the cleavage complex, which is thought to be the lethal lesion. Surprisingly, the measured concentrations of drug inducing 50% plasmid linearization correlated less well with the MICs (R 2 = 0.7). These findings suggest that the DNA supercoiling inhibition assay may be a useful screening test in identifying quinolones with promising activity against M. tuberculosis. The quinolone structure-activity relationship demonstrated here shows that C-8, the C-7 ring, the C-6 fluorine, and the N-1 cyclopropyl substituents are desirable structural features in targeting M. tuberculosis gyrase.

scholarly journals Monitoring of Foreign Drug Safety Information

2019 ◽  
Vol 7 (4) ◽  
pp. 221-226
Author(s):  
Editorial Article
Keyword(s):  
Nalidixic Acid ◽  
Drug Safety ◽  
Safety Profile ◽  
Safety Information ◽  
Expert Evaluation ◽  
Medicinal Products ◽  
Pipemidic Acid ◽  
Direct Acting Antiviral ◽  
Direct Acting ◽  
Drug Safety Information

Analysis of administrative decisions of foreign regulatory authorities on the recoil of medicines and/or the need for changes in the instructions for their medical use due to changes in the safety profile, conducted by experts of the Scientific Centre for Expert Evaluation of Medicinal Products revealed 23 administrative decisions. These decisions contained information on the following medicines registered in Russia: аmitriptyline, duloxetine, quetiapine, lamotrigine, topiramate, phenytoin, articaine, epinephrine, bupivacaine, oxybutynin, dexlansoprazole, pantoprazole, esomeprazole, famotidine, ketoconazole, minocycline, quinolone and fluoroquinolone (cinoxacin, ciprofloxacin, flumequine, levofloxacin, lomefloxacin, moxifloxacin, nalidixic acid, norfloxacin, ofloxacin, pefloxacin, pipemidic acid, prulifloxacin and rufloxacin), antiretrovirals (abacavir, abacavir, dolutegravir, lamivudine, zidovudine, atazanavir, cobicistat, emtricitabine, tenofovir, darunavir, didanosine, rilpivirine, efavirenz, enfuvirtide, etravirine, fosamprenavir, indinavir, lopinavir, ritonavir, maraviroc, raltegravir, rilpivirine, nevirapine, saquinavir, tipranavir), direct-acting antiviral drugs (daclatasvir, dasabuvir, elbasvir, grazoprevir, glecaprevir, pibrentasvir, sofosbuvir, ombitasvir, ritonavir). 

DNA and protein binding, double-strand DNA cleavage and cytotoxicity of mixed ligand copper(II) complexes of the antibacterial drug nalidixic acid

2017 ◽  
Vol 174 ◽  
pp. 1-13 ◽  
Author(s):  
Rangasamy Loganathan ◽  
Mani Ganeshpandian ◽  
Nattamai S.P. Bhuvanesh ◽  
Mallayan Palaniandavar ◽  
Amsaveni Muruganantham ◽  
...  
Keyword(s):  
Protein Binding ◽  
Nalidixic Acid ◽  
Dna Cleavage ◽  
Mixed Ligand ◽  
Antibacterial Drug ◽  
Double Strand Dna

scholarly journals Comparative activities of ciprofloxacin (Bay o 9867), norfloxacin, pipemidic acid, and nalidixic acid.

1983 ◽  
Vol 24 (2) ◽  
pp. 302-304 ◽  
Author(s):  
H L Muytjens ◽  
J van der Ros-van de Repe ◽  
G van Veldhuizen
Keyword(s):  
Nalidixic Acid ◽  
Pipemidic Acid

Analytical methods for the determination of some selected 4-quinolone antibacterials

2017 ◽  
Vol 36 (2) ◽  
Author(s):  
Fathallah Belal ◽  
Nahed El-Enany ◽  
Mary E.K. Wahba
Keyword(s):  
Nalidixic Acid ◽  
Analytical Methods ◽  
First Generation ◽  
Second Generation ◽  
Oxolinic Acid ◽  
Pipemidic Acid ◽  
Comprehensive Review ◽  
Piromidic Acid

AbstractA comprehensive review with 337 references for the analysis of some selected 4-quinolone drugs belonging to the first and second generations since 2006 up till now is presented. This group includes nalidixic acid, oxolinic acid, piromidic acid, pipemidic acid and rosoxacin from the first generation and enoxacin, fleroxacin, nadifloxacin, pefloxacin and rufloxacin from the second generation. The review covers most of the methods described for the analysis of these drugs, either

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