Sixteen 7-substituted gatifloxacin derivatives were synthesized and evaluated for antimycobacterial activity in vitro and in vivo against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB), and also tested for the ability to inhibit the supercoiling activity...

A novel cysteic acid modified carbon paste electrode (cysteic acid/CPE) based on electrochemical oxidation of l-cysteine was developed to simultaneously determine ofloxacin and gatifloxacin in the presence of sodium dodecyl benzene sulfonate (SDBS). Fourier transform infrared spectra (FTIR) indi...

Quantitative determination of gatifloxacin in tablets, solid lipid nanoparticles (SLNs) and eye-drops using a very simple and rapid chromatographic technique was validated and developed. Formulations were analyzed using a reverse phase SUPELCO® 516 C-18-DB, 50306-U, HPLC column (250 mm × 4.6 mm...

Generic and additional names: GatifloxacinCAS name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acidCAS registry #: 112811-59-3Molecular formula: C19H22FN3O4Molecular weight: 375.39Intellectual property rights: Kyorin Pharmaceutical Co.Bran...

The copper(II) complexes with the third-generation quinolone gatifloxacin (Hgati) were prepared in the absence or presence of the N,N′-donor heterocyclic ligands 2,2′-bipyridylamine (bipyam), 1,10-phenanthroline (phen) or 2,2′-bipyridine (bipy) and were characterized physicochemically and spe...

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin® for the treatment of resp...

A highly accurate and precise spectrofluorimetric method was established for quantitation of Gatifloxacin in pure material, pharmaceutical formulations and in the existence of its oxidative degradation product. The emission was recorded at 487 nm after the excitation at 290 nm. Using micelle, so...

The optical and swelling properties of gatifloxacin-loaded contact lens decrease owing to the precipitation of gatifloxacin (on hydration) in the matrix structure of the contact lens. This paper focuses on the use of Pluronic F68 both inside and outside (in the packaging solution) the contact le...

In this study, a series of novel HDAC inhibitors, using 1,2,4-oxadiazole-containing as the cap group, were synthesized and evaluated in vitro. Compound 14b, N-hydroxy-2-(methyl((3-(1-(4-methylbenzyl)piperidin-4-yl)-1,2,4-oxadiazol-5-yl)methyl)amino)pyrimidine-5-carboxamide, displayed the most po...

Plant–derived smoke – butenolide, called at present karrikin 1 (KAR1) is known as an important inductor of seed germination and seedling growth. In this study, tricyclic butenolides were synthesized and their effects on germination of dormant and non–dormant Avena fatua caryopses were compare...

Molecular analysis of the KAR1 gene of yeast has shown that it is required for both mitosis and conjugation. The gene was originally identified by mutations that prevent nuclear fusion. By in vitro mutagenesis and gene replacement we have demonstrated that the gene is an essential cell division ...

Calmodulin (CaM) is a universal regulator for a huge number of proteins in all eukaryotic cells. Best known is its function as a calcium-dependent modulator of the activity of enzymes, such as protein kinases and phosphatases, as well as other signaling proteins including membrane receptors, cha...

This chapter covers those bicyclic 5–5 systems with one ring junction nitrogen atom and one extra heteroatom. There are nine possible parent structures that are presented in this chapter, in which the double bonds can be arranged in different ways to give 22 basic structures. Reduced derivative...

The unsymmetrical 1,3-diketones 1 on reaction with malononitrile is resulted an interesting trifunctional intermediates 2 and 3. The intermediate 2 is hydrolyzed to give 2,6-dicarboxamido aniline 4 which on cyclisation gave two regioisomers of 1,2-dihydro-4(3H)-quinazolinones 5 and 6. The effect...

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between the histone substrate binding sites in or...

3,6-Dimethyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one 3 was prepared by an intramolecular cyclization of N-(4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl) acetamide 2 in ethanol in the presence of piperidine. N-allylation and N-propargyl alkylation of N-substituted pyrazolo[3,4-d] pyrimidin-4(...

Optically active 2-benzoyl-3,4-dimethyl-5-phenyl-1,3-oxazolidines, obtained by the reaction of l-ephedrine with phenylglyoxal, after keeping without solvent undergo a spontaneous stereospecific rearrangement to 4,5-dimethyl-3,6-diphenylmorpholin-2-one.

A number of 2-aminothiazoles (2a–e) and their amide derivatives (4–10) were prepared. The 2-aminothiazoles themselves were tested as allosteric enhancers of agonist binding to human adenosine A1 receptors. In a variety of experimental set-ups the compounds did not show any such effect, in cont...

The structure-activity relationship of atrial natriuretic polypeptides (ANPs) in the central action was investigated by examining the suppressive effects of the intracerebroventricular (i.c.v.) administration of ANPs on water intake induced by the i.c.v. injection of angiotensin II (AII) (0.1 nm...

The backbone dynamics of the 28 residue 15N-labelled human atrial natriuretic peptide have been examined by 15N NMR methods. 15N R1,R2 and {1H}–15N NOE values were determined for the oxidised and reduced forms of the peptide (ANPox and ANPrd, respectively), and analysed using reduced spectral d...