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At least 235 records · Page 13Linked to original sources
PubMed1987

Pyridonecarboxylic acids as antibacterial agents. 9. Synthesis and antibacterial activity of 1-substituted 6-fluoro-1,4-dihydro-4-oxo-7-(4-pyridyl)-1,8-naphthyridine-3- carboxylic acids.

The title compounds (7a-e) with ethyl, 2-fluoroethyl, 2-hydroxyethyl, vinyl, or cyclopropyl groups, respectively, at C-1 were prepared by the method involving the Balz-Schiemann reaction of 2-(4-pyridyl)pyridine- and 7-(4-pyridyl)-1,8-naphthyridinediazonium tetrafluoroborates (15 and 27). The 1-ethyl, 1-(2-fluoroethyl), and 1-vinyl derivatives showed in vitro activities as potent as the corresponding 7-(1-piperazinyl) analogues against Staphylococcus aureus 209P JC-1 and Escherichia coli NIHJ JC-2 but were less active against Pseudomonas aeruginosa 12. Among the 7-(4-pyridyl) derivatives having the different C-1 substituent, 1-cyclopropyl derivative 7e was found to be the most active. In vivo efficacy of 7e was superior to that of enoxacin against experimental infections due to S. aureus 50774. Some aspects of structure-activity relationships associated with the C-1, C-6, and C-7 substituents were discussed.

Animals↗
PubMed2003

2-nitroso-1,3-diphenyl-1,2,3,4-tetrahydrobenzo[b][1,6]naphthyridine.

The title compound, C(24)H(19)N(3)O, crystallizes in the centrosymmetric space group P2(1)/a with one molecule in the asymmetric unit. The tetrahydropyridine ring has a boat conformation. The dihedral angle between the fused pyridine rings is 16.2 (1) degrees. The equatorial and axial orientations of the two phenyl groups with respect to the tetrahydropyridine ring are confirmed. The nitroso group is coplanar with the attached C-N-C group. The interplanar angle formed between the fused tetrahydropyridine and benzene planes is 13.4 (1) degrees. The crystal packing is stabilized by an intermolecular C-H.O hydrogen bond, which forms a C(9) graph-set chain running along the [001] direction.

Crystallography, X-Ray↗
PubMed2005

4,5,6,8,9-Pentachloropyrimido[1,2-a][1,8]naphthyridin-10-one.

The title compound, C11H2Cl5N3O, crystallizes in the monoclinic system with two molecules in the asymmetric unit. The molecules are chemically identical but have different structural parameters. In the three-dimensional packing, the molecules are arranged in dimers that are connected by slipped pi-pi stacking, and these dimers are connected to one another through several C-H...O and Cl...Cl interactions.

Crystallography, X-Ray↗
PubMed2005

In vitro activities of novel 2-fluoro-naphthyridine-containing ketolides.

In vitro activities of erythromycin A, telithromycin, and two investigational ketolides, JNJ-17155437 and JNJ-17155528, were evaluated against clinical bacterial strains, including selected common respiratory tract pathogens. Against 46 macrolide-susceptible and -resistant Streptococcus pneumoniae strains, the MIC(90) (MIC at which 90% of the isolates tested were inhibited) of the investigational ketolides was 0.25 microg/ml, twofold lower than that of telithromycin and at least 64-fold lower than that of erythromycin A. Against erm(B)-containing pneumococci, the MIC(90) of all the ketolides was 0.06 microg/ml. The MIC(90) of the investigational ketolides against mef(A)-containing pneumococci or pneumococci with both mef(A) and erm(B) was 0.25 microg/ml, two-and fourfold lower, respectively, than that of telithromycin. In contrast, the MICs of the investigational ketolides against macrolide-resistant S. pneumoniae strains with ribosomal mutations were similar to or, in some cases, as much as eightfold higher than those of telithromycin. Against Haemophilus influenzae, MICs of all the ketolides were < or =2 microg/ml. Against three Moraxella catarrhalis isolates, the MIC of the ketolides was 0.25 microg/ml. The ketolides inhibited in vitro protein synthesis, with 50% inhibitory concentrations ranging from 0.23 to 0.27 microM. In time-kill studies against macrolide-susceptible and erm- or mef-containing pneumococci, the ketolides were bacteriostatic to slowly bactericidal, with 24-h log(10) decreases ranging from 2.0 to 4.1 CFU. Intervals of postantibiotic effects for the ketolides against macrolide-susceptible and -resistant S. pneumoniae were 3.0 to 8.1 h.

Anti-Bacterial Agents↗