Roussel Uclaf

About: Roussel Uclaf is a based out in . It is known for research contribution in the topics: Alkyl & Alkoxy group. The organization has 1888 authors who have published 2338 publications receiving 36508 citations.

Antibacterial activity of ofloxacin and other 4-quinolone derivatives: in-vitro and in-vivo comparison

Abstract: Ofloxacin (DL8280, RU43280) is a newly introduced oxazine quinolone derivative with broad and potent antibacterial activity. Ofloxacin showed excellent in-vitro activity against Enterobacteriaceae while most strains of Pseudomonas aeruginosa were inhibited by less than 2 mg/l. The compound was significantly more potent than norfloxacin against Acinetobacter spp. and Staphylococcus spp. Ofloxacin and norfloxacin behaved similarly with respect to inoculum size, effect of urine and serum, bactericidal properties and frequency of spontaneous resistant mutants. Ofloxacin displayed an in-vivo antibacterial activity up to five times greater than that of pefloxacin and norfloxacin, probably due to the conjunction of favourable pharmacokinetics, excellent bacterial susceptibility and good stability towards metabolic degradation.

2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivatives, process and intermediates for their preparation, their pharmaceutical use and compositions containing them

Abstract: The invention relates to the compounds of formula (I): … … in which:… - X and X', which may be identical or different, represent a hydrogen atom, a halogen atom or a cyano, NO2 or CF3 radical;… - R represents a hydrogen atom or an alkyl radical; and… - Ar represents an aryl radical, an aromatic heterocyclic radical or a heterocyclic radical fused to an aryl radical. … The compounds of formula (I) possess advantageous pharmacological properties which justify their use in therapy.

CoMFA validation of the superposition of six classes of compounds which block GABA receptors non-competitively.

Abstract: Thirty-six compounds, representing six different structural classes of insecticides which are known to act at the γ-aminobutyric acid receptor/chloride ionophore, have been superimposed by methods which maximise the commonality of steric and electrostatic fields. Maximal steric and electrostatic alignment was derived by pairwise comparisons of the different chemical classes with picrotoxinin. To test the validity of the combined superposition, a Comparative Molecular Field Analysis (CoMFA) was carried out within SYBYL, using recently published in vivo and in vitro binding data for insecticides. The resultant partial least-squares (PLS) analysis of sampled steric and electrostatic fields showed a significant statistical correlation with the published biological data. The predictive model obtained was shown to have a greater than 95% chance of significance.