Fenflumizole (2-(2,4-difluorophenyl)-4,5-bis(4-methoxyphenyl) imidazole) was given to rats in a single oral dose of 30 mg/kg. The plasma concentration of fenflumizole reached a peak 2-3 hr after the dosing in non-fasted as well as fasted rats. Two metabolites (demethylation products) of fenflumizole were also detected in the plasma, but only in traces. Fenflumizole (30 and 100 mg/kg) and aspiri...

Susceptibility to Helicobacter pylori infection is a poorly understood phenomenon. This study was undertaken to establish whether either smoking or chronic non-steroidal anti-inflammatory drug (NSAID) consumption might in some way predispose to H. pylori infection and hence lead to peptic ulceration. Serological evidence of H. pylori infection was assessed in 100 consecutive subjects receiving ...

The effects of an intravenous infusion of nicotine at a dose of 2 . 5, 5 . 0, 7 . 5, or 10 . 0 micrograms kg-1h-1 on pentagastrin-stimulated gastric mucosal blood flow and acid secretion were investigated in eight healthy male non-smokers. Each dose was tested in two males. Gastric neutral red clearance served as a measure of mucosal blood flow. Nicotine reduced volume secretion, acid secretion...

The synthesis of some new 1,3,4-oxadiazole derivatives and 1,2,4-triazine-5-one has been described. IR, H NMR and mass spectral data support the structures of newly synthesized compounds. All the compounds have been tested in vivo for their anti-inflammatory activity by carrageenin-induced rat paw edema method. The compounds, which show good antiinflammatory activity, have been screened for the...

A series of pyrazolo[3,4-b]quinolines have been synthesized using one-pot water mediated synthetic route under microwave irradiation involving the condensation of 2-chloroquinoline-3-carbaldehydes with semicarbazide or 2,4-dinitrophenyl hydrazine. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. The pharmacological evaluation showe...

The new compound 1-(2-chloro-6-fluorophenyl)-5-methylindolin-2-one (1), designed using the prodrug approach, was easily obtained in 85% yield and characterized by nuclear magnetic resonance, elemental analysis, mass spectrometry and infrared spectroscopy. The lactam 1 showed anti-inflammatory and analgesic activity comparable to that of the COX-2 inhibitor lumiracoxib, without gastro-ulceration...

Novel, non-steroidal anti-inflammatory drug (NSAID), acetaminophen conjugates 6a–l with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates (6d, 6e, 6h, and 6k) exhibit more potent anti-inflammatory activity than their parent drugs, (b) the potent bis-conjugates show no visible stomach le...