thiourea and imidazole

Clinical use of non-steroidal anti-inflammatory drugs (NSAIDs) is associated with significant toxicity particularly in the gastrointestinal tract and kidney. Various approaches such as formulation co-administration (of agents to protect the stomach), chemical manipulation and synthesis of new safer anti-inflammatory drugs reported in the literature to overcome the toxicity of NSAIDs have been summarized. As far as synthesis of new more effective and safer anti-inflammatory drugs is concerned, we have reported recent findings in the area of synthesis of heterocyclic compounds such as pyrimidines, imidazole, benzimidazole, thiazole, thiazolidine, acridine, thiourea, alkanoic acid derivatives and other related heterocyclic compounds and their role as inflammation inhibitors.

Topics: Acridines; Alkanes; Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzimidazoles; Carboxylic Acids; Gastrointestinal Diseases; Heterocyclic Compounds; Humans; Imidazoles; Pyrimidines; Thiazoles; Thiourea

A series of novel propargylamine-modified pyrimidinylthiourea derivatives (1-3) were designed and synthesized as multifunctional agents for Alzheimer's disease (AD) therapy, and their potential was evaluated through various biological experiments. Among these derivatives, compound 1b displayed good selective inhibitory activity against AChE (vs BuChE, IC

Topics: Acetylcholinesterase; Alzheimer Disease; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors; Cognitive Dysfunction; Dose-Response Relationship, Drug; Drug Discovery; Humans; Imidazoles; Mice; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Pargyline; Propylamines; Pyrimidines; Rats; Scopolamine; Structure-Activity Relationship; Thiourea

The involvement of hydrogen peroxide (H2O2) generated by nicotinamide adenine dinucleotide phosphate-oxidase (NADPH oxidase) in the antioxidant defense system was assessed in salt-challenged Arabidopsis thaliana seedlings. In the wild-type, short-term salt exposure led to a transient and significant increase of H2O2 concentration, followed by a marked increase in catalase (CAT, EC 1.11.16), ascorbate peroxidase (APX, EC 1.11.1.11) and glutathione reductase (GR, EC 1.6.4.2) activities. Pre-treatment with either a chemical trap for H2O2 (dimethylthiourea) or two widely used NADPH oxidase inhibitors (imidazol and diphenylene iodonium) significantly decreased the above-mentioned enzyme activities under salinity. Double mutant atrbohd/f plants failed to induce the antioxidant response under the culture conditions. Under long-term salinity, the wild-type was more salt-tolerant than the mutant based on the plant biomass production. The better performance of the wild-type was related to a significantly higher photosynthetic activity, a more efficient K(+) selective uptake, and to the plants' ability to deal with the salt-induced oxidative stress as compared to atrbohd/f. Altogether, these data suggest that the early H2O2 generation by NADPH oxidase under salt stress could be the beginning of a reaction cascade that triggers the antioxidant response in A. thaliana in order to overcome the subsequent reactive oxygen species (ROS) production, thereby mitigating the salt stress-derived injuries.

Topics: Antioxidants; Arabidopsis; Arabidopsis Proteins; Ascorbate Peroxidases; Catalase; Fluoresceins; Gene Expression Regulation, Plant; Glutathione Reductase; Hydrogen Peroxide; Imidazoles; Malondialdehyde; Mutation; NADPH Oxidases; Onium Compounds; Sodium Chloride; Stress, Physiological; Thiourea; Time Factors

The effects of new and potent NOS inhibitors, S-methyl-L-thiocitrulline (S-Me-TC), 3-bromo 7-nitro indazole (3-Br-7-NI), and 1-(2-trifluoromethylphenyl) imidazole (TRIM), were examined on the pilocarpine-induced seizures in mice. 3-Br-7-NI and TRIM decreased the frequency of status epilepticus and mortality, while TRIM. In addition, significantly reduced the incidence of seizures. The latencies to onsets of seizures, status epilepticus, and mortality were significantly prolonged by all three NOS inhibitors, while duration of seizures was reduced by 3-Br-7-NI and TRIM. These data suggest an excitatory effect of NO in the neuronal structure involved in the pilocarpine-induced seizures.

Topics: Animals; Anticonvulsants; Citrulline; Disease Models, Animal; Enzyme Inhibitors; Imidazoles; Male; Mice; Nitric Oxide Synthase; Seizures; Thiourea