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Non‐steroidal anti‐inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity related with all routine NSAIDs. Replacing this functional group with the 1,3,4‐oxadiazole bioisostere is a generally used strategy to obtain an anti‐inflammatory agent devoid of GI side effects. In the present work, a novel group of 5‐(3,4‐dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one Mannich bases were synthesized and characterized on the basis of IR, 1H NMR, and elemental analysis results. The target compounds were first tested for cytotoxicity to determine a non‐toxic concentration for anti‐inflammatory screening. Anti‐inflammatory effects of the compounds were evaluated by in vitro lipopolysaccharide (LPS)‐induced NO production and in vivo carrageenan footpad edema with ulcerogenic profile. In LPS‐induced RAW 264.7 macrophages, most of the compounds showed inhibitory activity on nitrite production while compounds 5a, 5h, and 5j exhibited the best profiles by suppressing the NO production. To evaluate the in vivo anti‐inflammatory potency of the compounds, the inflammatory response was quantified by increment in paw size in the carrageenan footpad edema assay. The anti‐inflammatory data scoring showed that compounds 5a–d, 5g, and 5j, at the dose of 100 mg/kg, exhibited anti‐inflammatory activity, which for compound 5g was comparable to that of the reference drug indomethacin with 53.9% and 55.5% inhibition in 60 and 120 min, respectively.
A series of novel 1,3,4‐oxadiazole‐2‐one derivatives was synthesized by Mannich reaction of 5‐(3,4‐dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one and different substituted piperidines. The synthesized compounds were tested for their in vivo and in vitro anti‐inflammatory and ulcerogenic profiles. Preliminary pharmacological evaluation of the compounds showed that some of the compounds possess good to moderate anti‐inflammatory activity.
Abstract The single radial immunodiffusion assay has been the accepted method for determining the potency of inactivated influenza vaccines since 1978. The world‐wide adoption of this assay for vaccine standardisation was facilitated through collaborative studies that demonstrated a high ... mehr
Abstract Background Whether morbidity from the 1918‐19 influenza pandemic discriminated by socioeconomic status has remained a subject of debate for 100 years. In lack of data to study this issue recent literature have hypothesized that morbidity was “socially neutral”. Objectives ... mehr