Design, synthesis, in silico studies, and antidiabetic activity of several sulfanilamide incorporated 2,3-disubstitut-ed thiazolidin-4-ones

A panel of 2,3-disubstituted thiazolidin-4-ones 4a-n was synthesised from Schiff bases 3a-n derived from sulfanilamide, by reaction with thioglycolic acid. The compounds were characterised by means of IR, NMR, and Mass spectral data. Compounds 4a-n were screened for DPPH scavenging assay and compounds 4e, 4h, 4i, and 4n exhibited moderate activity. Compounds 4e, 4h, and 4i were tested at 200 mg/kg and 4e at 50 mg/kg b.w. orally for antidiabetic activity in fructose induced diabetic rats. They exhibited significant antidiabetic activity compared to the control group. Pioglitazone was used as a standard drug. The tested compounds exhibited better and ignificant serum cholesterol lowering activity when compared with the control and standard groups. They also reduced the triglyceride level after the 21st day; however, it was insignificant when compared to the control group. Compound 4n displayed the highest binding energy when docked with PPAR-γ followed by compounds 4e, 4h, and 4i when compared to pioglitazone. The physicochemical, drug likeness and ADME properties of the title compounds were found to be satisfactory.

Se sintetizó un panel de tiazolidinas-4-onas 2,3-disustituidas 4a-n a partir de las bases de Schiff 3a-n derivadas de la sulfanilamida por reacción con ácido tioglicólico. Los compuestos se caracterizaron por IR, RMN y datos espectrales de masa. Los compuestos 4a-n se analizaron para DPPH y los compuestos 4e, 4h, 4i y 4n mostraron una actividad moderada. Los compuestos 4e, 4h y 4i se probaron a 200 mg/kg y 4e a 50 mg/kg b.w. oralmente para la actividad antidiabética en ratas diabéticas, inducida por fructosa. Los compuestos mostraron una actividad antidiabética muy significativa en comparación con el grupo control. La pioglitazona se utilizó como fármaco estándar. Los compuestos ensayados mostraron una mejor y significativa actividad reductora del colesterol sérico en comparación con los grupos control y estándar. Estos compuestos también redujeron el nivel de triglicéridos después del 21° día, aunque fue insignificante en comparación con el grupo control. El compuesto 4n mostró la mayor afinidad de unión cuando se acopló a PPAR-γ, seguido de 4e, 4h y 4i en comparación con la pioglitazona. Las propiedades fisicoquímicas, la similitud con el fármaco y las propiedades ADME de los compuestos fueron satisfactorias, lo que los convierte en útiles agentes antidiabéticos.

Um painel de 2,3-disubstituído thiazolidina-4-ones 4a-n foram sintetizados a partir de bases Schiff 3a-n derivado da sulfanilamida por reacção com ácido tioglicólico. Os compostos eram caracterizado por IR, NMR e dados espectrais de massa. Os compostos 4a-n foram rastreados para O ensaio DPPH de limpeza radical e os compostos 4e, 4h, 4i e 4n exibiram actividade moderada. Os compostos 4e, 4h e 4i foram testados a 200 mg/kg e 4e a 50 mg/kg de peso corporal por via oral para antidiabéticos. actividade em ratos diabéticos induzidos por frutose. Exibiram uma actividade antidiabética altamente significativa actividade em comparação com o controlo. A pioglitazona foi utilizada como droga padrão. Os compostos testados exibiu uma melhor e significativa actividade de redução do colesterol sérico quando comparado comde triglicéridos após o 21° dia; no entanto, foi insignificante quando comparado com o controlo. O composto 4n mostrou a maior afinidade de ligação quando acoplado com PPAR-γ seguido de 4e, 4h, 4i quando comparado com pioglitazona. O propriedades físico-químicas, de semelhança com drogas e ADME dos compostos do título de propriedade também foram encontrados paraser satisfatórios, tornando-os agentes antidiabéticos úteis.

A Study on the Health and Nutritional Status of Bus Drivers in the Masan Area / 대한지역사회영양학회지

This study was carried out on 178 bus drivers in the Masan area to investigate their health and nutritional status. THe nutritional status of the subjects was surveyed using a self-administered questionnaire, and blood analyses were conducted through annual health examinations in June, 1999. The results were as follows: About 51% were classified as normal, 33% as health-concerned, and 17% as disease-suspected. The levels of total serum cholesterol were significantly higher in the over 20 year group (194.64 +/- 41.42 mg/dl) than in the under 10 year group (175.00 +/- 31.33 mg/dl) with respect to the length of their driving careers. Systolic blood pressure (SBP) was significantly higher in the 51 to 60 age group than in the other groups (p < 0.05). The total serum cholesterol increased with increasing age (p < 0.001), and SBP increased with increasing Body Mass Index (BMI)(p < 0.001). Diastolic blood pressure (DBP), total cholesterol (p < 0.01), hemoglobin (p < 0.05)and glutamate-pyruvate-aminotransferase (GPT)(p < 0.05) were significantly higher in the BMI of over 20, than in the BMI under 20. The GPT was significantly higher in the BMI over 25 than in the BMI under 25. In The mean daily energy intake was 1912.7 kcal (76.5% of the RDA) and the protein intake was 74.3 g (106.2% of the RDA). Compared with the recommended allowance, the energy, calcium, thiamin, and riboflavin intakes were below, and the Fe, vitamin A, vitamin C intakes were above the Korean RDA. The average carbohydrate, protein, fat ratio of energy intake was 66 : 15 : 19, respectively. The length of their driving careers had a positive correlation with their ages and total serum cholesterol levels, and their ages had a positive correlation with their blood pressures, total serum cholesterol and hemoglobin levels and BMI. Their BMI had a positive correlation with their ages, blood pressures, total serum cholesterol, hemoglobin, GPT and GOT levels. The results of this study indicate that bus drivers needed regular exercise, and control of their body weights to prevent chronic diseases, and that their health status should be monitored as the length of their driving careers and ages increase.

A study on the Values of Total Serum Cholesterol in Healthy Non-Pregnant and Pregnant Women / 예방의학회지

The author investigated the values of total serum cholesterol and its correlation with the physical factors to have potential as a line in the chain of basic investigation to establish maternal health program. The study group was composed of 167 healthy non-pregnant and 209 pregnant women in the age of 20-39 residing in Pusan area. The obtained results were as follows: 1. No significant differences were found in height and systolic and diastolic blood pressure in both groups except for the elevation of Broca's index by gaining the weight in pregnant women. 2. There were significant differences in the total serum cholesterol level of the healthy and pregnant women as 165.9 and 212.6 mg/dl, respectively, not showing the differences in the age. Total serum cholesterol values in both group followed approximately normal distrubution curve. 3. The significant correlation to the values of total serum cholesterol were found between weight and Broca's index in healthy women and between weight, Broca's index and duration of pregnancy in pregnant women. 4. The values of total serum cholesterol in pregnant women showed increasing tendency with the duration of pregnancy as 168.1 in 12 weeks and below, 209.6 mg/dl in 13-26 weeks and 235.4 mg/dl in 27 weeks and above group. Total serum cholesterol values by duration of pregnancy followed normal distribution curve.