Synthesis and pharmacological activities of novel 1-alkyl-4-aryl-6-hydroxyperhydro-1,4-diazepine-2,3-diones

The present work involves the synthesis of 1-alkyl-4-aryl-6- hydroxyperhydro-1,4-diazepine-2,3-diones through the reaction of epichlorohydrin with some selected arylamine followed by the reaction of the formed intermediates with the corresponding -cyclohexyl, alkyl, or aralkyl amines. The resulting N,N disubstituted-1,3-diamino-2-propanols were cyclized with diethyl oxalate to afford the target compounds. The structures of the obtained compounds were verified by spectral and elemental methods of microanalysis. Fifteen of the final compounds were subjected to preliminary pharmacological screening as regards their anticonvulsant activity. In addition, evaluation of the hypotensive activity of twenty two compounds was performed. Most of the tested compounds gave 100% protection against pentylenetetrazole-induced convulsions with a faster onset of action [15 min] than diazepam [30 min]. On the other hand, most of the tested compounds gave mild to ~ 50-80% reduction in blood pressure in comparison to that of propranolol. Moreover, the cytotoxic activity of twenty eight final compounds was determined and only three of them elicited mild cytotoxic effects. Also, the median lethal dose [LD50] of four target representative compounds was determined and was found to range between 10-20 mg/kg [i.p.]

Efficacy and pathogenicity of three live infectious bursal disease vaccines [intermediate plus strains] in commercial native chickens breed in Egypt

In this study, three of live intermediate plus IBDV vaccines [A, B, and C] which are commonly used in Egypt were selected and their pathogenicity and efficacy were investigated. Groups of native breed chicks were vaccinated at 14 days of age with each vaccine by eye drop route and in drinking water then challenged with virulent field IBDV 14 days post vaccination [PV]. The efficacy and pathogenicity of each vaccine were evaluated based on clinical signs, mortalities, gross lesion, Bursa/ body weight ratio [BF/BW], and histopathological lesions of the bursa. It was found that these vaccines are efficient as they conferred 100% protection in all vaccinated and challenged groups compared with 20% mortality in unvaccinated challenged group. However, they did not prevent bursal atrophy or histological lesions. The bursal atrophy was observed at 7days PV in groups vaccinated with vaccine [A] while it was observed at 10 days PV in groups vaccinated with vaccines [B] and [C]. Vaccine [A] was proved to be more invasive compared with vaccines [B] and [C] as evidenced by higher bursal lesion scores and lower relative BF/BW ratios at certain intervals PV. When vaccine B and C were given in drinking water, moderate to severe bursal changes were observed. Meanwhile, when these vaccines [B and C] were given by eye drop route, mild to moderate changes in the bursa were observed indicating that vaccination by eye drop route would be better than in drinking water. It would be concluded that, all studied vaccines are efficacious and they vary in invasiveness and pathogenicity. Vaccines [B] and [C] are less pathogenic than vaccines [A] and the vaccination by eye drop route will result in less severe bursal lesions and better immune response than in drinking water

New 1, 4-disustituted-6-hydroxyperhydro-1,4-diazepine- 2,3-dione derivatives

A series of 1,4-disubstituted-6-hydroxyperhydro-1,4-diazepine-2,3-diones were designed and synthesized through the reaction of epichlorohydrin with an excess of the appropriate primary amine. The resulting secondary diamine derivatives were allowed to react with diethyl oxalate to afford the target compounds in good yields. Structures of the target compounds were verified on the basis of spectral and elemental methods of analysis. Twelve new derivatives were subjected to preliminary pharmacological screening regarding their CNS depressant activity such as sedative, hypnotic, anticonvulsant as well as muscle relaxant activities, in addition to evaluation of the hypotensive activity of some representative compounds. Most of the tested compounds gave high percentage reduction in spontaneous locomotor activity [SLA] compared with diazepam. Concerning the rota-rod coordination test, mice cannot remain on the rod more than 20 seconds in comparison with the reference drug used indicating a good muscle relaxant activity of the test compounds. Moreover, these compounds gave 100% protection against pentylenetetrazole-induced convulsions with a rapid onset of action. On the other hand, most of the test compounds gave mild to comparable reduction in blood pressure in comparison to that produced by using propranolol. Moreover, the acute toxicity [LD50] test was carried out for only one representative compound

Biomedical and hormonal aspects of apple vinegar

Apple vinegar was used for controlling body weight and high cholesterol level. Based on the data, the uptake of apple vinegar in two doses [5 ml each] daily by healthy control and hypercholesterolemic volunteers of varying ages, for five weeks led to a nonsignificant decrease in the body weight. A significant decrease in serum cholesterol level was observed only in middle aged hypercholesterolemic patients. Serum triglycerides level showed a nonsignificant decrease in all the studied subjects. There was a nonsignificant change in blood hemoglobin level in all subjects before and after treatment with apple vinegar. Apple vinegar could increase the serum insulin level significantly in hypercholesterolemic patients by increasing second-phase insulin secretion. Serum triiodothyronine [T3] revealed a significant increase after treatment with apple vinegar in both healthy control and hypercholesterolemic patients, while thyroxine [T4] showed a nonsignificant increase. In in vitro studies, apple vinegar showed a marked antibacterial action and some antifungal effects

Ultrasonic tissue characterization

Reflected ultrasonic single from soft tissue are examined to determine the acoustic parameters which discriminate between healthy and diseased tissues, and their temperature and frequency dependence. The velocity, the attenuation coefficient, and the slope of the acoustic attenuation with frequency in plexiglass, bovine liver, normal breast and cancer breast specimens are measured over a frequency range from 0.8-4 MHz. Human female breast is examined both histologically and acoustically. It is found that the attenuation in soft tissues is strongly dependent on the temperature and transducer's frequency. It is also found that the acoustic velocity does not vary strongly with frequency for plexiglas, bovine liver and normal breast specimens, however, it varies significantly for cancer breast specimens. Also, the acoustic velocity is found to be temperature dependent. Pathological tissues are found to have higher attenuation and velocity compared to that for normal breast tissues

Investigation of a model for estimating the attenuation of ultrasonic signals

mathematical model is developed to simulate attenuation of soft tissues. A comparison is done between the results of linear model [zero phase and minimum phase] and nonlinear model. The nonlinear minimum phase model is verified to be the best model for simulating the attenuation of ultrasound in soft tissues, as compared to the zero phase and the minimum phase linear models

Comparative phytochemical investigation of certain Melaleuca species grown in Egypt

Comparative TLC, PC and GLC analysis of the extracts of five Melaleuca species grown in Egypt viz. M. armillaris Sol.ex Gaerther, M. bracteata. F. Mne, M. elliptica Smith, M.quinquenervia Cav, and M. styphelloides Smith [Fam. Myrtaceae], revealed similarities in their phytoconstituents. TLC and GLC analysis of the unsaponifiable matter indicated that cholesterol, beta-sitosterol, stigmasterol and oleanolic acid are present in all species except, stigmasterol which could not be detected in M. armillaris while beta-amyrin was detected in M. armillaris leaf and stem. GLC analysis of the fatty acid methyl esters revealed high percentage of saturated fatty acids with palmitic acid as the main constituent. Flavonoids were studied using paper chromatography, while saponins were studied by TLC and their percentages were determined by the haemolytic index

Synthesis of some new furochromones

Khellin and visnagin are the principal furochromones of Ammi J/ visnaga L., kheilin has spasmolytic action on smooth muscle fibres particularly in renal and biliary colics. Visnagin which has one less methoxyl group-on C-9 hasn't the same success. This led us to attempt to introduce different groups into visnagin on C-9 with the hope to obtain other biologically active compounds