Sameh M. El-Nabtity

Synthesis and Some Pharmacological Studies of New Benzenesulfonamide Derivatives

Summary. New benzenesulfonamide derivatives containing pyrazole and oxadiazole moieties were prepared starting from sodium saccharin. The structures of the novel compounds were characterized by elemental analyses and spectroscopic methods. The new compounds are structurally related to the COX-2 inhibitor celecoxib (Celebrex®). A pharmacological study of the pyrazoles revealed that several compounds possess higher analgesic and antiinflammatory activities than celecoxib, particularly 11 and 17. Most of the pyrazoles showed a significant increase in the sleeping time of thiopentone anaesthesized mice and also protected mice against the convulsive and lethal effects of pentylenetetrazole. Moreover, the ulcerogenic activity of those compounds showing a pronounced antiinflammatory effect was also studied.

Design, synthesis, anticonvulsant activity, and pharmacophore study of new 1,5-diaryl-1H-1,2,4-triazole-3-carboxamide derivatives

Abstract1,5-Diaryl-1H-1,2,4-triazole-3-carboxamide derivatives were designed, synthesized, and evaluated for its anticonvulsant activity using maximal electroshock (MES) and chemoshock (scPTZ and Strychnine) animal screen methods. Neurotoxicity was also assessed. In MES model, compound 4f showed 100% of phenytoin activity after both 0.5 and 4 h. In scPTZ model, compound 4e showed 100% of sodium valproate activity. In Strychnine model, compound 4e showed 120% more delay of onset of convulsion and 124% more delay of time of death relative to sodium valproate. Most of the target compounds showed mild neurotoxicity especially compound 4f which showed excellent activity against electroshock. Pharmacophoric study reveals that the synthesized compounds showed good fitting on the pharmacophoric query with good RMSDX results.

Effect of Florfenicol on Hematology, Cardiac Enzymes and its Residues in Broiler Chickens by HPLC

The current study was conducted on multiple oral doses (40 mg/kg for 3 successive days) of florfenicol (FF) to determine its effect on some hematological parameters, cardiac enzymes and its residues in blood and tissues (liver, muscles and kidneys) of broiler chickens. Seventy broiler chickens were used and divided into two groups, each consisted of 35 birds. The first group was left as a control, while the second was given FF for 3 successive days. The FF residues in tissues were determined using reversed phase-high performance liquid chromatography (RP-HPLC) with ultraviolet (UV) detector at 223 nm. Results indicated a widespread distribution of FF in most of the tested tissues. All tissue samples were considered FF free on the 9 th day after the last oral dose except liver. Florfenicol administration elicited a significant decrease in all blood parameters (hemoglobin concentration (Hb), red blood cell count (RBCs), mean corpuscular volume (MCV), mean corpuscular hemoglobin concentration (MCHC) and lymphocytes) from 1 st up to 7 th day except packed cell volume (PCV) which showed no significant change on 1 st day but decreased on 3 rd , 5 th and 7 th day after stopping medication. Moreover, monocytopenia was observed on the 5 th and 7 th day and white blood cells (WBCs) showed the same effect on the 5 th day, while heterophiles revealed highly elevation. All cardiac enzymes (aspartate aminotransferase (AST), lactate dehydrogenase (LDH), creatine kinase MB (CK-MB) and Troponin I) were highly elevated. In conclusion, broiler chicken meat can be consumed safely after 9 days post FF treatment.

Immunological and Biochemical Profiles of Tilmicosin in Rabbits

This study aimed to evaluate the effect of tilmicosin on rabbit immunity after daily subcutaneous (S.C) injection for 3 successive days. Fifteen New Zealand male rabbits were divided into 3 groups; the first group was left as a control, the second was non treated vaccinated against pasteurellosis (1 mL S.C in the skin fold of the back of the rabbit), while, the third was vaccinated and treated by tilmicosin in a dose of 10 mg/kg BW daily for 3 days. Whole blood and serum samples were collected from each rabbit on 1 st ,3 rd ,9 th ,14 th ,21 st and 28 th days post drug administration to determine some immunological and biochemical parameters. Histopathological examination of liver, kidneys and heart of all groups was also carried out. The results revealed that tilmicosin elicited a significant increase in B-lymphocytes, nitric oxide production by macrophages and lysozyme activity of the serum. Meanwhile, the drug had no significant changes on alanine aminotransferase enzyme (ALT) and aspartate aminotransferase enzyme (AST) levels (liver enzymes). On the 21 st day ALT showed significant decrease. Moreover; there were no significant changes on urea and creatinine levels (kidney functions) when compared with control group. Histopathological findings of the vaccinated and treated groups showed lesion score from 1 st and 2 nd degree. It could be concluded that tilmicosin afforded a good effect on rabbits’ immunity without negative effects on liver and kidney functions.

Synthesis and Biological Activities of 2-Carboxyphenyloxamoylamino Acids,their Salts with 2-ethoxy-6,9-Diaminoacridine and D-glucosamine

As a result of this work, 17 new compounds were obtained. This group of compounds (2-carboxyphenyloxamoylamino acids) alone or with biologically active base showed diverse biological activity-Anti-inflammatory, antimicrobial and hepatoprotective activity- which can be used in medicine after further investigations.