Saccharine is a pharmacologically significant active scaffold for various biological activities, including antibacterial and anticancer activities. Herein, saccharinyl hydrazide (1) was synthesized and converted into 2-[(2Z)-2-(1,1-dioxo-1,2-dihydro-3H-1λ6,2- benzothiazole-3-ylidene) hydrazinyl] acetohydrazide (5), which was employed as a key precursor for synthesizing a novel series of small molecules bearing different moieties of monosaccharides, aldehydes, and anhydrides. Potent biological activities were found against Staphylococcus and Escherichia coli, and the results indicated that compounds 6c and 10a were the most active analogs with an inhibition zone diameter of 30–35 mm. In cell-based anticancer assay over Ovcar-3 and M-14 cell lines, compound 10a was the most potent analog with IC50 values of 7.64 ± 0.01 and 8.66 ± 0.01 µM, respectively. The Petra Orisis Molinspiration (POM) theoretical method was used to calculate the drug score of tested compounds and compare them with their experimental screening data. Theoretical DFT calculations were carried out in a gas phase in a set of B3LYP 6-311G (d,p). Molecular docking studies utilizing the MOE indicated the best binding mode with the highest energy interaction within the binding sites. The molecular docking for Ovcar-3 was carried out on the ovarian cancer protein (3W2S), while the molecular docking for M-14 melanoma was carried out on the melanoma cancer protein (2OPZ). The MD performed about 2ns simulations to validate selected compounds’ theoretical studies.
Aim: To evaluate our experience of radical treatment in management of liver hydatid cyst. As liver is considered the organ most frequently infected with hydatid disease. Methods: We performed a retrospective study concerning surgical management of liver hydatid cyst at Advanced Hepato-Pancreateco-Biliary Center. Our study done from June 2011 to May 2018 on 103 patients presented with hepatic hydatid cyst. Results: Total pericystectomy was carried out in 80 (77.67%) patients; while hepatic resection was carried out in 14 (13.59%) patients. Laparoscopic management was done in 6 (5.82%) patients (5 cases with total pericystectomy and 1 case with sub-total pericystectomy and omentoplasty). Twenty-one patients developed post-operative complications, four patients suffered from biliary leak. There was no mortality. Follow-up period ranged from 6 to 60 months with no recurrence. Conclusion: Radical surgical procedures were safe and effective in management of hepatic hydatid cyst when it was done by experienced surgeons, with lower morbidity rates and no recurrence.
Background:The liver is one of the most frequently damaged organs when abdominal trauma occurs. Currently, conservative management becomes the treatment of choice in hemodynamic stable patients.Aim: To evaluate the results of an operative and conservative management of liver injury patients.Patients and methods: From March 2011 to June 2015, 113 patients suffered from hepatic trauma were referred to Zagazig University hospital, trauma unit. The patients were classified according to the way of management: Group I, operative management; Group II, conservative management. Variables analyzed included demographic data, injury classification, associated lesions, surgical treatment, morbidity, mortality, and hospital stay.Results: 113 patients had hepatic trauma. 39 (34.5%) patients were managed nonoperatively. The commonest type of trauma was blunt and the main cause was motor vehicle in 59 (52.2%) patients. The second cause was stab injury with 33 (29.2%) patients. The least cause was gunshot injury in 21 (18.6%) patients. There was no significant difference in hospital stay between patients operated on and these managed non-operatively. There was no mortality in the patients managed conservatively.Conclusions: Conservative management is a safe approach for hemo-dynamically stable patients with liver trauma. Conservative management patients should be admitted to intensive care unit for at least 48-72 hours for close monitoring of vital signs repeated clinical examinations and follow up investigations as indicated. Failure of conservative treatment did not show a higher incidence of complications or mortality. Good results obtained from conservative management resulted from a highly cooperated trauma team including surgery, anethesia, intensive care, cardiothoracic and neurosurgery doctors.
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