One-pot three-component synthesis of peptidomimics for investigation of antibacterial and antineoplastic properties

AbstractThe α-hydroxyphosphonate generated from dialkyl phosphites and 1-phenyl-1H-pyrazole-4-carbaldehyde derivative was, in situ, trapped by isothiocyanates, isocyanates or acetic anhydride to produce dialkyl phosphorylmethyl-carbamothioates, -carbamates and/or -methyl acetates in good yields. The reactions were carried out in tetrahydrofuran (THF) in one step at room temperature, using K2CO3 catalyst. Antimicrobial and antineoplastic activities of the synthesized compounds were estimated. The results showed that all new compounds cause moderate to good antibiotic activities. However, phosphorylmethylcarbamothioates exhibited the highest growth inhibition. Furthermore, selected nine new synthesized compounds were evaluated for anticancer activity against eight human tumor cell lines (MCF7, MDA-MB-435, BT-549, IGROVI, SK-OV-3, PX-3, PU-145, and HEPG2). The majority of these compounds revealed moderate to potent activity against MCF7, PU-145, and HEPG2. Among them, two of the phosphorylmethylcarbamothioates showed excellent broad spectrum of anticancer activity with IC50 values ranging from 16.6 to 26.9 and 17.2 to 36.9μmolL−1, respectively (for 5-fluorouracil IC50: 17.7 to 38.8μmolL−1). Phosphorylmethyl methylcarbamothioate, in particular was more potent than 5-fluorouracil against all tested human carcinoma cell lines

Performance of privatised and private firms : empirical evidence from Egypt

Privatisation has been a major political and economic phenomenon over the past few decades, and researchers continue to target it for both theoretical and empirical work. The objective of this thesis is to evaluate the Egyptian experiment concerning its privatisation programme, and to determine whether this programme has affected the performance of privatised firms. Using 15 years of data, which cover the period 1990/1991 to 2004/2005; this thesis empirically investigates three main issues. Firstly, it examines whether the performance of privatised firms improves following privatisation through comparing pre- and postprivatisation performance in terms of profitability, operating efficiency, output, leverage and level of employment. Secondly, it evaluates the performance changes of privatised Egyptian firms after matching them to control firms (private firms) based on size and industry. Thirdly, it evaluates the impact of the post-privatisation sectoral environment and the pre-privatisation experience on post-privatisation performance. For the first two issues, several statistical techniques, such as parametric t-test, the non-parametric Wilcoxon signed-rank test, and Mann-Whitney test are performed. The results from this analysis indicate clearly that there are significant increases in both profitability and operating efficiency as well as significant declines in the leverage and employment, but there is no significant change in the output. Furthermore, the results show a significant difference in performance changes between privatised firms and private firms according to most performance measures. As to the third issue, several multi-regressions are used to model the relationship between the post-privatisation performance (as dependent variable) and ownership structure, the performance experience of the privatised firms pre-privatisation, the performance of their counterparts from competitor firms (private firms), and firm size (as independent variables). The results from this analysis demonstrate that the ownership structure really matters and that the performance of privatised firms depends on the degree of state ownership involvement; also, through the passage of time, the competitive environment has a significant impact on most performance measures of privatised firms. As such, this thesis represents the first study in Egypt to evaluate and compare the performance of privatised firms with the performance of their counterparts from private firms. The study contributes to the work on privatisation by comparing the performance changes of privatised firms to those of already private ones, so that the study can determine whether the post-privatisation performance matches that of the private firms. A caveat to the finding of this thesis is that the privatised firms might need a longer period to reflect more fully the impact of the privatisation programme on some of their performance measures.Arab Academy for Science and Technology, Egyp

BIOCHEMICAL STUDIES ON THE ISOLATED FRACTIONS OF DIFFERENT VARIETIES OF RICE

Rice is the staple food of the people of the world food grain. Besides bean the main source of calories and proteins, rice is an important cereal because it has the highest digestibility, biological value and protein efficiency ratio among all the cereals (KAUL et al. 1973). Although rice is an important food in mid and upper Egypt, the isolated fractions of grain rice cultivated in Egypt need to be fully investigated. The objective of the present work was to study the proximate analysis, mineral content, lipids and the amino acid content of some varieties of rice and its isolated fractions

Emergency general surgery: impact of distance and rurality on mortality

Funding This work was made possible by a grant from NHS Grampian and NHS Highlands Endowment Funding. No funding was received from the National Institutes of Health (NIH); Wellcome Trust; or Howard Hughes Medical Institute (HHMI). Acknowledgements The authors acknowledge the support of the eDRIS Team (Public Health Scotland) for their involvement in obtaining approvals, provisioning, and linking data, and the use of the secure analytical platform within the National Safe Haven. We also acknowledge P. Murchie for support with contextualizing the work within the rural medical practitioner literature.Peer reviewedPublisher PD

Comprehensive assessment of the management of acute cholecystitis in Scotland : population-wide cohort study

Funding The study was funded by an NHS Grampian endowment fund (NER 11062). © The Author(s) 2023. Published by Oxford University Press on behalf of BJS Society Ltd. Elements of this paper were presented as an oral presentation at the Surgical Research Society in Nottingham, UK on 25 March 2023. Data from this paper have also been presented in the Moynihan prize presentation section of the Association of Surgeons of Great Britain and Ireland, Harrogate, UK on 18 May 2023Peer reviewedPublisher PD

Earliest signs and management of leakage after bariatric surgeries: Single institute experience

Background: The aim of this study was to describe the clinical presentation and outcomes of treatment in patients who develop gastrointestinal leaks after different bariatric surgeries.Methods: Retrospective review of 632 consecutive bariatric surgical procedures performed from 1999–2009 in Alexandria University Hospital, Egypt.Results: Leakage occurred in 10 patients. Symptoms and signs included tachycardia, fever, tachypnea, left shoulder pain, abdominal pain, chest pain, and/or change in the nature of the drain effluent. The earliest signs of presentation were tachycardia and unilateral decrease in air entry in all patients. The average time to diagnosis was 3.9± 2.6 days. In four patients contrast study was negative (40%). Six leaks occurred after laparoscopic sleeve gastrectomy (6.3%), 2 after laparoscopic gastric bypass (3.6%), one after open gastric bypass (2.3%), and 1 after laparoscopic vertical banded gastroplasty (2.4%). The most common leak location was at the esophagogastric junction (70%). Four patients (40%) required reoperations. A percutaneous abdominal drainage was placed in five patients (50%). In 2 patients (20%), the prophylactic drain was maintained in situ till cessation of leakage. Two patients (20%) died. Mean hospital length of stay was 13.9 ± 7.8 days.Conclusions: Tachycardia and unequal breath sound in the early postoperative course are worrisome signs that warrant laparoscopic exploration even if contrast studies were negative. Patients with signs of sepsis or hemodynamic instability require emergent exploration. Leaks that are more insidious may be treated successfully with percutaneous drainage or maintenance of prophylactic drains.Keywords: Morbid obesity; Bariatric surgery; Complication; Lea

Meta‐analysis of laparoscopic transcystic versus transcholedochal common bile duct exploration for choledocholithiasis

Peer reviewedPublisher PD

Causes of death after emergency general surgical admission : population cohort study of mortality

Funding: This study was funded by the NHS Highland Endowments fund.Peer reviewedPublisher PD

Intermolecular interactions of 3,5-bis(4-Methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide in a cocrystal with 1,3-bis(4-Methoxyphenyl)prop-2-en-1-one and dimethylformamide solvate

Two new multicomponent crystals consisting of 3,5-bis(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (1) with 1,3-bis(4-methoxyphenyl)prop-2-en-1-one (2) and with dimethylformamide (DMF), both in 1:1 ratio, prepared and structurally characterized. The occurrence of 1 in different crystal structures enabled a comparison of hydrogen bonding contacts between the two structures as well as with the known structure of pure 1. The backbone of molecule 1 was similar in the structures but the orientation of the methoxy groups varied. Molecule 1 was involved in various combinations of the possible hydrogen bonding contacts, including N–H…O=C, N–H…OMe, and N–H…S. Both N–H hydrogens in the cocrystal (1–2) and the solvate (1-DMF) participated in hydrogen bonding but only one hydrogen atom took part in the structure of pure 1. The S atom accepted contacts in both the structures of pure 1 and cocrystal 1–2 but not in that of the 1-DMF solvate. The oxygen atoms of both methoxy groups acted as acceptors in the structure of pure 1, whereas one oxygen was involved in the 1-DMF solvate and none in cocrystal 1–2

(Z)-2-(1-(5-Methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethylidene)-N-phenylhydrazine-1-carbothioamide

Reaction of equimolar equivalents of 1-(5-methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethan-1-one (1) and N-phenylhydrazinecarbothioamide (2) in boiling ethanol containing a catalytic amount of concentrated hydrochloric acid for 4 h gave (Z)-2-(1-(5-methyl-1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl)ethylidene)-N-phenylhydrazine-1-carbothioamide (3) with 88% yield. The structure of 3 was established using single-crystal X-ray diffraction and magnetic resonance spectroscopy