Technetium-labeled danofloxacin complex as a model for infection imaging

AbstractDanofloxacin, a fluoroquinolone derivative antibiotic, was synthesized, successfully labeled with technetium-99m and formulated for the development of a potential diagnostic imaging agent of the bacterial infection and inflammation with higher efficiency than that of the commercially available 99mTc-ciprofloxacin. Factors affecting the labeling yield were optimized. The radiolabeled antibiotic was subjected to preclinical assessments such as purity, stability, and pharmacokinetic investigations in animals. The biodistribution studies indicated that the uptake of 99mTc-danofloxacin was high in the infectious lesion (T/NT=7.2±0.1) at 2h post injection. The abscess to normal ratio indicated that the danofloxacin tracer can be used for infection diagnosis. The radiolabeled compound was cleared quickly from most of the body organs. The results displayed that 99mTc-danofloxacin could not differentiate between infection and sterile inflammation

Role of magnetic resonance imaging in the evaluation of the popliteus musclotendinous injuries as a part of the posterolateral corner injuries of the knee

Introduction: The popliteus musclotendinous complex is considered to be one of the main stabilizers of the posterolateral corner of the knee having different attachments and variable sites of injuries, the use of MRI helps the radiologists to depict such injuries consistently.Purpose of the study: To study the role of MRI in evaluating the popliteus musclotendinous injuries as a part of the PLCof the knee.Patients and methods: Our study included 15 patients with trauma to the knee undergoing MRI using 1.5 T magnet using the following sequence: Axial, Coronal, sagittal proton density fat sat, T1, T2 and T2 gradient and conventional X-ray/CT [All patients did conventional X-ray Knee (AP and Lateral views), two patients did CT study of the knee].Results: Out of 15 studied patients with PLC injuries, eight (53.33%) patients had popliteus complex injuries, 7 (87.5%) patients showed combined injuries with other posterolateral structures while one (12.5) patient had isolated popliteus musclotendinous complex injury.Conclusion: MRI imaging is crucial in the evaluation of the different sites and patterns of injuries of the popliteus musclotendinous complex when suspecting PLC injury.Keywords: Popliteus muscle, Popliteus tendon, Posterolateral corner, Popliteofibular ligament, MR

Report on needs and priorities in the field of international cooperation agreements on water management in the target MACs

This report aims to provide a revision of the water related goals within the international agreements joined by the three case study countries,Egypt, Morocco and Tunisia, while emphasizing the critical points that should be developed and reinforced in the near future through an integrated approach for water policies, initiatives and management

Synthesis and antibacterial activity of 3-arylidene chromen-2, 4-dione derivatives

Abstract: Derivatives of 3-arylidene chromen-2, 4-dione 1 were synthesized to be used as a starting material for synthesizing some new fused heterocyclic compounds containing coumarin moiety. When compounds 1 reacted with hydrazine derivatives, hydroxylamine hydrochloride, urea, thiourea, semicarbazide and thiosemicarbazide it gave the corresponding compounds 2-5. Compound 4a, b reacted with methyl iodide in DMF and K2CO3 at room temperature to afford the corresponding 6a, b. All these compounds were screened InVitro for their antibacterial activity

Spectroscopic, thermodynamic, kinetic studies and oxidase/antioxidant biomimetic catalytic activities of tris(3,5-dimethylpyrazolyl)borate Cu(II) complexes

A series of copper(II) complexes, viz. [TpMeMeCu(Cl)(H2O)] (1), [TpMeMeCu(OAc)(H2O)] (2), [TpMeMeCu(NO3)] (3) and [TpMeMeCu(ClO4)] (4) containing tris(3,5-dimethylpyrazolyl)borate (KTpMeMe), have been synthesized and fully characterized. The substitution reaction of 1 with thiourea was studied under pseudo-first-order conditions as a function of concentration, temperature and pressure in methanol and acetonitrile as solvents. Two reaction steps that both depended on the nucleophile concentration were observed for both solvents. Substitution of coordinated methanol is about 40 times faster than the substitution of chloride. In acetonitrile, the rate constant for the displacement of coordinated acetonitrile was more than 20 times faster than the substitution of chloride. The reported activation parameters indicate that both reaction steps follow a dissociative mechanism in both solvents. On going from methanol to acetonitrile, the rate constant for the displacement of the solvent becomes more than 200 times faster due to the more labile acetonitrile, but the substitution mechanism remained to have a dissociative character. The antioxidant activities of 1–4 were evaluated for superoxide dismutase (SOD), glutathione-s-transferase (GST0 and glutathione reduced (GSH-Rd) activity. 1 and 2 were found to show (p < 0.05) the highest antioxidant activity in comparison to 3 and 4, which can be ascribed to the geometric configuration as well as the nature of the co-ligand. 1 showed catechol oxidase activity with turnover numbers of 20 min−1 and a coordination affinity for 3,5-DTBC of K1, = 31 mM−1. K1 is rather large and seems to be typical for faster biomimetic models, and also for the enzyme itself (25 mM−1). The reaction rate depended linearly on the complex concentration, indicating a first-order dependence on the catalyst concentration

Radioiodination and biodistribution of newly synthesized 3-benzyl-2-([3-methoxybenzyl]thio)benzo[g]quinazolin-4-(3H)-one in tumor bearing mice

3-Benzyl-2-((3-methoxybenzyl)thio)benzo[g]quinazolin-4(3H)-one was previously synthesized and proved by physicochemical analyses (HRMS, 1H and 13C NMR). The target compound was examined for its radioactivity and the results showed that benzo[g]quinazoline was successfully labeled with radioactive iodine using NBS via an electrophilic substitution reaction. The reaction parameters that affected the labeling yield such as concentration, pH and time were studied to optimize the labeling conditions. The radiochemical yield was 91.2 ± 1.22% and the in vitro studies showed that the target compound was stable for up to 24 h. The thyroid was among the other organs in which the uptake of 125I-benzoquinazoline has increased significantly over the time up to 4.1%. The tumor uptake was 6.95%. Radiochemical and metabolic stability of the benzoquinazoline in vivo/in vitro and biodistribution studies provide some insights about the requirements for developing more potent radiopharmaceutical for targeting the tumor cells. Keywords: Benzo[g]quinazoline, Radioiodination, Biodistribution, Tumor cell, NB

Synthesis, characterization and medical efficacy (hepatoprotective and antioxidative) of albendazole-based copper(II) complexes – an experimental and theoretical approach

<div><p>A series of albendazole-based copper(II) complexes with different counter anions, [Cu(Albz)(H₂O)₂](ClO₄)₂ (<b>1</b>), [Cu(Albz)₂(Cl)]Cl·2H₂O (<b>2</b>), [Cu(Albz<b>)</b>₂(NO₃)](NO₃) (<b>3</b>), and [Cu₂(Albz)₂(μ-SO₄)₂(H₂O)₂] (<b>4</b>) (Albz = albendazole), have been synthesized and characterized. Their structures and properties were characterized by elemental analysis, thermal analysis (TGA, DTG and DTA), IR, UV–vis and ESR spectroscopies, cyclic voltammetry, electrical molar conductivity, and magnetic moment measurements. A square-planar geometry is proposed for <b>1</b>, whereas the five-coordinate copper(II) complexes <b>2</b>, <b>3</b>, and <b>4</b> have a square pyramidal geometry. Theoretical calculations (DFT) using B3LYP/6–311 + G(d,p) level of theory corroborated the experimental results to investigate both the drug Albz and its copper(II) complex, <b>1</b>. The hepatoprotective and antioxidative efficacy of Albz and <b>1–4</b> were evaluated against carbon tetrachloride-induced acute hepatotoxicity in rats. Hepatotoxicity in experimental rats was evidenced by significant decrease in the antioxidant enzyme activities (SOD, GSH-S-transfers, and GSH-Rd levels). The results have strong impact for designing anticancer drugs, combined with their potential cytotoxic and antioxidant activities, which can be targeted selectively against cancer cells and increase their therapeutic index and advantages over other anticancer drugs. The DNA cleavage studies of Albz and its copper(II) complexes using genomic DNA indicated that Albz has no role in cleavage of DNA, and only <b>1</b> played a marked role in the DNA cleavage without any external additives.</p></div

Программа спецкурса для студентов 4 курса дневного и заочного форм обучений по спецкурсу "Конституционно-правовая ответственность в Республике Беларусь и зарубежных странах"

The Mediterranean region is characterized by increasing pressures over its natural resources and significant disparities among countries (UNEP/MAP, 2016). The region is considered as one of the most water scarce regions in the World with an average water availability below 1000m3 per capita for most of the countries located in the Southern and Eastern rims of the Mediterranean, and even below 500m3 in many of them (e.g. Algeria, Libya, Tunisia or Jordan). Growing population, irrigation expansion and urbanization are increasing pressures on water resources quantity and quality that will be likely exacerbated by political instability and climate change, reducing available water resources per capita and affecting socio-economic and environmental conditions. In light of this, a number of international initiatives are being developed to ensure sustainable development in the region and contribute to a sustainable management and use of water resources. In this context, the MADFORWATER project tries to address different water resources management issues that include the low availability and use of locally-adapted technologies for wastewater treatment and reuse for irrigation; a lack or inefficiency of economic and regulatory instruments to foster water saving irrigation technologies and practices and water reuse in agriculture; limited capacity building and social acceptance of treated wastewater reuse in agriculture; and, in essence, insufficiently integrated water management strategies. To respond to these challenges, the MADFORWATER project general objective is “to develop an integrated set of technological and management instruments for the enhancement of wastewater treatment, treated wastewater reuse for irrigation and water efficiency in agriculture, with the final aim to reduce water vulnerability in selected basins in Egypt, Morocco and Tunisia” (MADFORWATER Document of Action – part B – page 1).The selected basins, chosen due to their relevance and representativeness for the Mediterranean region in relation to population, GDP, wastewater, hydrology and geographical location, are all subjected to exacerbating water scarcity, and count on high potential to increase wastewater reuse (currently 7% used), (MADFORWATER Document of Action – part B – page 1). This Deliverable (D1.1) “Report on needs and priorities in the field of international cooperation agreements on water management in the target Mediterranean African Countries (MACs)” is part of Work Package 1 (WP1) “Water and water-related vulnerabilities in Egypt, Morocco and Tunisia”. The main objective of this work package is to analyze water stress and water vulnerability in the three MACs, paying special attention to wastewater treatment, water reuse and water efficiency in agriculture and the impacts on food security, socio-economic growth, sustainability of agriculture and environmental protection. For this, D1.1 aims to provide a revision of the water related goals within the international agreements joined by the three case study countries, while emphasizing the critical points that should be developed and reinforced in the near future through an integrated approach for water policies, initiatives and management. It also sets a reference framework and knowledge base for different activities in the MADFORWATER project