SYNTHESIS OF AMINO ACETYLENIC BENZOPHENONE DERIVATIVES AS H3-ANTAGONISTS

Objective: To synthesize new amino acetylenic benzophenone derivatives with significant H3-antagonist's activity.Methods: Amino acetylenic benzophenone derivatives were synthesized from the reaction of 2-hydroxybenzophenone with 3-bromoprop-1-in to generate 2-(prop-2-yn-1-yloxy)-1,3-benzophenone (AZ-1). A mixture of 2-(prop-2-yn-1-yloxy)-1,3-benzophenone, paraformaldehyde, cyclic amine, cuprous chloride (catalytic amount) in peroxide free dioane through Mannich reaction yielded the designed amino acetylenic benzophenone derivatives (AZ-2-7).Results: The IR, H1-NMR, 13C NMR, and elemental analysis were consistent with the assigned structures. The designers of these compounds as H3-antagonists were based on the nationalization of the important criteria that provide effective inhibitory binding with H3-receptor. Molecular docking results of compounds (AZ-2-7) showed a good H3-receptor antagonistic activity relative to thioperamide of-6 (kcal/mol) especially AZ-2 which has-8.6 (kcal/mol).Conclusion: Docking results provide a good lead to designing more effective H3 antagonists in managing many CNS diseases like Alzheimer, epilepsy, depression, schizophrenia and many others

Distribution of some Heavy Metals Pollution Caused byAl- Daura Refinery in the Surrounding Region

Due to the higher increase in the oil industry activities in Iraq, since there are a little information of the environmental status of the areas around the refinery locations, and the concerns of a possible environmental pollution that will cause health and life threats to living organisms, this study was carried out.To understand the status of heavy metals pollution in areas inside and surrounding Al-Daura refinery activities, (17) testing locations were chosen, ten locationsoutsidethe refinery and sevenlocationsinside it.One additional location was chosen in a rural (control) area, in the University of Baghdad, to compare between the heavy metals concentration in the study area and a sample from the rural area not affected by the pollution. The soil samples have been taken from (5 and 60 cm) depth from the top surface of the soil. Three samples were taken from each depth for each location to take an average of results.All the samples of soil were taken during the period from Dec/2010 to Feb/2011.The experimental work has been includes the heavy metals concentrations, such as Zinc, Nickel, Lead and Cadmium, have been measured at each selected depth for each testing locations.The results indicate that the mean concentration of Zn and Ni is (62.4 µg/g) and (100.5 µg/g) respectively and this valuesexceeded the mean allowable value by (Alloway, 1995 [2]; Kabata-Pendias and Pendias, 1992 [6]).The most concentrations of Zn, Ni and Pb, with some exceptions, accumulate at the top soil and decrease with the depth except Cd

Digital architecture and designing architecture space and ITS effect on future life strategy

Technological advancements have altered nearly every aspect of individuals’ existence and operation in society. When technologies develop, architecture evolves as well: the architectural techniques change, as does the architectural outcome. The digital revolution reflected on architecture, as did other scientific and life fields. Its impact on the work and architectural space was evident. The architectural production became not limited to designing in traditional ways and directing it as computer drawings. Still, it went beyond that, as the designs produced became the product of an intelligent design process directly influenced by the digital community in general. Architectural space has gone through many developments throughout history influenced by technology and building techniques on the one hand and by functional and environmental issues and human factors on the other hand. The architectural space appeared in the form of a living being that grows over time and is influenced by all the variables of the times and expresses the personality of its inhabitants. If the architect determines space and its composition according to human needs, it is also influenced by the imagination of architecture and its vision of freedom. Therefore, the problem of research was determined by "the lack of a clear vision of the development of architectural space and how it is affected by the digital revolution," where the research aims to identify indicators of the development of architectural space in light of digital development and how architectural thought deals with the changes brought about by information technology, and how it was expressed in the form of areas that meet the needs of users, which in turn changed in terms of sensory needs or physical needs. The research thus assumed "the existence of mechanisms, strategies, levels, and degrees of digital use within the process of designing architectural and urban space to generate digital space," and to achieve this will begin to learn about the evolution of space and what it is over time with a quick presentation of the most prominent developments in the architectural and urban space, especially in the recent years, to a final formulation of the characteristics of knowledge of digital areas

The future of an intelligent and responsive architecture design after the COVID 19 epidemic

An intelligent building is much more than a set of walls; it’s a dynamic organism that employs integrated technologies to share data about the building among various systems to enhance efficiency and provide a better experience for its users. There are a number of challenges with intelligent buildings. They must respond to people’s requirements and needs, including their health and well-being; they must be resource-efficient, and they must include the most useful aspects of new technologies. The current COVID-19 outbreak has pushed architects to consider the future of architectural design technologies. Is it possible that the epidemic may influence the design of our buildings, causing them to become smarter or more intelligent? What role did architecture play throughout the epidemic and in the post-pandemic stage, as well? This paper aims to discuss the future of intelligent design technologies in light of the current Coronavirus epidemic and how it might reshape our architecture design. Finally, the impact of COVID-19 on people’s daily routines in the building design will be discussed

DESIGN, SYNTHESIS AND BIOLOGICAL SCREENING OF AMINOACETYLENIC TETRAHYDROPHTHALIMIDE ANALOGUES AS NOVEL CYCLOOXYGENASE (COX) INHIBITORS

Objective: To design and synthesise a new amino acetylenic tetrahydro phthalimide derivative and investigate their selective inhibitory activity to COXs.Methods: Aminoacetylenic tetrahydro phthalimide derivatives were synthesised by alkylation of tetrahydro phthalimide with propargyl bromide afforded 2-(prop-2-yn-1-yl)-2,3,3a,4,7,7a-hexahydro-1H-isoindole-1,3-dione. The alkylated tetrahydro phthalimide was subjected to Mannich reaction afforded the desired amino acetylenic tetra phthalimide derivatives (AZ 1-6). The elemental analysis was indicated by the EuroEA elemental analyzer and biological characterization was via IR, 1H-NMR, [13]C-NMR, DSC was determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer and DMSO-d6 as a solvent, molecular docking was done using the Autodock Tool software (version 4.2). ChemBioDraw was used in the drawing of our schemes.Results: The IR, 1H-NMR, 13C-NMR, DSC and elemental analysis were consistent with the assigned structures. The designers of the compounds as COXs inhibitor activity were based on the nationalisation of the important criteria that provide effective inhibitory binding with COXs–receptor. The results indicated that the synthesised compounds (AZ1-6) showed a close similarity in the binding affinity to both COXs and may be more specific to COX-1. AZ-5 showed the highest % of inhibition for COX-1 even better than aspirin. Which may suggest that the aryl group is required for COX-2 inhibition.Conclusion: For the first time, we indicate the requirement of aromaticity in COX-2 structural inhibitory activity.Â

Achondroplasia manifesting as enchondromatosis and ossification of the spinal ligaments: a case report

<p>Abstract</p> <p>Introduction</p> <p>A girl presented with achondroplasia manifested as mild knee pain associated with stiffness of her back. A skeletal survey showed enchondroma-like metaphyseal dysplasia and ossification of the spinal ligaments. Magnetic resonance imaging of the spine further clarified the pathological composites.</p> <p>Case presentation</p> <p>A 7-year-old girl presented with the classical phenotypic features of achondroplasia. Radiographic documentation showed the co-existence of metaphyseal enchondromatosis and development of spinal bony ankylosis. Magnetic resonance imaging showed extensive ossification of the anterior and posterior spinal ligaments. Additional features revealed by magnetic resonance imaging included calcification of the peripheral vertebral bodies associated with anterior end-plate irregularities.</p> <p>Conclusion</p> <p>Enchondromas are metabolically active and may continue to grow and evolve throughout the patient's lifetime; thus, progressive calcification over a period of years is not unusual. Ossification of the spinal ligaments has a specific site of predilection and often occurs in combination with senile ankylosing vertebral hyperostosis. Nevertheless, ossification of the spinal ligaments has been encountered in children with syndromic malformation complex. It is a multifactorial disease in which complex genetic and environmental factors interact, potentially leading to chronic pressure on the spinal cord and nerve roots with subsequent development of myeloradiculopathy. Our patient presented with a combination of achondroplasia, enchondroma-like metaphyseal dysplasia and calcification of the spinal ligaments. We suggest that the development of heterotopic bone formation along the spinal ligaments had occurred through an abnormal ossified enchondral mechanism. We postulate that ossification of the spinal ligaments and metaphyseal enchondromatous changes are related to each other and represent impaired terminal differentiation of chondrocytes in this particular case. Standard radiographic examination showed spinal bony ankylosis only. The pathological composites of the vertebrae have been clarified using scanning technology. Extensive spinal ligament ossification associated with calcification of the peripheral vertebral bodies and anterior end-plate irregularities were notable. We report what may be a novel spinal and extraspinal malformation complex in a girl with achondroplasia.</p

Progressive non-infectious anterior vertebral fusion, split cord malformation and situs inversus visceralis

BACKGROUND: Progressive non-infectious anterior vertebral fusion is a unique spinal disorder with distinctive radiological features. Early radiographic findings consist of narrowing of the anterior aspect of the intervertebral disk with adjacent end plate erosions. There is a specific pattern of progression. The management needs a multi-disciplinary approach with major input from the orthopaedic surgeon. CASE REPORT: We report a 12-year-old-female with progressive anterior vertebral fusion. This occurred at three vertebral levels. In the cervical spine there was progressive fusion of the lateral masses of the Axis with C3. Secondly, at the cervico-thoracic level, a severe, progressive, anterior thoracic vertebral fusion (C7-T5) and (T6-T7) resulted in the development of a thick anterior bony ridge and massive sclerosis and thirdly; progressive anterior fusion at L5-S1. Whereas at the level of the upper lumbar spines (L1) a split cord malformation was encountered. Situs inversus visceralis was an additional malformation. The role of the CT scan in detecting the details of the vertebral malformations was important. To our knowledge, neither this malformation complex and nor the role of the CT scan in evaluating these patients, have previously been described. CONCLUSION: The constellations of the skeletal abnormalities in our patient do not resemble any previously reported conditions with progressive anterior vertebral fusion. We also emphasise the important role of computerized tomography in the investigation of these patients in order to improve our understanding of the underlying pathology, and to comprehend the various stages of the progressive fusion process. 3D-CT scan was performed to improve assessment of the spinal changes and to further evaluate the catastrophic complications if fracture of the ankylosed vertebrae does occur. We believe that prompt management cannot be accomplished, unless the nature of these bony malformations is clarified

Water-in-oil microemulsions exhibit antimicrobial activity

Objectives: Previous research from this group has identified significant antimicrobial activity associated with oil-in-water (O/W) microemulsions. This activity has been exhibited against both bacteria and fungi (including yeasts) and bacterial biofilms and is dependent upon the position of the microemulsion within its stability zone. This novel work aims to identify antimicrobial activity of water-in-oil (W/O) microemulsions. Materials &amp; Methods: A simple, thermodynamically stable water-in-oil microemulsion was tested for its time-related antimicrobial activity against a selected panel of test microorganisms (i.e.: Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, Candida albicans ATCC 10231 and Staphylococcus aureus ATCC 6538P) and its effectiveness as a self-preserving system against a similar panel (Pseudomonas aeruginosa ATCC 9027, Candida albicans ATCC 10231, Staphylococcus aureus ATCC 6538P and Aspergillus niger ATCC 16404). Results: The microemulsion exhibited significant antimicrobial activity against all the selected microorganisms. Decreases in the viability of cultures (P. aeruginosa, C. albicans, E. coli and S. aureus) were observed over a short period of time after exposure to a known concentration of the first microemulsion. The results for the four samplings in the preservative effectiveness test according to the European Pharmacopeia requires a significant reduction in bacterial count, and this requirement was achieved in all samplings. Conclusions: Thermodynamically stable water-in-oil microemulsions are antimicrobially active, self-preserving systems, as are their oil-in-water counterparts

Патология верхних конечностей у детей с мукополисахаридозами

Background. Despite the success in the treatment of children with mucopolysaccharidoses (MPS) as a result of the widespread of  enzyme  replacement  therapy  and  hematopoietic  stem  cells  transplantation,  orthopedic  manifestations  continue  to  be a  significant  problem,  while  the  pathology  of  the  upper  limbs  in  children  with  MPS  is  not  sufficiently  represented  in  the literature. The aim of this studywas to analyze orthopedic and neurological manifestations in the upper extremities of children with  mucopolysaccharidosis  based  on  a  sequential  case  series. Materials  and  Methods. We  carried  out  a  comprehensive analysis of clinical and radiological involvement of the upper extremities in 49 patients with MPS. Results. The most common complaints reated to the upper extremities were difficulties in the daily activities (dressing, self-care, playing), impairment of the fine motor skills, and muscle weakness. The most frequent clinical manifestations related to the upper extremities were limited active shoulder abduction, impaired hand grip, flexion contractures of the elbow joint, ulnar deviation of the hand. All patients with MPS types I, II, and VI had limited active and passive extension and flexion of the metacarpophalangeal and interphalangeal joints. In patients with MPS IV, hypermobility of the hand joints prevailed. We noticed minimal presence of typical clinical manifestations related to compression of the median nerve secific for carpal tunnel syndrome. The majority of patients showed a decrease in tendon and periosteal reflexes. The most pronounced decrease in muscle strength was observed in to extensors (elbow, fingers) and shoulder abductors, which may contribute to the predominant formation of a flexion pattern of contractures. On radiographs of the hand, the “melting sugar” symptom and shortening of the metacarpal bones were observed in most patients. Conclusion.Clinical and radiological manifestations related to the upper extremities take  place  in  all  types  of  the  mPS,  and  lead  to  functional  disorders  that  complicate  daily  life  and  self-care.  Upper  limb pathology in children with MPS requires earlier detection and more active treatment after comprehensive risk assessment.Актуальность. Несмотря на успехи в лечении детей с мукополисахаридозами (МПС) в результате широкого внедрения ферментзаместительной терапии и трансплантации гематопоэтических стволовых клеток, ортопедические проявления продолжают оставаться значительной проблемой, при этом патология верхних конечностей у детей с МПС отражена в литературе недостаточно.Материалы и методы Нами проведен комплексный анализ клинических и рентгенологических проявлений со стороны верхних конечностей у 49 пациентов с МПС.Результаты. Наиболее частыми жалобами со стороны верхних конечностей были неловкость при выполнении повседневных движений (одевание, самообслуживание, пользование предметами), нарушение мелкой моторики, мышечная слабость. Наиболее частым клиническим проявлением со стороны верхних конечностей было ограничение активного отведения плеча, нарушение кистевого схвата, сгибательные контрактуры в локтевом суставе, ульнарная девиация кисти. У всех пациентов с МПС I, II и VI типов имело место ограничение активного и пассивного разгибания и сгибания пястнофаланговых и межфаланговых суставов. У пациентов с МПС IV преобладала гипермобильность суставов кисти. При оценке симптомов, характерных для синдрома карпального канала отмечено отсутствие типичных клинических проявлений, обусловленных компрессией срединного нерва. У большинства пациентов отмечалось снижение сухожильных и периостальных рефлексов. Наиболее выраженное снижение силы мышц отмечалось в отношении разгибания пальцев кисти, отведения плеча и разгибания в локтевом суставе, что может способствовать формировании флексионного паттерна контрактур суставов верхних конечностей. На рентгенограммах кисти симптом «тающего сахара» и укорочение пястных костей наблюдались у большинства пациентов.Заключение. Клинические и рентгенологические проявления со стороны верхних конечностей наблюдаются при всех изученных нами типах заболевания, и приводят к функциональным нарушениям, затрудняющим повседневную жизнь и самообслуживание. Патология верхних конечностей у детей с МПС требует более раннего выявления и более активной лечебной тактики после всесторонней оценки рисков