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This study presents an efficient synthesis pathway for etrasimod, starting from (+)-cis-4-acetoxy-2-cyclopenten-1-ol, yielding 5.6% overall with 98% enantiomeric excess. The crucial intermediate, (4R)-anilinocyclopent-2-enone, was derived from the (S)-alcohol/isocyanate adduct through a concerted, Al2O3-promoted decarboxylative rearrangement, which inverted the configuration. A tetracyclic fused lactam was formed via a one-pot acylation-Michael addition, followed by keto α-arylation. Subsequent removal of the oxo group facilitated the synthesis of cyclopenta[b]indol-3-ylacetic acid through a series of reactions, including methanolysis, indoline oxidation, and hydrolysis.

AbstractThe synthesis of two new hexahydroisoquinoline-4-carbonitrile derivatives (3aand 3b) is reported along with spectroscopic data and their crystal structures. In compound 3a, the intramolecular O—H···O hydrogen bond constraints the acetyl and hydroxyl groups to be syn. In the crystal, inversion dimers are generated by C—H···O hydrogen bonds and are connected into layers parallel to (10–1) by additional C—H···O hydrogen bonds. The layers are stacked with Cl···S contacts 0.17 Å less than the sum of the respective van der Waals radii. The conformation of the compound 3bis partially determined by the intramolecular O—H···O hydrogen bond. A puckering analysis of the tetrahydroisoquinoline unit was performed. In the crystal, O—H···O and C—H···O hydrogen bonds together with C—H···π(ring) interactions form layers parallel to (01–1) which pack with normal van der Waals interactions. To understand the binding efficiency and stability of the title molecules, molecular docking, and 100 ns dynamic simulation analyses were performed with CDK5A1. To rationalize their structure-activity relationship(s), a DFT study at the B3LYP/6-311++G** theoretical level was also done. The 3D Hirshfled surfaces were also taken to investigate the crystal packings of both compounds. In addition, their ADMET properties were explored.Communicated by Ramaswamy H. Sarma

AbstractAnti-SARS-CoV-2 drugs are urgently needed to prevent the pandemic and for immunization. Their protease inhibitor treatment for COVID-19 has been used in clinical trials. In Calu-3 and THP1 cells, 3CL SARS-CoV-2 Mpro protease is required for viral expression, replication, and the activation of the cytokines IL-1, IL-6, and TNF-. The Mpro structure was chosen for this investigation because of its activity as a chymotrypsin-like enzyme and the presence of a cysteine-containing catalytic domain. Thienopyridine derivatives increase the release of nitric oxide from coronary endothelial cells, which is an important cell signaling molecule with antibacterial activity against bacteria, protozoa, and some viruses. Using DFT calculations, global descriptors are computed from HOMO-LUMO orbitals; the molecular reactivity sites are analyzed from an electrostatic potential map. NLO properties are calculated, and topological analysis is also part of the QTAIM studies. Both compounds 1and 2were designed from the precursor molecule pyrimidine and exhibited binding energies (-14.6708 kcal/mol and −16.4521 kcal/mol). The binding mechanisms of molecule 1towards SARS-COV-2 3CL Mpro exhibited strong hydrogen bonding as well as Vdw interaction. In contrast, derivative 2was bound to the active site protein’s active studied that several residues and positions, including (His41, Cys44, Asp48, Met49, Pro52, Tyr54, Phe140, Leu141, Ser144, His163, Ser144, Cys145, His164, Met165, Glu166, Leu167, Asp187, Gln189, Thr190, and GLn192) are critical for the maintenance of inhibitors inside the active pocket. Molecular docking and 100 ns MD simulation analysis revealed that Both compounds 1and 2with higher binding affinity and stability toward the SARS-COV-2 3CL Mpro protein. Binding free energy calculations and other MD parameters support the finding.Communicated by Ramaswamy H. Sarma

AbstractOne of the most common viral infections worldwide is the Human Papilloma Virus (HPV) which has been linked to cancer and other diseases in many countries. Monosaccharide esters are significant in the field of carbohydrate chemistry because they are efficient in the synthesis of pharmacologically active compounds. Therefore, the present study aimed to perform thermodynamic, molecular docking and molecular dynamics study of a series of previously designed monosaccharaides, methyl β-d-galactopyranoside (MGP, 1) esters (2–10) with along with their physicochemical and pharmacokinetic properties. We have optimized the MGP esters employing the DFT study at the B3LYP/6-311 + G (d,p) level of theory. The subsequent analysis also investigated the electronic energies, enthalpies, entropies, polarizability, and natural bond orbital (NBO) of these modified esters. Then, MGP esters were docked into CTX-M-15 extended-spectrum beta-lactamase from Escherichia coli(PDB: 4HBT) and E2 DNA-binding domain from human papillomavirus type 31 (PDB: 1A7G), and the results revealed that most of the esters can efficiently bind to the target. Desmond was used to doing molecular dynamics simulations at 200 ns in addition to molecular docking to look at the binding conformational stability of the protein–ligand complex. Based on RMSD and RMSF, it was determined that the stability of the protein-ligand combination was maintained during the whole 200 ns simulations for all compounds. Finally, a pharmacokinetic study suggests that modified esters of MGP exhibited better pharmacokinetic characteristics and were less hazardous than the parent drug. This work demonstrated that potential MGP esters can efficiently bind to 4HBT and 1A7G proteins and opened avenues for the development of newer antimicrobial agents that can target dangerous pathogens.Communicated by Ramaswamy H. Sarma

AbstractIn 2022, the ongoing multi-country outbreak of monkeypox virus—now occurring outside Africa, too is a global health concern. Monkeypox is a zoonotic virus, which causes disease mainly in animals, and then it is transferred to humans. Recently, in the monkeypox epidemic, a large number of human cases emerged while the global health community worked to tackle the outbreak and save lives. Herein, a multi-epitope-based vaccine is designed against monkeypox virus using two surface-associated proteins: MPXVgp002 accession number > YP_010377003.1 and MPXVgp008 accession number > YP_010377007.1 proteins. These proteins were utilized for B- and T-cell epitopes prediction. The epitopes were further screened, and the screen filtered KCKDNEYRSR, RSCNTTHNR, and RTRRETGAS with the antigenicity scores of 0.5279, 0.5604, and 0.7628, respectively. Overall, the epitopes can induce immunity in 99.74% population of the world. Further, GPGPG linkers were used for joining the epitopes and EAAAK linker was used for adjuvant attachment. It has a three-dimensional structure modelled for retaining the structural stability. Three pairs of amino acid residues that were able to make disulfide bonds were chosen: Gly1-Ser82, Cys7-Tyr10, and Phe51-Ile55. Molecular docking of vaccine was done with toll-like receptors, viz., 2, 3, 4, and 8 immune cell receptors. The docking results revealed that the vaccine as potential molecule due to its better binding affinity with toll-like receptors 2, 3, 4 and 8. Top complex in docking in with each receptor was selected based on lowest energy scores— −888.7 kcal/mol (TLR-2), −976.3 kcal/mol (TLR-3), −801.9 kcal/mol (TLR-4), and −955.4 kcal/mol (TLR-4)—were subjected to simulation. The docked complexes were evaluated in 500 ns of MD simulation. Throughout the simulation time, no significant deviation occurred. This confirmed that the vaccine as potential vaccine candidate to interact with immune cell receptors. This interaction is important for the immune system activation. In conclusion, the proposed vaccine construct against monkeypox could induce an effective immune response and speed up the vaccine development process. However, the study is completely based on the computational approach, hence, the experimental validation is required.Communicated by Ramaswamy H. Sarma

AbstractInfection by the human immunodeficiency virus still represents a continuous serious concern and a global threat to human health. Due to the appearance of multi-resistant virus strains and the serious adverse side effects of the antiretroviral therapy administered, there is an urgent need for the development of new treatment agents that are more active, less toxic, and with increased tolerability to mutations. Quinoxaline derivatives are a class of heterocyclic compounds with a wide range of organic and remedial applications. In addition, they are known to significantly inhibit HIV reverse transcriptase (RT) and HIV replication in cell cultures. For these reasons, we are investigating the synthesis and computational studies of quinoxaline derivatives with a focus on their effects on the HIV RT enzyme, and we present here the structure of one such molecule, methyl 2-[(2E)-3-oxo-1,2,3,4-tetrahydroquinoalin-2-ylidene] acetate, which was confirmed by X-ray diffraction studies. In the crystal, N—H···O and C—H···O hydrogen bonds form ribbons whose mean planes are inclined to (111) by 25.69(8)°. The ribbons are formed into stacks by C—H···π(ring) interactions and π-stacking interactions between carbonyl groups. The Hirshfeld surface map allows us to understand the nature of interactions in the contribution to crystal packing. A density functional theory (DFT) calculation was performed to optimize the geometrical parameters and then they were compared with the solid-state phase. The molecular electrostatic potential map displays reactive sites on the surface, which are responsible for intermolecular interaction in the chemical species. Computational molecular docking, in addition to molecular dynamics simulations and MMGB/PBSA binding energy techniques, was used to assess the affinity of the molecule for the HIV reverse transcriptase enzyme. The new quinoxaline derivative is more powerful in terms of binding affinity and binding conformation stability with the HIV reverse transcriptase enzyme, which suggests the molecule is a good candidate for further biological optimization.Communicated by Ramaswamy H. Sarma

AbstractTwo new compounds namely, ethyl (2E)-3-(dimethylamino)-2-(3-methoxyquinoxalin-2-yl)propen-2-enoate (II) and ethyl 2-(3-oxo-4-(prop-2-yn-1-yl)-3,4-dihydroquinoxalin-2-yl)-3-phenylpropanoate (III) have been synthesized from ethyl 2-(oxo-3,4-dihydroquinoxalin-2-yl) acetate (I). The compounds were characterized using NMR (1H and 13C), Fourier transform infrared and confirmed by single crystal X-ray diffraction studies. The quinoxaline portion of IIis almost planar with the substituent containing the dimethylamino and carboxyethyl groups rotated well out of its mean plane. In the crystal, C—H···O and C—H···N hydrogen bonds as well as C—H···π(ring) interactions form chains having a U-shaped cross-section and running along the c-axis direction. Two sets of pair-wise C—H···O hydrogen bonds connect the chains into corrugated sheets. In III, the three substituents on the dihydroquinoxaline moiety are rotated well out of its mean plane. Three sets of C—H···O hydrogen bonds as well as C—H···π(ring) and π–π-stacking interactions form layers approximately parallel to [001]. These are associated along the c-axis direction by additional C—H···π(ring) interactions. Additionally, the Hirshfeld surface analyses showed that the H···H contact is the most important interaction for both IIand III.In addition to this, molecular docking and dynamics studies were carried for these two compounds with the c-Jun N-terminal kinases (JNK1) molecule.Communicated by Ramaswamy H. Sarma

ABSTRACTThis research investigates the synthesis of a new Finite Frequency Observer (FFO) to detect faults affecting wind turbines. First, the wind turbine nonlinear behaviour is approximated using Takagi-Sugeno (T-S) fuzzy modelling technique for observer design purposes. Then, through the H-/H∞ optimisation technique with Finite Frequency (FF) specification, the FFO design conditions are formulated using the Lyapunov method as a set of LMIs. Finally, to assess the efficiency of the FFO-based detection approach, simulations results are applied to a dynamic 4.8 MW WT model, where an Unknown Input Observer method is used for comparison.

AbstractHere we report synthesis of three new compounds namely, 1-acetyl-1H-benzimidazolo-2(3H)-one (I), N-(5-acetyl-6-methyl-2-oxo-2H-pyran-4-yl)-N-(2-acetamidophenyl)acetamide (II) and N-(2-acetamidophenyl)-N-2-oxo-2H-pyran-4-yl)acetamide (III) have been synthesized and characterized by single crystal X-ray diffraction. Compounds Iand IIcrystallize in the monoclinic space groups P21/n, and P21/c, respectively, while IIIcrystallizes in the triclinic space group P-1. The theoretical parameters of I–IIIhave been calculated through density functional theory (DFT) by using the hybrid functional B3LYP and basis set 6-311++G**. These theoretical parameters have been compared with the experimental ones obtained by XRD. The significant intermolecular interactions arising in crystal packing are rationalized by means of the Hirshfeld surface analysis method. The major intermolecular contacts in the Hirshfeld surfaces of I–IIIare from H…H contacts. In addition, binding modes of I–IIIwithin Tyrosine-protein kinase JAK2 were investigated using molecular docking and molecular dynamics simulation studies.Communicated by Ramaswamy H. Sarma

Abstract6-Methyl-7H,8H,9H-[1,2,4]triazolo[4,3-b][1,2,4]triazepin-8-onehas been synthesized, characterized by spectroscopic techniques (FT-IR, 1H and 13C NMR) and finally the structure was confirmed by single crystal X-ray diffraction studies. In the title molecule, C6H7N5O, the 7-membered ring adopts a bowl-like conformation. In the crystal, the molecules form stacks along the c-axis direction through offset π-stacking interactions between the 5-membered rings and C–H···N hydrogen bonds. The stacks are associated viaa combination of N–H···N, C–H···O and C–H···N hydrogen bonds. Further, the Hirshfeld surface analysis reveals the nature of molecular interactions and the fingerprint plot provides information about the percentage contribution from each individual molecular contact to the surface. In addition, due to its biological interest the target molecule adenosine A1 receptor was found based on Structural Activity Relationship (SAR) analysis and, further, subjected into molecular docking and molecular dynamics analysis to understand the binding interaction and stability of the molecule in adenosine A1 receptor system. Furthermore, the Density Functional Theory (DFT) calculations were carried for free compound and the compound in active site (single point DFT), to know the internal stability.Communicated by Ramaswamy H. Sarma

•A 6-bromo-3-cyanocoumarin is synthesized and single crystal XRD showed that the asymmetric unit contained two molecules that are independent relative to crystallography.•Hirshfeld surface analysis inferred that highest interaction from inside surface to outside is C—H.•Void analysis showed that the compound will have good response to an applied stress.•Computational study results are consistent with the corresponding ones of single crystal XRD.•ADME parameter analysis showed that the compound is member of a class of drugs with a high GI absorption.

La production scientifique est prise en compte dans la validation de l’ensemble de la formation théorique des chirurgiens en formation. L’objectif de cette étude était d’évaluer la production scientifique indexée des chirurgiens en formation, toute spécialité confondue. L’hypothèse était que l’activité de publication des jeunes chirurgiens est abondante et de bonne qualité.

ABSTRACTThis paper presents a robust fault detection and isolation (FDI) scheme for a variable speed wind turbine. The proposed scheme (extreme learning machine–state-dependent differential Riccati equation (ELM-SDDRE)) is an observer model-based approach, especially, a non-linear observer using SDDRE based on an improved model of the wind turbine by using the ELM. The standard SDDRE can be used for small model uncertainties. However, when the uncertainties are large, the SDDRE cannot detect and isolate the faults. The main objective of the ELM is the prediction of unknown nominal model dynamics to construct a new improved nominal model used by the observer for FDI. This makes the effect of uncertainties weak and consequently allows better faults detection. The faults considered in this paper are sensor faults in the rotating speeds of the rotor and generator outputs. The effectiveness of the proposed approach is illustrated through simulation.

Benzimidazole derivatives are of substantial importance because of their wide array of pharmacological activities. These nitrogen-containing heterocycles are used as therapeutic agents in medicinal chemistry. The title compound has been prepared using click chemistry (Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC)) involving 1-propargyl-6-methoxy benzimidazolone as the dipolarophile and benzylazide as the dipole. The crystallographic study showed that the compound with formula C18H17N5O2 adopts a "pincer-like" conformation in the crystal. Inversion-related NH⋯O hydrogen bonds form dimers which are elaborated into layers parallel to (10–2) by CH⋯O and CH⋯N hydrogen bonds and CH⋯π(ring) and π-stacking interactions. The Hirshfeld surface analysis of the title compound was performed using the Crystal Explorer program while the density functional theory (DFT) calculation was performed by the hybrid B3LYP method.

Inhibitive performance of 3-methylquinoxaline-2 (1H) -thione denoted (MQ = S) on mild steel corrosion in 1.0 M H3PO4was investigated using electrochemical measurements. It is revealed that this product acts as an excellent corrosion inhibitor for mild steel in 1.0 M H3PO4where its inhibition reaches 93% at 5 × 10−4M and increases with immersion time. Potentiodynamic polarization curves indicated that this compound acts as a mixed-type inhibitor. In addition, the MQ = S has its inhibition at high temperature. It was found that the adsorption of this compound obeyed the Langmuir adsorption isotherm.

El cáncer de vejiga es el quinto en frecuencia entre las neoplasias malignas y afecta sobre todo a una población anciana. El factor de riesgo principal es el tabaco. El diagnóstico suele efectuarse a causa de una hematuria o, más raramente, de hiperactividad vesical o dolores pélvicos. La primera etapa del diagnóstico consiste en una resección transuretral de la vejiga. La forma más común es el carcinoma urotelial: el 90% de los casos. La resección hace posible una primera estimación del estadio y del grado de la enfermedad. Se distinguen entonces los tumores infiltrantes del músculo vesical, que pueden ser metastásicos, y tumores más superficiales, cuya extensión a distancia no es común pero tienden a recidivar. En las formas que infiltran el músculo se efectúa una evaluación de extensión para descartar una invasión ganglionar o visceral, cuyo tratamiento consiste en quimioterapia a base de cisplatino. En los otros casos que infiltran el músculo, el tratamiento de referencia es una quimioterapia neoadyuvante seguida de cistectomía ampliada y vaciamiento ganglionar. Hay alternativas que permiten conservar la vejiga, pero con una eficacia oncológica inferior. Algunas formas superficiales que no invaden el músculo deben someterse a una nueva resección para definir mejor el riesgo de evolución. De forma global, los tumores de bajo riesgo se vigilan tras una instilación postoperatoria precoz, en los de riesgo intermedio se efectúan instilaciones de mitomicina C o de bacilo de Calmette-Guérin (BCG) durante 1 año; en los de alto riesgo, instilaciones de BCG durante 3 años, y en los de muy alto riesgo, una cistectomía ampliada. Los tumores no uroteliales responden a una estrategia distinta, y la cistectomía radical asociada a quimioterapia es el enfoque más corriente, sea cual sea el estadio inicial de la enfermedad.

Asthma is a chronic disease that continues to be an important public health problem. While there have been published guidelines for diagnosis and treatment of asthma, the real medical practice varies among different healthcare providers. Aim: To describe the asthma care modalities among asthma specialists in Lebanon. Methods: This cross-sectional study included a survey of demographic characteristics of asthma specialists, parameters of asthma diagnosis, follow-up, treatment, patient education, use of asthma guidelines, and involvement in continuous medical education. Results: A total of 100 registered asthma specialists in Lebanon who attended the 2013 annual meeting of Lebanese Pulmonary Society (LPS) were approached. Seventy-five questionnaires were returned achieving a response rate of 75%. Seventy participants (50 males and 20 females) filled out the questionnaire. The average age was 43 ±8.5years. 33% of the specialists reported seeing 10-20 asthmatic patients weekly. Spirometry was used by 81.4% of respondents on newly diagnosed patients while 36% used peak flow monitoring. Most of the specialists (91%) asked about cough and wheezing, 22% monitored spirometry during follow-up visits. The rate of different medications reported to be "often" used for moderate asthma were: 94% for inhaled steroids, 61% for long-acting beta-agonists (LABA). About 88% of respondents indicated that they were aware of asthma practice guidelines. Moreover, 93% of specialists attended continuous medical education on asthma in the past year. Conclusion: This survey showed deficiencies in asthma care in line with international guidelines (GINA and NAEPP) among asthma specialists in Lebanon. However, their practice was comparable to their peers in Chicago in regard of diagnostic tools utilization.

AbstractObjectiveHospitals are expected to serve the medical needs of casualties in the face of a disaster or other crisis, including man-made conflicts. The aim of this study was to evaluate the impact of the 2011 Yemeni revolution on hospital disaster preparedness in the capital city of Sana’a.MethodsThe study was conducted in September 2011 and 2013. For evaluation purposes, the hospital emergency response checklist published by the World Health Organization (WHO) was used. Additional information was also obtained to determine what steps were being taken by hospital authorities to improve hospital preparedness.ResultsThe study selected 11 hospitals. At the time of the first evaluation, 7 hospitals were rated “unacceptable” for level of preparedness and 4 were rated “insufficient,” receiving a WHO checklist rating of 10 to 98. At the second evaluation, 5 hospitals were rated “unacceptable,” 3 “insufficient,” and 1 “effective,” receiving a rating of 9 to 134.ConclusionsUnfortunately, this study shows that between 2011 and 2013, no significant progress was made in hospital disaster preparedness in Sana’a. In a disaster-prone country like Yemen, the current situation calls for drastic improvement. Health system authorities must take responsibility for issuing strategic plans as well as standards, guidelines, and procedures to improve hospital disaster preparedness. (Disaster Med Public Health Preparedness.2015;9:396–402)

AbstractThis article analyzes interviews related to the 1916–19 Sharifian siege of Medina that were published in a collection on the city's history by Saudi Arabian historian Ahmad Murshid. These oral histories narrate how Fakhri Pasha (Turkish: Fahreddin), the Ottoman military commander stationed in Medina during the siege, expelled residents from their homes, strictly controlled the supply of food in the city, and managed military operations out of the Holy Mosque of the Prophet Muhammad. The article seeks to explore the perspective of ordinary civilians who experienced the siege, a perspective largely missing from the literature on the subject. The interviews are positioned here as a valuable historical source for understanding the impact of the siege on these individuals and on their families, communities, and identities. Their memories underscore the interviewees’ deep attachment to their city, as well as to their identity as madanīs and as legitimate narrators of Medina's history.

Abstract: The 2-propargyl-5-o-hydroxyphenyltetrazole (PHPT) has been tested as corrosion inhibitor for low carbon steel in simulated cooling water. The polarization curves showed that PHPT acts as mixed-type inhibitor. Its inhibition efficiency was found to enhance with increase of the inhibitor concentration and immersion time due to the formation of the inhibitor film on the metal surface as indicated by electrochemical impedance spectroscopy measurements. To complete the formulation further, a non oxidizing biocide was added. Its presence with PHPT does not affect its inhibitory performance and it can be served as a basic component of the formulation for cooling water system. [Copyright &y& Elsevier]

Estrogen modulates NMDA receptors function in the brain. It increases both dendritic spine density and synapse number in the hippocampus, an effect that can be blocked by NMDA antagonist. In this study, we investigated the effect of 17β‐estradiol and progesterone treatment on NMDA receptors in ovariectomized rats. Two different doses were used for 10 weeks. Receptor autoradiography was done on brain sections using [3H] MK‐801 as a ligand. Our results showed a significant increase in [3H] MK‐801 binding in the dentate gyrus, CA3 and CA4 areas of the hippocampus of ovariectomized compared to sham operated rats. In addition, we observed similar changes in CA1. 17β‐estradiol treatment in both doses reduced the binding back to the normal level while progesterone treatment did not show any effect. Spatial reference memory was tested on Morris water maze task. Ovariectomy severely impaired spatial reference memory. Estradiol but not progesterone treatment significantly improved the memory performance of the ovariectomized rats. Low dose treatment showed better learning than high dose estrogen treatment. The decrease in the antagonist sites by estradiol treatment could result in an increase in the sensitivity of the hippocampus to the excitatory stimulation by glutamate system and hence the effect of estradiol on learning and memory. The changes of NMDA receptors in the hippocampus support the concept that estrogen‐enhancing effect on spatial reference memory could be through the enhancing of NMDA function.

Growth hormone (GH) and insulin‐like growth factor‐I (IGF‐I) are known to play an important role in bone metabolism. The regulation of plasma levels of GH and IGF‐I by ovarian steroids is well known, however, their effect on local GH and IGF‐I is still unclear. In this study, we investigated the effect of ovariectomy and ovarian steroid treatment on the femur GH and IGF‐I levels as well as on bone density in the rat. Nine month‐old rats were ovariectomized (OVX) or sham‐operated (SHAM) and 9 weeks after the surgery they were treated with daily s.c. injections of either 17β‐estradiol (OVX + E), progesterone (OVX + P), or vehicle (OVX + V) for another 10 weeks. GH and IGF‐I levels in the femur extracts were measured by specific radioimmunoassay (RIA). Ovariectomy decreased GH and had no effect on IGF‐I levels. Estradiol treatment increased femur GH and IGF‐I levels compared to SHAM rats. Progesterone restored GH and increased IGF‐I levels. Ovariectomy decreased, estrogen restored and progesterone partially restored femur bone density. Our results demonstrate that ovariectomy and ovarian steroids modulate the levels of GH and IGF‐I in the bone of aged OVX rats. However, these effects appear to be limited to supraphysiological concentrations of estradiol and progesterone. © 2001 Orthopaedic Research Society. Published by Elsevier Science Ltd. All rights reserved.

Immobilisation causes denervation-like changes in the motor endplates, decreases the content of IGF-I, and increases the number of IGF-I receptors in the spinal cord. In the rat we investigated whether similar changes occur after a fracture of the midshaft of the femur which had been treated by intramedullary fixation with adequate or undersized pins.A more pronounced reduction in muscle wet weight was seen after fixation by undersized pins as well as decreased ash density of the ipsilateral tibia which did not completely return to normal within the 12-week experimental period. The nicotinic cholinergic receptors in the motor endplates of tibialis anterior were increased (p < 0.01) and there was a significant increase (p < 0.02) in IGF-I receptors in the lumbar spinal cord ipsilateral to the fracture after treatment by undersized nails. These changes may be associated with the impaired proprioception, co-ordination and motor activity which are sometimes seen after fractures.

Transplantation of autologous iris pigment epithelium (IPE) into the subretinal space has been suggested as one approach for the treatment of age-related macular degeneration. Autologous rabbit IPE cells were transplanted to the subretinal space to define the technique of transplantation and examine the survival of the transplanted cells.

Isotopic and chemical analysis for spring waters from El-Fayoum area have been used to identify the recharge sources of these waters. The similarity of the isotopic content between the springs and River Nile and Bahr Youssef indicates that the springs are recharged mainly from the seepage of surface water. The springs have about twice the salinity of surface waters due to increases in Ca++, Mg++ and HCO3- concentrations while Lake Quarun is greatly enriched in both major element chemistry and heavy isotopes relative to surface waters and springs. Most of the trace elements were highest in daline Lake Quarun, lowest in surface waters, and intermediate in the springs. Very high nitrate pollution was observed in one of the springs.

The possibility of estimating groundwater inflow to irrigation drains in Minia, Egypt, using stable isotopes has been explored. The evaporation pan technique described here makes use of small variations in the concentration of naturally occurring stable isotopes (oxygen-18 and deuterium) in irrigation-fed groundwater and surface water as well as agricultural drainage water. The agreement between the stable isotope pan experiments carried out at Minia with others conducted at different locations in Egypt makes it feasible to estimate the inflow of groundwater to be about 42% of the total drainage water.

A hydrochemical and environmental isotopes study was undertaken for Mallawi area in El-Minia province in upper Egypt. The results of hydrochemical analysis indicate that the salinity ranges from 200-950 ppm and that the predominate water type is meteoric and mixed water. The interrelation between different anions and cations were discussed in terms of probable different contribution of dissolution of either halide minerals or gypsum or limestone rocks. The correlation between the deuterium content and the salinity as well as the major anions has been studied to determine the recharge source. The results indicate a trend of decrease of salinity chloride and sulphate content with increasing deuterium concentration, while the bicarbonate shows the opposite relationship. The hydrochemical and environmental isotopes data point out a recent recharge of groundwater with some contribution of palaeowater (characterized by low content of deuterium, oxygen 18 and no tritium). This contribution is different from well to another and is clearer in the Eastern fringe than in the Western Part of the River Nile Valley.

The ability of sense peptides(coded for by sense DNA) and corresponding antisense peptides (coded for by corresponding antisense DNA) to interact specifically was used to design antisense peptide inhibitors of interleukin-1 isoforms IL-1ß and IL-1a. These inhibitors appear to act as “mini receptors”, binding to both isoforms and thereby sterically blocking the normal interaction between interleukin-1 and its receptors.

Representative isolates from 10 distinct extended-spectrum beta-lactamase-producing strains of Klebsiella pneumoniae that caused hospital outbreaks in the United Kingdom from 1991 to 1994 were examined for relationships between their enzymes and plasmids. The beta-lactamases were identified by a combination of isoelectric focusing and gene sequencing. SHV-2 beta-lactamase was produced by isolates from four outbreaks, SHV-5 was involved in three, and SHV-4, TEM-15, and TEM-26 were involved in one outbreak each. All of the extended-spectrum beta-lactamases were encoded by self-transmissible plasmids, with sizes ranging from about 70 to 160 kb. No similarities between the restriction digest patterns of the extended-spectrum beta-lactamase-encoding plasmids were detected, except to some extent between those that produced TEM-15 and TEM-26. Thus, outbreaks of hospital infection with these organisms in the United Kingdom from 1991 to 1994 involved distinct organisms and resistance plasmids and appeared to be unrelated.

Nach den Antisense‐Oligonucleotiden kommen die Antisense‐Peptide: Diese leiten sich ab von dem DNA‐Strang, der nicht die Proteine codiert, sondern nur als Matrize zur DNA‐Vervielfältigung dient. Aus einem DNA‐Stück lassen sich so komplementäre Sense‐ und Antisense‐Peptide ableiten. Das Prinzip wurde genutzt, um Peptidinhibitoren für die Interleukine 1α und 1β zu entwickeln. Diese Antisense‐Peptidinhibitoren fungieren als „Mini‐Rezeptoren”︁ für die Interleukine, an die sie so binden, daß die normale Wechselwirkung zwischen Interleukin 1 und dessen Rezeptoren blockiert ist.

ABSTRACTRepresentative isolates from 10 distinct extended-spectrum ß-lactamase-producing strains of Klebsiella pneumoniaethat caused hospital outbreaks in the United Kingdom from 1991 to 1994 were examined for relationships between their enzymes and plasmids. The ß-lactamases were identified by a combination of isoelectric focusing and gene sequencing. SHV-2 ß-lactamase was produced by isolates from four outbreaks, SHV-5 was involved in three, and SHV-4, TEM-15, and TEM-26 were involved in one outbreak each. All of the extended-spectrum ß-lactamases were encoded by self-transmissible plasmids, with sizes ranging from about 70 to 160 kb. No similarities between the restriction digest patterns of the extended-spectrum ß-lactamase-encoding plasmids were detected, except to some extent between those that produced TEM-15 and TEM-26. Thus, outbreaks of hospital infection with these organisms in the United Kingdom from 1991 to 1994 involved distinct organisms and resistance plasmids and appeared to be unrelated.

A new 2-(5-methyl-2-Nitro-1H-imidazol-1-yl)ethyl benzoate (IMDZ-B) was synthesized and characterized using elemental analyses, NMR and Fourier transform infra-red (FTIR) techniques. Its effect on brass corrosion in 1.0 M H3PO4solution was investigated by using electrochemical measurements coupled with X-ray diffraction analysis (XRD), Scanning electron microscopy (SEM) and Energy-dispersive X-ray spectroscopy (EDX). The polarization measurements showed that the IMDZ-B acts as a mixed type inhibitor. Indeed, it is found that the IMDZ-B compound is a very good inhibitor, which its inhibition efficiency increases with concentration to reach a maximum of 99.5% at 10−3 M. In addition, the obtained electrochemical parameters from impedance indicated that the IMDZ-B molecules act by adsorption on metallic surface. This adsorption was found to obey Langmuir's adsorption isotherm. However, the temperature effect on the performance of IMDZ-B was also studied. It is found that the IMDZ-B takes its performance at high temperature. In addition, the obtained kinetic and thermodynamic parameters showed that the IMDZ-B molecules act via two adsorption modes, physisorption and chemisorptions, and its process is endothermic and spontaneous. Finally, the XRD and SEM/EDX analyses confirmed the electrochemical obtained results.

Le progrès technologique a rendu l’information plus accessible. Twitter est un réseau de micro-blogging. Toutes les sociétés savantes en urologie ont désormais un compte Twitter. Les congrès sont retransmis en temps réel via ce réseau. L’objectif de ce travail est d’évaluer le potentiel de Twitter en tant que source d’information en onco-urologie et son exploitation en recherche biomédicale.

La télémédecine est considérée aujourd’hui comme l’une des composantes les plus dynamiques de l’avenir du système de soins, mais le statut de son utilisation en urologie reste inconnu. L’objectif de ce travail est de faire un état des lieux de la littérature scientifique et de déterminer l’intérêt de ce groupe de technologies dans l’optimisation du parcours de santé du patient en urologie.