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Design and optimization of piperidinesubstituted thiophene[3,2-d]pyrimidine-based HIV-1 NNRTIs with improved drug resistance and pharmacokinetic profiles

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Acta Pharmaceutica Sinica B 2024年第7期14卷 3110-3124页

作者： Yanying Sun Zhenzhen Zhou Zhongling Shi Fabao Zhao Minghui Xie Zongji Zhuo erik De Clercq christophe.Pannecouqueb Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesShandong UniversityJinan 250012China Rega Institute for Medical Research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province Jinan 250012China

HIV-1 reverse transcriptase(RT)has received great attention as an attractive therapeutic target for acquired immune deficiency syndrome(AIDS),but the inevitable drug resistance and side effects have always been major challenges faced by non-nucleoside reverse transcriptase inhibitors(NNRTIs).This work aimed to identify novel chemotypes of anti-HIV-1 agents with improved drugresistance profiles,reduced toxicity,and excellent druggability.A series of diarylpyrimidine(DAPY)derivatives were prepared via structural modifications of the leads K-5a2 and *** them,15a with dimethylphosphine oxide moiety showed the most prominent antiviral potency against all of the tested viral panel,being 1.6-fold(WT,eC_(50) Z 1.75 nmol/L),3.0-fold(L100I,eC_(50) Z 2.84 nmol/L),2.4-fold(K103N,eC_(50) Z 1.27 nmol/L),3.3-fold(Y181C,eC50 Z 5.38 nmol/L),2.9-fold(Y188L,eC_(50) Z 7.96 nmol/L),2.5-fold(e138K,eC_(50) Z 4.28 nmol/L),4.8-fold(F227L/V106A,eC_(50) Z 3.76 nmol/L)and 5.3-fold(ReS056,eC_(50) Z 15.8 nmol/L)more effective than that of the marketed drug *** docking results illustrated the detailed interactions formed by compound 15a and WT,F227L/V106A,and ReS056 ***,15a-HCl carried outstanding pharmacokinetic(t1/2 Z 1.32 h,F Z 40.8%)and safety profiles(LD_(50)>2000 mg/kg),which demonstrated that 15a HCl is a potential anti-HIV-1 drug candidate.

关键词： HIV-1 NNRTIs NNIBP Structural alert Anti-HIV-1 drug candidate

Lighting up aggregate emission of perylene diimide by leveraging polymerization-mediated through-space charge transfer and π-π stacking

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Science China Chemistry 2024年

作者： Suiying Ye Désirée Füglistaller Tian Tian Anjay Manian Sudhir Kumar Celine Nardo Andrew J.Christofferson Salvy P.Russo Chih-Jen Shih Jean-christophe.Leroux Yinyin Bao Institute of Pharmaceutical Sciences Department of Chemistry and Applied Biosciences ETH Zurich Vladimir-Prelog-Weg 3 Institute for Chemical and Bioengineering Department of Chemistry and Applied Biosciences ETH Zurich Vladimir-Prelog-Weg 1-5 ARC Centre of excellence in exciton Science School of Science RMIT University School of Science STEM College RMIT University

The molecular engineering of fluorescent organic/polymeric materials, specifically those emitting in the deep red to near-infrared spectrum, is vital for advancements in optoelectronics and biomedicine. Perylene diimide(PDI), a well-known fluorescent scaffold, offers high thermal and photophysical stability but suffers from fluorescence quenching in solid or aggregate states due to intense π-π interactions. To mitigate this, simple and versatile methods for strong PDI aggregate emission without extensive synthetic demands are highly desirable but still lacking. Here, we report a straightforward strategy to enhance the solid-state emission of PDI by introducing certain degree of through-space charge transfer(TSCT) via controlled radical polymerization,which can efficiently distort the typical face-to-face PDI stacking, enabling greatly enhanced deep red emission. This is achieved by growing electron-donating star-shape styrenic(co)polymers from a multidirectional electron-accepting PDI initiator. The incorporation of polycyclic aromatic monomers further shifted the emission into the near-infrared region, albeit with a reduced intensity. Overall, the emission of the PDI-based TSCT polymers can be systematically manipulated by leveraging the balance between PDI stacking and the TSCT degree, as confirmed by both experimental study and theoretical calculations. Our approach circumvents complex synthetic procedures, offering highly emissive materials with large Stokes shifts and showing broad potential for optoelectronic technology.

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Co-Morbidities Associated with Prematurity in Two Referral Hospitals in Cameroon

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Open Journal of Pediatrics 2024年第4期14卷 738-753页

作者： Diomede Noukeu Njinkui Dominique enyama Yolande Djike Fokam Cyrelle O. Mefotse Saha Beatrice Moudze Kaptue Charlotte eposse Koube Annick A. Tchouamo Sime christophe.Akazong Adjahoung Marthe e. Barla edgar Mandeng Ma Linwa Seraphin Nguefack Faculty of Medicine and Pharmaceutical Sciences of the University of Dschang Dschang Cameroon Faculty of Health Sciences University of Buea Buea Cameroon Faculty of Health Sciences University of Mountains Bangangte Cameroon Douala Laquintinie Hospital Douala Cameroon Faculty of Medicine and Pharmaceutical Sciences University of Douala Douala Cameroon Douala General Hospital Douala Cameroon Faculty of Medicine and Biomedical Sciences University of Yaound I Yaound Cameroon

Introduction: Prematurity is the leading cause of neonatal death in Africa. More than a million children die each year due to co-morbidities related to prematurity. In addition to being one of the causes of neonatal deaths, the health problems associated with prematurity can also lead to severe lifelong impairment in those who survive. Objectives: This paper aims to determine the epidemiology and identify co-morbidities of prematurity in the neonatology units of the Douala General Hospital (DGH) and the Laquintinie Hospital of Douala (LHD). Patients and Methodology: We conducted an analytical retrospective cohort study from January 2015 to January 2018 in the neonatology department of the GDH and the LHD, which are considered reference hospitals for the management of preterm babies in Cameroon. We included all newborns aged less than 37 weeks admitted to the neonatology units of the GDH and the LHD. The descriptive component was based on the analysis of quantitative variables using measures of central tendency. The analytical component was evaluated using Spearman correlations and the Chi-square and Fisher tests. Simple and multiple logistic regressions measured factors predictive of mortality. The Kaplan Meier survival curve used the Log Rank test and significance at p ≤ 0.05. Results: We recorded 908 preterm newborns in neonatal service and 1,124 preterm deliveries in maternity, representing an incidence of 32.5% in neonatal unit and 10.6% in maternity. 51% of whom were girls, given a sex ratio M/F of 0.9. Hypertension was the main prenatal pathology (9.1%), while premature rupture of membranes: PROM (35.5%) and eclampsia/pre-eclampsia (18.6%) were the most common obstetrical pathologies. 75.9% of deliveries were vaginal with 65.2% being performed in our referral hospitals. Gestational age ranged from 22 to 36 weeks, with a mean of 32.4 weeks. Late preterm birth rate was 53.7%, and birth weight varied between 590 and 3200 g with an average of 1747 ± 479 g. The per

关键词： epidemiology Co-Morbidities Prematurity Douala

Classification of Sandstone-Related Uranium Deposits

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Journal of earth Science 2022年第2期33卷 236-256页

作者： Michel Cuney Julien Mercadier christophe.Bonnetti Universitéde Lorraine GéoRessourcesCNRSCREGUNancy F54500France 2.State Key Laboratory of Nuclear Resources and EnvironmentEast China University of TechnologyNanchang 330013China

Sandstone type deposits are the most common type of uranium deposits in the world.A large variety of sub-types have been defined,based either on the morphology of the deposits(e.g.,tabular,roll front,etc),or on the sedimentological setting(e.g.,paleovalley,paleochannel,unconformity),or on tectonic or lithologic controls(e.g.,tectonolithologic,mafic dykes/sills),or still on a variety of others characteristics(phreatic oxidation type,interlayer permeable type,multi-element stratabound infiltrational,solution front limb deposit,humate type,etc.),reflecting the diversity of the characteristics of these deposits,but making it difficult to have a clear overview of these ***,uranium deposits occurring in the same sedimentological setting(e.g.,paleochannel),presenting similar morphologies(e.g.,tabular),may result from different genetic mechanisms and thus can be misleading for exploration *** aim of the present paper is to propose a new view on sandstone-related uranium deposits combining both genetic and descriptive *** dual view is indeed of primordial importance because all the critical characteristics of each deposit type,not limited to the morphology/geometry of the ore bodies and their relationships with depositional environments of the sandstone,have to be taken into account to propose a comprehensive classification of uranium *** this respect,several key ore-forming processes,like the physical-chemical characteristics of the mineralizing fluid,have to be used to integrate genetic aspects in the *** a succession of concentration steps,potentially temporally-disconnected,are involved in the genesis of some uranium mineralization,the classification here proposed will focus on the main mechanisms responsible for the formation and/or the location of ore *** objective of this paper is also to propose a robust and widely usable terminology to define and categorize sandstone uranium deposits,considering

关键词： sandstone uranium genetic classification redox control depositional environment fluids ore deposit geology

A quantum cascade laser infrared spectrometer for CO_2 stable isotope analysis：Field implementation at a hydrocarbon contaminated site under bio-remediation

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Journal of environmental Sciences 2016年第2期28卷 60-74页

作者： christophe.Guimbaud Cécile Noel Michel Chartier Valéry Catoire Michaela Blessing Jean christophe.Gourry Claude Robert Laboratoire de Physique et de Chimie de l'environnement et de l'espace (LPC2e) CNRS et Universite d'Orleans (UMR 7328)45071 Orleans cedex 2 France Bureau de Recherches Geologiques et Minieres (BRGM) 45060 Orleans cedex 2 France

Real-time methods to monitor stable isotope ratios of CO_2 are needed to identify biogeochemical origins of CO_2 emissions from the soil–air interface. An isotope ratio infra-red spectrometer（IRIS） has been developed to measure CO_2 mixing ratio with δ~13C isotopic signature, in addition to mixing ratios of other greenhouse gases（CH_4, N2_O）. The original aspects of the instrument as well as its precision and accuracy for the determination of the isotopic signature δ~13C of CO_2 are discussed. A first application to biodegradation of hydrocarbons is presented, tested on a hydrocarbon contaminated site under aerobic bio-treatment. CO_2 flux measurements using closed chamber method is combined with the determination of the isotopic signature δ~13C of the CO_2 emission to propose a non-intrusive method to monitor in situ biodegradation of hydrocarbons. In the contaminated area, high CO_2 emissions have been measured with an isotopic signature δ~13C suggesting that CO_2 comes from petroleum hydrocarbon *** first field implementation shows that rapid and accurate measurement of isotopic signature of CO_2 emissions is particularly useful in assessing the contribution of contaminant degradation to the measured CO_2 efflux and is promising as a monitoring tool for aerobic bio-treatment.

关键词： Isotope ratio infrared spectrometry Isotopic signature δ^(13)C of CO_2 Biodegradation monitoring Hydrocarbons BTeX

experiments on thermo-hydro-mechanical behaviour of Opalinus Clay at Mont Terri rock laboratory, Switzerland

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Journal of Rock Mechanics and Geotechnical engineering 2017年第3期9卷 120-128页

作者： Paul Bossart David Jaeggi christophe.Nussbaum Swiss Geological Survey at swisstopo Wabern Switzerland

Repositories for deep geological disposal of radioactive waste rely on multi-barrier systems to isolate waste from the biosphere.A multi-barrier system typically comprises the natural geological barrier provided by the repository host rock e in our case the Opalinus Clay e and an engineered barrier system(eBS).The Swiss repository concept for spent fuel and vitrified high-level waste(HLW)consists of waste canisters,which are emplaced horizontally in the middle of an emplacement gallery and are separated from the gallery wall by granular backfill material(GBM).We describe here a selection of five in-situ experiments where characteristic hydro-mechanical(HM)and thermo-hydro-mechanical(THM)processes have been *** first example is a coupled HM and mine-by test where the evolution of the excavation damaged zone(eDZ)was monitored around a gallery in the Opalinus Clay(eD-B experiment).Measurements of pore-water pressures and convergences due to stress redistribution during excavation highlighted the HM *** same measurements were subsequently carried out in a heater test(He-D)where we were able to characterise the Opalinus Clay in terms of its THM *** yielded detailed data to better understand the THM behaviours of the granular backfill and the natural host *** a presentation of the Swiss concept for HLW storage,we designed three demonstration experiments that were subsequently implemented in the Mont Terri rock laboratory:(1)the engineered barrier(eB)experiment,(2)the in-situ heater test on key-THM processes and parameters(He-e)experiment,and(3)the full-scale emplacement(Fe)*** first demonstration experiment has been dismantled,but the last two ones are on-going.

关键词： Deep geological disposal Radioactive waste Demonstration experiments engineered barrier system(eBS) Granular backfill material(GBM) Bentonite Thermo-hydro-mechanical(THM) behaviour

Overlap syndrome consisting of PSC-AIH with concomitant presence of a membranous glomerulonephritis and ulcerative colitis

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World Journal of Gastroenterology 2014年第16期20卷 4811-4816页

作者： Odile Warling christophe.Bovy Carla Combra Timothée Noterdaeme Jean Delwaide edouard Louis Department of Internal Medicine CHU de LiègeUniversity of Liège4000 LiegeBelgium Department of Internal Medicine NephrologyCHU de LiègeUniversity of Liège4000 LiegeBelgium Department of Abdominal Surgery and Transplantation CHU de LiègeUniversity of Liège4000 LiegeBelgium Department of Cardiovascular Surgery German Heart Center80636 MunichGermany Department of Internal Medicine GastroenterologyCHU de LiègeUniversity of Liège4000 LiegeBelgium

The association of primary sclerosing cholangitis(PSC)and autoimmune hepatitis(AIH)is known as an overlap syndrome(OS).OS can also be described in the setting of concomitant presence of AIH and *** diseases can in some cases be associated with ulcerative *** this case report we describe,to our knowledge,the first case in the literature of a young Caucasian male suffering from ulcerative colitis and an overlap syndrome consisting of an association betweenPSC-AIH,with the concomitant presence of a membranous glomerulonephritis.

关键词： Primary sclerosing cholangitis Autoimmune hepatitis Overlap syndrome Ulcerative colitis Membranous glomerulonephritis

Numerical investigation of electric field distortion induced by internal defects in composite insulators

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High Voltage 2017年第4期2卷 253-260页

作者： Gbah Kone christophe.Volat Hassan ezzaidi Modeling and Diagnostic of Power Network equipment Laboratory University of Quebec at Chicoutimi555 Bd.de l'UniversitéQCCanada G7H 2B1

This paper presents an exhaustive study of numerical investigations based on three-dimensional finite-element method modelling of several non-ceramic insulators of 69,110 and 230 kV having different internal semi-conductive defects in terms of size and *** internal defects were positioned close to the high-voltage electrode,the ground electrode and at floating *** simulations effected on the distortion of the axial and radial e-field components close to the insulator shank between *** results obtained showed that the radial e-field component is more sensitive to the presence of an internal defect as it shows a greater distortion in presence of the *** was also observed that the e-field component distortion increases with longer internal defect and that this increase is particularly important for a defect at floating ***,it was demonstrated that the length of the insulator,for a defect of constant length,has no significant influence on the e-field component ***,the results demonstrated that the presence of a grading ring,as used on the 230 kV insulator,does not have any influence on the e-field component distortion,independently of the defect position.

关键词： distortion insulator defect

Ultrafiltration for environmental safety in shellfish production: A case of bloom emergence

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Water Science and engineering 2021年第1期14卷 46-53页

作者： Clemence Cordier Alexandra Voulgaris christophe.Stavrakakis Patrick Sauvade Franz Coelho Philippe Moulin Aix-Marseille Universite M2P2 UMR 7340Equipe Procedes MembranairesLaboratoire de Mecanique Modelisation et Procedes PropresAix en Provence 13545France Plateforme experimentale Mollusques Marins Station Ifremer de BouinPolder des ChampsBouin 85230France Suez-Aquasource Toulouse 31029France

The process of ultrafiltration(UF)of natural seawater often encounters the problems of variation in water quality and coastal *** validate the feasibility of UF in shellfish farms,this study compared the hydraulic performance and pollutant removal efficiency of the UF process with those of the commonly used treatments that combine several filtration steps with ultraviolet(UV)*** comparison was conducted in the cases of natural seawater and a coastal *** that the UF process encountered the specific type of pollution,this study evaluated the filtration performance of the UF process and the retention of total suspended solids(TSS),bacteria,phytoplankton,and zooplankton.A real coastal bloom was considered in the case study of an experimental shellfish hatchery/nursery in *** results show that both treatments were able to eliminate approximately 50%of ***,in contrast with UV treatment combined with filtration,the UF process retained total amounts of phytoplankton,zooplankton,and bacteria in the *** the hydraulic performance of the UF process was impacted by the coastal bloom,the fouling was eliminated through chemical cleaning conducted at a frequency less than once per 12 *** the severe pollution,this study confirmed the pollution resistance and treatment performance of the UF process,indicating that UF has the potential to enhance the biosecurity level.

关键词： Ultrafiltration environmental safety Aquaculture Shellfish culture Coastal bloom