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Discovery of N-benzyl hydroxypyridone carboxamides as a novel and potent antiviral chemotype against human cytomegalovirus (HCMV)

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Acta Pharmaceutica Sinica B 2022年第4期12卷 1671-1684页

作者： Sameera Senaweera Tiffany C.Edwards Jayakanth Kankanala Yan Wang Rajkumar Lalji Sahani Jiashu Xie Robert J.Geraghty Zhengqiang Wang Center for Drug Design College of PharmacyUniversity of MinnesotaMinneapolisMN 55455USA Translational Medicine R&D Center Shenzhen Institutes of Advanced TechnologyChinese Academy of SciencesShenzhen 518055China

Current drugs for treating human cytomegalovirus(HCMV)infections are limited by resistance and treatment-associated toxicities.In developing mechanistically novel HCMV antivirals,we discovered an N-benzyl hydroxypyridone carboxamide antiviral hit(8a)inhibiting HCMV in submicromolar range.We describe herein the structure–activity relationship(SAR)for 8a,and the characterization of potent analogs for cytotoxicity/cytostatic property,the preliminary mechanism of action,and the absorption,distribution,metabolism and excretion(ADME)properties.The SAR revealed a few pharmacophore features conferring optimal antiviral profile,including the 5-OH,the N-1 benzyl,at least one–CH_(2)−in the linker,and a di-halogen substituted phenyl ring in the amide moiety.In the end,we identified numerous analogs with sub-micromolar antiviral potency and good selectivity index.The preliminary mechanism of action characterization used a pUL89-C biochemical endonuclease assay,a virus entry assay,a time-of-addition assay,and a compound withdrawal assay.ADME profiling measuring aqueous solubility,plasma and liver microsomal stability,and parallel artificial membrane permeability assay(PAMPA)permeability demonstrated largely favorable drug-like properties.Together,these studies validate the N-benzyl hydroxypyridone carboxamide as a viable chemotype for potent and mechanistically distinct antivirals against HCMV.

关键词： Human cytomegalovirus N-Benzyl hydroxypyridone carboxamides Structureeactivity relationship Mechanism of action

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Biobanking in LMIC settings for infectious diseases: Challenges and enablers

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Biosafety and Health 2022年第5期4卷 290-292页

作者： sameera Ezzat Ruzica Biga Zisis Kozlakidis National Liver Institute Menoufia UniversityShibin el Kom 32511Egypt Mounir Armanious Research Center(MARC) Giza 12561Egypt University Cote D’Azur Nice 06103France International Agency for Research on Cancer World Health OrganizationLyon 69372France

Biobanking facilities are well established in high-income settings,where substantial funding has been invested in infrastructure.In contrast,such facilities are much less developed in resource-restricted settings.However,low-and middle-income countries(LMICs)still face a disproportionately high infectious diseases burden.Thus,the further development of infrastructure facilities,including biobanks is warranted as an important component of this unfolding clinical research environment.This perspective manuscript summarises the challenges and enablers for biobanking in LMICs,with a particular focus on infectious diseases,incorporating some of the lessons learned from the recent coronavirus disease 2019(COVID-19)pandemic.

关键词： Biobanking Research infrastructures Infectious diseases Low-and-middle income countries LMICs

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On ideal convergence of double sequences in 2-fuzzy n-normed linear space

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Applied Mathematics(A Journal of Chinese Universities) 2022年第2期37卷 177-186页

作者： Vakeel A.Khan sameera A.A.Abdullah Kamal M.A.S.Alshlool Umme Tuba Nazneen Khan Department of Mathematics Aligarh Muslim UniversityAligarh 202002India Department of Mathematics Sultan Qaboos UniversityMuscatOman

The purpose of this paper is to define the notions of convergence, Cauchy st–convergence, st–Cauchy, I –convergence and I –Cauchy for double sequences in 2–fuzzy n–normed spaces with respect to α–n–norms and ... 详细信息

关键词： 2-fuzzy n-normed spaces -n-norm I-convergence I-Cauchy

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Enhancing CNN for Forensics Age Estimation Using CGAN and Pseudo-Labelling

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Computers, Materials & Continua 2023年第2期74卷 2499-2516页

作者： Sultan Alkaabi Salman Yussof sameera Al-Mulla Institute of Informatics and Computing in Energy Universiti Tenaga NasionalMalaysia College of Engineering and IT University of DubaiUAE

Age estimation using forensics odontology is an important process in identifying victims in criminal or mass disaster cases.Traditionally,this process is done manually by human expert.However,the speed and accuracy may vary depending on the expertise level of the human expert and other human factors such as level of fatigue and attentiveness.To improve the recognition speed and consistency,researchers have proposed automated age estimation using deep learning techniques such as Convolutional Neural Network(CNN).CNN requires many training images to obtain high percentage of recognition accuracy.Unfortunately,it is very difficult to get large number of samples of dental images for training the CNN due to the need to comply to privacy acts.A promising solution to this problem is a technique called Generative Adversarial Network(GAN).GAN is a technique that can generate synthetic images that has similar statistics as the training set.A variation of GAN called Conditional GAN(CGAN)enables the generation of the synthetic images to be controlled more precisely such that only the specified type of images will be generated.This paper proposes a CGAN for generating new dental images to increase the number of images available for training a CNN model to perform age estimation.We also propose a pseudolabelling technique to label the generated images with proper age and gender.We used the combination of real and generated images to trainDentalAge and Sex Net(DASNET),which is a CNN model for dental age estimation.Based on the experiment conducted,the accuracy,coefficient of determination(R2)and Absolute Error(AE)of DASNET have improved to 87%,0.85 and 1.18 years respectively as opposed to 74%,0.72 and 3.45 years when DASNET is trained using real,but smaller number of images.

关键词： Dental forensics age estimation generative adversarial network pseudo-labelling convolutional neural network

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Differentiating Postmortem Claw Marks by the Asian Water Monitor(Kabaragoya)from Antemortem Sharp Weapon Trauma Based on the Injury Pattern

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Journal of Forensic Science and Medicine 2022年第3期8卷 114-117页

作者： Piumi Dileka Chiranthika Madhupoorni A.Gunathilaka Thilinika Ranchamali sameera A.Gunawardena Department of Forensic Medicine and Toxicology Faculty of MedicineUniversity of ColomboColomboSri Lanka

The Asian water monitor(Varanussalvator)or kabaragoya isthe predominant large animalscavenger of human remainsin Sri Lanka;however,its significance is rarely discussed in the forensic literature.This is the case of a 54‑year‑old male with a history of dementia,depression,and wandering behavior whose body was found,partially submerged in a river,2 days after he was reported missing.There were several linear wounds with regular margins over his arms and face which raised the suspicion of homicidal sharp weapon trauma.The injuries were seen in clusters and did not involve harder structures such as tendons,ligaments,or bones.There were no signs of inflammation or bleeding.They were attributed to kabaragoya claw marks,which are postmortem artifacts that mimic incised wounds.However,there were no areas of tissue loss to indicate that the animal had begun feeding on the corpse.This case discusses the problems faced by medicolegal investigators when encountering this phenomenon which is relatively underreported in the forensic literature.

关键词： Animal predation antemortem trauma monitor lizards postmortem artifacts postmortem trauma

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Investigating tight oil reservoir production performance:Influence of geomechanical parameters and their distribution

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Petroleum Research 2023年第4期8卷 490-498页

作者： sameera M.Hamd-Allah Nagham Jasim Al-Ameri Petroleum Engineering Department College of EngineeringUniversity of BaghdadIraq

Geomechanical properties have a prominent influence on reservoir stresses,which consequently reduce permeability and porosity with pressure depletion.These properties significantly affect the accuracy of reservoir modeling and recovery calculation,but have not been fully studied;therefore,more work is needed.Full field data and laboratory measurements are included in the study.The work involves deriving an equation by combining experimental data for permeability and porosity reduction during a change in stress with the poroelastic stress equation to investigate the impact of Poisson's ratio and Young's modulus on the reduction of permeability and porosity with pressure depletion.Most simulation studies assume constant geomechanical properties across the entire reservoir or for each individual reservoir layer.In this study,three approaches were considered for the Poisson's ratio and Young's modulus in the reservoir model:1)constant average values assigned to the entire reservoir,2)constant average values assigned to each layer,and 3)constant values assigned to each grid block.The validity of the model results was checked by history matching with production and pressure data.For the studied tight reservoir,the Poisson's ratio and Young's modulus significantly affected the permeability and porosity reduction with pressure depletion.The impact of Young's modulus was more pronounced than Poisson's ratio.The simulation results for oil rate,cumulative oil production,and water cut for the reservoir and a selected well showed that applying the three suggested geomechanical approaches resulted in a substantial discrepancy in the model outcome.In general,the coupled model with the mapped geomechanical properties resulted in lower oil and water production.This is attributed to the large values of mapped Young's modulus in parts of the reservoir which resulted in large permeability reduction and subsequently lower oil and water production is expected.In contrast lower Young's modulus per layer was obtained due to averaging pr

关键词： Tightreservoir Simulation Geomechanicsproperties Heterogeneity Compactioneffect Mechanical earth model

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In vitro and in vivo evaluation of cerium oxide nanoparticles in respiratory syncytial virus infection

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Bioactive Materials 2023年第6期24卷 124-135页

作者： Akhil Patel Jessica Kosanovich sameera Sansare Sricharani Balmuri Vinayak Sant Kerry M.Empey Shilpa Sant Department of Pharmaceutical Sciences School of PharmacyUniversity of PittsburghPittsburghPA15261USA Center for Clinical Pharmaceutical Sciences Department of Pharmacy and TherapeuticsSchool of PharmacyClinical and Translational Science InstituteDepartment of ImmunologySchool of MedicineUniversity of PittsburghPittsburghPA15261USA Department of Bioengineering Swanson School of EngineeringMcGowan Institute for Regenerative MedicineUPMC Hillman Cancer CenterUniversity of PittsburghPittsburghPA15261USA

Respiratory syncytial virus(RSV)is the most common cause of viral bronchiolitis among children worldwide,yet there is no vaccine for RSV disease.This study investigates the potential of cube and sphere-shaped cerium oxide nanoparticles(CNP)to modulate reactive oxygen(ROS)and nitrogen(RNS)species and immune cell phenotypes in the presence of RSV infection in vitro and in vivo.Cube and sphere-shaped CNP were synthesized by hydrothermal and ultrasonication methods,respectively.Physico-chemical characterization confirmed the shape of sphere and cube CNP and effect of various parameters on their particle size distribution and zeta potential.In vitro results revealed that sphere and cube CNP differentially modulated ROS and RNS levels in J774 macrophages.Specifically,cube CNP significantly reduced RSV-induced ROS levels without affecting RNS levels while sphere CNP increased RSV-induced RNS levels with minimal effect on ROS levels.Cube CNP drove an M1 phenotype in RSV-infected macrophages in vitro by increasing macrophage surface expression of CD80 and CD86 with a concomitant increase in TNFαand IL-12p70,while simultaneously decreasing M2 CD206 expression.Intranasal administration of sphere and cube-CNP were well-tolerated with no observed toxicity in BALB/c mice.Notably,cube CNP preferentially accumulated in murine alveolar macrophages and induced their activation,avoiding enhanced uptake and activation of other inflammatory cells such as neutrophils,which are associated with RSV-mediated inflammation.In conclusion,we report that sphere and cube CNP modulate macrophage polarization and innate cellular responses during RSV infection.

关键词： Cerium oxide nanoparticles Reactive oxygen species Respiratory syncytial virus Macrophage phenotypes Immunomodulation Nanoparticle shape Bioactive nanoparticles

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Designing an optimal stope layout for underground mining based on a heuristic algorithm

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International Journal of Mining Science and Technology 2015年第5期25卷 767-772页

作者： Sandanayake Don Suneth sameera Topal Erkan Asad Mohammad Waqar Ali Mining Engineering Western Australian School of MinesCurtin University

An optimal layout or three-dimensional spatial distribution of stopes guarantees the maximum profitability over life span of an underground mining operation.Thus,stope optimization is one of the key areas in underground mine planning practice.However,the computational complexity in developing an optimal stope layout has been a reason for limited availability of the algorithms offering solution to this problem.This article shares a new and efficient heuristic algorithm that considers a three-dimensional ore body model as an input,maximizes the economic value,and satisfies the physical mining and geotechnical constraints for generating an optimal stope layout.An implementation at a copper deposit demonstrates the applicability and robustness of the algorithm.A parallel processing based modification improving the performance of the original algorithm in terms of enormous computational time saving is also presented.

关键词：启发式算法采场布局地下开采布局设计三维矿体模型计算复杂性空间分布规划实践

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Identification,Isolation and Characterization of GaCyPI Gene in Gossypium arboreum under Cotton Leaf Curl Virus Disease Stress

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Phyton-International Journal of Experimental Botany 2021年第6期90卷 1613-1632页

作者： Zunaira Sher Muhammad Umair Majid sameera Hassan Fatima Batool Beenish Aftab Bushra Rashid Centre of Excellence in Molecular Biology University of the PunjabLahore53700Pakistan Department of Biological Sciences Faculty of Fisheries&Wild LifeUniversity of Veterinary and Animal Sciences-Ravi CampusPattoki55300Pakistan

Pakistan is facing the threat of Cotton Leaf Curl Virus(CLCuV)which is transmitted through whitefly to cotton crop.Molecular mechanism of leaf epicuticular wax protects the plants from different pathogens including insect attack and disease transmission.Objective of current study is the isolation and characterization of a wax related gene GaCyPI from Gossypium arboreum under CLCuV infection.A fragment of 475 bp was isolated from the total RNA and 3’and 5’RACE-PCR products were arranged by overlapping the extended sequences at both the ends.Deduced protein sequence of GaCyPI showed homology with Cyclophilin cis-trans isomerase gene of Gossypium ramondii and Gossypium barbadanse.Multiple sequence alignment also revealed homology among the coding sequences of same gene.GaCyPI protein comprised of 173 amino acids and ORF finder revealed the 69 bases upstream at 5’while 350 bp at 3’UTR.InterProScan revealed that it belongs to Cyclophilin-type peptidyl prolyl cis/trans isomerase(PPIase)family.Active sites are visible at specific amino acid positions and 3D structure was stable in Ramachandran plot.Prosa server showed protein residues have average 3D-1D score>=0.2 and Z-Score was−6.74.Phylogenetic analysis revealed that G.raimondii is the closest species that shares the same sequence.Hence,GaCyPI has strong role in plants’epicuticular wax and its genetic transformation may protect the cotton from whitefly which transmits CLCuV.

关键词： Cotton plant wax virus transmission cyclophilin gene family expressed sequence tag

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Analysis of trace dicyandiamide in stream water using solid phase extraction and liquid chromatography UV spectrometry

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Journal of Environmental Sciences 2015年第9期27卷 38-42页

作者： Huidong Qiu Dongdi Sun sameera R.Gunatilake Jinyan She Todd E.Mlsna Department of Chemistry and Chemical Engineering Chongqing University of Science and Technology Department of Chemistry Mississippi State University

An improved method for trace level quantification of dicyandiamide in stream water has been developed. This method includes sample pretreatment using solid phase extraction.The extraction procedure（including loading, washing, and eluting） used a flow rate of1.0 m L/min, and dicyandiamide was eluted with 20 m L of a methanol/acetonitrile mixture（V/V = 2：3）, followed by pre-concentration using nitrogen evaporation and analysis with high performance liquid chromatography–ultraviolet spectroscopy（HPLC–UV）. Sample extraction was carried out using a Waters Sep-Pak AC-2 Cartridge（with activated carbon）.Separation was achieved on a ZIC-Hydrophilic Interaction Liquid Chromatography（ZIC-HILIC）（50 mm × 2.1 mm, 3.5 μm） chromatography column and quantification was accomplished based on UV absorbance. A reliable linear relationship was obtained for the calibration curve using standard solutions（R^2〉 0.999）. Recoveries for dicyandiamide ranged from 84.6% to 96.8%, and the relative standard deviations（RSDs, n = 3） were below 6.1% with a detection limit of 5.0 ng/m L for stream water samples.

关键词： Dicyandiamide Solid phase extraction Stream water samples High performance liquid chromatography–ultraviolet spectrometry

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