2,355 results match your criteria synthesize series


Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors.

Eur J Med Chem 2021 Sep 11;226:113845. Epub 2021 Sep 11.

Weifang Medical University, No.7166 Baotong Road, Weifang, 261053, PR China. Electronic address:

To resolve the problem of drug resistance caused by epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer, we used the principle of collocation to design and synthesize a series of aminopyrimidine derivatives with 4,5,6,7-tetrahydrothieno [3,2-c]pyridine side chains (according to the binding mode of AZD9291 to EGFR) for use as EGFR kinase inhibitors. The most promising compound A12, a non-covalently bound reversible inhibitor, showed excellent kinase inhibitory activity against EGFR, with an IC value of 4.0 nM and more than 42-fold selectivity for EGFR (IC = 170. Read More

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September 2021

Transition metal-catalyzed synthesis of new 3-substituted coumarin derivatives as antibacterial and cytostatic agents.

Future Med Chem 2021 Sep 17. Epub 2021 Sep 17.

Faculty of Chemical Engineering & Technology, Department of Organic Chemistry, University of Zagreb, Marulićev trg 20, HR-10000, Zagreb, Croatia.

The aim of this study was to synthesize new coumarin-based compounds and evaluate their antibacterial and antitumor potential. Using transition metal-catalyzed reactions, a series of 7-hydroxycoumarin derivatives were synthesized with aliphatic and aryl moiety attached directly at C-3 of the coumarin ring and through the ethynyl or 1,2,3-triazole linker. The 3-substituted coumarin derivative bearing bistrifluoromethylphenyl at the C-4 position of 1,2,3-triazole () showed strong and selective antiproliferative activity against cervical carcinoma cells. Read More

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September 2021

A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice.

Eur J Med Chem 2021 Sep 13;226:113827. Epub 2021 Sep 13.

Division of Life Science, State Key Laboratory of Molecular Neuroscience and Molecular Neuroscience Center, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China; Hong Kong Center for Neurodegenerative Diseases, Hong Kong Science Park, Hong Kong, China; Guangdong Provincial Key Laboratory of Brain Science, Disease and Drug Development, Shenzhen-Hong Kong Institute of Brain Science, HKUST Shenzhen Research Institute, Shenzhen, Guangdong, 518057, China. Electronic address:

Cholinergic neurons are ubiquitous and involved in various higher brain functions including learning and memory. Patients with Alzheimer's disease exhibit significant dysfunction and loss of cholinergic neurons. Meanwhile, such cholinergic deficits can be potentially relieved pharmacologically by increasing acetylcholine. Read More

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September 2021

Post-Mastectomy Pain Syndrome: An Up-to-Date Review of Treatment Outcomes.

JPRAS Open 2021 Dec 11;30:97-109. Epub 2021 Aug 11.

Division of Plastic and Reconstructive Surgery, Northwestern University Feinberg School of Medicine, Chicago, Illinois.

Background: Post-mastectomy pain syndrome (PMPS) is a known debilitating surgical complication. While research on prevention, risk factors, and treatments have been conducted, there remains no cohesive treatment paradigm. The aim of our study is to synthesize the existing evidence on PMPS treatment, which may facilitate the implementation of standardized, effective management strategies. Read More

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December 2021

Hierarchical N-doped CNTs grafted onto MOF-derived porous carbon nanomaterials for efficient oxygen reduction.

J Colloid Interface Sci 2021 Aug 28;606(Pt 2):1833-1841. Epub 2021 Aug 28.

School of Materials and Energy, Guangdong University of Technology, Guangzhou, PR China.

The rational design and preparation of nonprecious metal-based oxygen reduction reaction (ORR) catalysts to facilitate electron and mass transport are of great significance in oxygen-involved energy applications. Herein, a stepwise approach to synthesize a type of hierarchically porous N-doped carbon nanotubes (CNTs) grafted onto zinc-based coordination polymer derived carbon nanomaterials (M-NCNT, M = Fe/Co/Ni) is proposed. At first, an isostructural zinc-based metal-organic framework (MOF) to HKUST-1(Cu) (ZnHKUST-1) is solvothermally prepared, and then under pyrolysis to obtain MOF-derived porous carbon. Read More

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Spatially Graded Millimeter Sized MoWS Monolayer Alloys: Synthesis and Memory Effect.

ACS Appl Mater Interfaces 2021 Sep 8. Epub 2021 Sep 8.

Tianjin Key Laboratory of Photoelectric Materials and Devices, School of Materials Science and Engineering, Tianjin University of Technology, Tianjin 300384, P. R. China.

The band gap engineering of two-dimensional (2D) transition metal dichacogenides (TMDs) could significantly broaden their applications, especially in electronics and optoelectronics. Alloying is a more effective approach to synthesize 2D ternary TMD materials with tunable bandgaps by regulating the compositions. Whether the alloying could induce memory effects is of interest as a scientific problem and worthy to be studied. Read More

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September 2021

Immune checkpoint inhibitor administration during pregnancy: a case series.

ESMO Open 2021 Sep 3;6(5):100262. Epub 2021 Sep 3.

Department of Clinical Therapeutics, School of Medicine, National and Kapodistrian University of Athens, Athens, Greece. Electronic address:

Background: Immune checkpoint inhibitors have been widely implemented in current clinical practice. Although cancer occurs in ∼1 out of 1000 pregnancies, treatment remains challenging. Until now, limited data exist regarding immunotherapy administration during pregnancy. Read More

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September 2021

C1'-Branched acyclic nucleoside phosphonates mimicking adenosine monophosphate: Potent inhibitors of Trypanosoma brucei adenine phosphoribosyltransferase.

Eur J Med Chem 2021 Aug 25;225:113798. Epub 2021 Aug 25.

Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic. Electronic address:

Some pathogens, including parasites of the genus Trypanosoma causing Human and Animal African Trypanosomiases, cannot synthesize purines de novo and they entirely rely on the purine salvage pathway (PSP) for their nucleotide generation. Thus, their PSP enzymes are considered as promising drug targets, sparsely explored so far. Recently, a significant role of acyclic nucleoside phosphonates (ANPs) as inhibitors of key enzymes of PSP, namely of 6-oxopurine phosphoribosyltransferases (PRTs), has been discovered. Read More

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Synthesis of α-l-Araf and β-d-Galf series furanobiosides using mutants of a GH51 α-l-arabinofuranosidase.

Bioorg Chem 2021 Aug 8;116:105245. Epub 2021 Aug 8.

TBI, Université de Toulouse, CNRS, INRAE, INSA, Toulouse, France. Electronic address:

The GH-51 α-l-arabinofuranosidase from Thermobacillus xylanilyticus (TxAbf) possesses versatile catalytic properties, displaying not only the ability to hydrolyze glycosidic linkages but also to synthesize furanobiosides in α-l-Araf and β-d-Galf series. Herein, mutants are investigated to evaluate their ability to perform self-condensation, assessing both yield improvements and changes in regioselectivity. Overall yields of oligo-α-l-arabino- and oligo-β-d-galactofuranosides were increased up to 4. Read More

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Synthesis of chlorogenic acid and p-coumaroyl shikimate by expressing shikimate gene modules in Escherichia coli.

J Appl Microbiol 2021 Sep 1. Epub 2021 Sep 1.

Department of Bioscience and Biotechnology, Bio/Molecular Informatics Center, Konkuk University, Seoul, Republic of Korea.

Aim: Chlorogenic acid and p-coumaroyl shikimate are hydroxycinnamic acid derivatives. These compounds are nutraceutical supplements due to their biological activities including prevention of cardiovascular disease and cancers. These two compounds were synthesized in Escherichia coli through two-culture system using two mutants, which are biochemically interdependent. Read More

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September 2021

Synthesis and Antibacterial Activities of Amidine Substituted Monocyclic β-Lactams.

Med Chem 2021 Aug 30. Epub 2021 Aug 30.

Ningxia Centre of Organic Synthesis and Engineering Technology, Ningxia Academy of Agriculture and Forestry Sciences, No. 590, Huanghe East Road, Jinfeng District, Yinchuan, Ningxia 750002. China.

Background: Mononcyclic β-lactams are regarded as the most resistant class of β-lactams against a series of β-lactamases though possess limited antibacterial activity. Aztreonam being the first clinically approved monobactam needs broad-spectrum efficacy through structural modification.

Objective: We strive to synthesize a number of monocyclic β-lactams by varying the substituents at N1, C3 and C4 positions of azetidinone ring and study the antimicrobial effect on variable bacterial strains. Read More

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Synthesis and Bio-evaluation of 2-Alkyl Substituted Fluorinated Genistein Analogues Against Breast Cancer.

Med Chem 2021 Aug 29. Epub 2021 Aug 29.

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, China.

Background: Breast cancer is the leading cause of cancer death in women. The current methods of chemotherapy for breast cancer generally have strong adverse reactions and drug resistance. Therefore, the discovery of novel anti-breast cancer lead compounds is urgently needed. Read More

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Organotin (IV) complexes with sulphonyl hydrazide moiety. Design, synthesis, characterization, docking studies, cytotoxic and anti-leishmanial activity.

J Biomol Struct Dyn 2021 Aug 30:1-11. Epub 2021 Aug 30.

Department of Pharmacy, Faculty of Biological Sciences, University of Malakand, Chakdara, Khyber Pakhtunkhwa, Pakistan.

Due to a lack of therapeutic options for the pathological condition of leishmaniasis, which is characterized by polymorphic lesions and skin surface infections, Leishmania genus parasites damaged dermis and mucosa. There was a need to synthesize and characterize some new complexes. This study evaluated the biological activities preferably anti-Leishmanial activity of organotin (IV) containing sulphonyl hydrazide derivatives. Read More

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Discovery of Oral Anticancer 1,2-Bis(hydroxymethyl)benzo[]pyrrolo[2,1-]phthalazine Hybrids That Inhibit Angiogenesis and Induce DNA Cross-Links.

J Med Chem 2021 Sep 30;64(17):12469-12486. Epub 2021 Aug 30.

Institute of Biomedical Sciences, Academia Sinica, Taipei 11529, Taiwan.

Designing hybrid molecules with dual functions is one approach to improve the therapeutic efficacy of combination treatment. We have previously conjugated phthalazine and bis(hydroxymethyl)pyrrole pharmacophores to form hybrids bearing antiangiogenesis and DNA interstrand cross-linking activities. To improve the bioavailability, we adopted a benzology approach to design and synthesize a new series of 1,2-bis(hydroxymethyl)benzo[]pyrrolo[2,1-]phthalazines. Read More

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September 2021

Acute Disseminated Encephalomyelitis and Acute Hemorrhagic Leukoencephalitis Following COVID-19: Systematic Review and Meta-synthesis.

Neurol Neuroimmunol Neuroinflamm 2021 11 27;8(6). Epub 2021 Aug 27.

From the Division of Neuroimmunology and Neuroinfectious Diseases (G.S.M., C.R.S.M., F.J.M., S.K.H.), Department of Neurology, Massachusetts General Hospital, Boston, MA; and Department of Pathology (M.M.-L.), Massachusetts General Hospital, Boston, MA.

Background And Objectives: Since the onset of the COVID-19 pandemic, a growing number of reports have described cases of acute disseminated encephalomyelitis (ADEM) and acute hemorrhagic leukoencephalitis (AHLE) following infection with COVID-19. Given their relatively rare occurrence, the primary objective of this systematic review was to synthesize their clinical features, response to treatments, and clinical outcomes to better understand the nature of this neurologic consequence of COVID-19 infection.

Methods: Patients with a history of COVID-19 infection were included if their reports provided adequate detail to confirm a diagnosis of ADEM or AHLE by virtue of clinical features, radiographic abnormalities, and histopathologic findings. Read More

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November 2021

Myxedema Psychosis: Systematic Review and Pooled Analysis.

Neuropsychiatr Dis Treat 2021 18;17:2713-2728. Epub 2021 Aug 18.

Department of Health Care Sciences, Center for Clinical Research and Management Education, Dresden International University, Dresden, Germany.

Background And Objective: The term myxedema psychosis (MP) was introduced to describe the occurrence of psychotic symptoms in patients with untreated hypothyroidism, but the optimal assessment and treatment of this condition are unclear. We aimed to synthesize data from the literature to characterize the clinical presentation and management of MP.

Methods: We performed a systematic review according to the PRISMA (preferred reporting items for systematic reviews and meta-analyses) guidelines in PubMed (Medline), Embase, Google Scholar, and Cochrane databases, including observational studies, case series, and case reports published from 1/1/1980 to 31/12/2019 in the English language. Read More

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Comparative Study of a Series of Tc(CO) Mannosylated Dextran Derivatives for Sentinel Lymph Node Detection.

Molecules 2021 Aug 7;26(16). Epub 2021 Aug 7.

Institute of Nuclear and Radiological Sciences and Technology, Energy & Safety, NCSR "Demokritos", 15310 Athens, Greece.

Sentinel lymph node detection (SLND) is rapidly entering common practice in the management of patients with tumors. The introduction of mannose molecules to Tc-labeled dextrans, so far, showed that the sentinel node could trap these agents due to their recognition by the mannose receptors of lymph node macrophages. The current study aimed to synthesize, characterize, and biologically evaluate a series of mannosylated dextran derivatives labeled with Tc for potential use in SLND. Read More

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Active mobility, active participation: a systematic review of modified ride-on car use by children with disabilities.

Disabil Rehabil Assist Technol 2021 Aug 26:1-15. Epub 2021 Aug 26.

College of Public Health and Human Sciences, Oregon State University, Corvallis, OR, USA.

Background: Modified ride-on cars (MROC) are a low-cost option to provide self-directed mobility to children with mobility limitations, in lieu of or as a precursor to other powered mobility devices.

Objectives: We appraised evidence to (1) describe and categorize MROC study characteristics, (2) synthesize existing knowledge of children's use of MROCs and (3) frame outcomes within the International Classification of Functioning, Disability and Health (ICF) framework.

Methods: Articles were identified through four electronic databases: Medline, CINAHL, PsycNET, and Web of Science. Read More

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A review of remdesivir for COVID-19 in pregnancy and lactation.

J Antimicrob Chemother 2021 Aug 24. Epub 2021 Aug 24.

Division of Respirology, Mount Sinai Hospital, Toronto, ON, Canada.

Mounting evidence suggests that pregnant people have an elevated risk of severe COVID-19-related complications compared with their non-pregnant counterparts, underscoring the need for effective prevention and treatment strategies. However, despite progress in innovative and flexible trial designs during the COVID-19 pandemic, regressive policies excluding pregnant and breastfeeding people from biomedical research persist. Remdesivir, a broad-spectrum antiviral, was the first drug licensed for the treatment of COVID-19, based on data showing it reduced the time to recovery in hospitalized patients. Read More

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Interventions for palliative symptom control in COVID-19 patients.

Cochrane Database Syst Rev 2021 08 23;8:CD015061. Epub 2021 Aug 23.

Department of Palliative Care, Medical Center - University of Freiburg, Faculty of Medicine, University of Freiburg, Freiburg, Germany.

Background: Individuals dying of coronavirus disease 2019 (COVID-19) may experience distressing symptoms such as breathlessness or delirium. Palliative symptom management can alleviate symptoms and improve the quality of life of patients. Various treatment options such as opioids or breathing techniques have been discussed for use in COVID-19 patients. Read More

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Pneumothorax in otherwise healthy non-intubated patients suffering from COVID-19 pneumonia: a systematic review.

J Thorac Dis 2021 Jul;13(7):4519-4529

Department of Thoracic Surgery, Saint-Pierre University Hospital, Université Libre de Bruxelles (ULB), Brussels, Belgium.

Background: Cases of spontaneous pneumothorax have been described in patients suffering from coronavirus disease 2019 (COVID-19) pneumonia. The aim of this study is to systematically review all the cases of spontaneous pneumothorax that occurred in healthy patients with no underlying lung disease and who did not receive invasive mechanical ventilation.

Methods: A PubMed research was conducted. Read More

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Evolution in the Acute Management of Open Fracture Treatment? Part 1.

J Orthop Trauma 2021 Sep;35(9):449-456

Department of Orthopaedic Surgery, University of Southern California, Los Angeles, CA.

Introduction: Despite decades of advancement in wound debridement, prophylactic antibiotic therapy, fracture stabilization, and soft tissue reconstruction, infection remains a serious complication after open fracture. Inconclusive historical data and new challenges with resistant organisms and antimicrobial stewardship having created a difficult environment within which to develop sound, evidence-based treatment protocols that can be applied universally. The first part of this 2-part series will synthesize the historical perspective along with the current concepts surrounding bacteriology and antibiotic use/stewardship. Read More

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September 2021

From Co-MOF to CoNi-MOF to Ni-MOF: A Facile Synthesis of 1D Micro-/Nanomaterials.

Inorg Chem 2021 Sep 19;60(17):13168-13176. Epub 2021 Aug 19.

School of Chemistry and Chemical Engineering, Institute for Innovative Materials and Energy, Yangzhou University, Yangzhou 225002, Jiangsu, P. R. China.

Controlling the growth of metal-organic frameworks (MOFs) at the micro-/nanoscopic scale will result in new physical properties and novel functions into the materials without changing the chemical identities and the characteristic features of the MOFs themselves. Herein, we report a facile approach to synthesize a series of MOFs [Co-MOF, CoNi-MOFs ( and represent the molar ratio of Co and Ni and / = 1:1, 1:5, 1:10, 1:15, and 1:20), and Ni-MOF] with a one-dimensional micro-/nanoscaled rod-like architecture. From Co-MOF to CoNi-MOFs to Ni-MOF, the diameters of the rods turn to be spindly with the increase of Ni content which will facilitate the supercapacitor performances. Read More

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September 2021

Introduction-First Billion Years: Habitability.

Astrobiology 2021 08;21(8):893-905

Planetary Habitability Laboratory, University of Puerto Rico Arecibo, Arecibo, Puerto Rico.

The physical processes active during the first billion years (FBY) of Earth's history, such as accretion, differentiation, and impact cratering, provide constraints on the initial conditions that were conducive to the formation and establishment of life on Earth. This motivated the Lunar and Planetary Institute's FBY topical initiative, which was a four-part conference series intended to look at each of these physical processes to study the basic structure and composition of our Solar System that was set during the FBY. The FBY Habitability conference, held in September 2019, was the last in this series and was intended to synthesize the initiative; specifically, to further our understanding of the origins of life, planetary and environmental habitability, and the search for life beyond Earth. Read More

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Discovery of Quinoxaline-Based P1-P3 Macrocyclic NS3/4A Protease Inhibitors with Potent Activity against Drug-Resistant Hepatitis C Virus Variants.

J Med Chem 2021 Aug 18;64(16):11972-11989. Epub 2021 Aug 18.

Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, Worcester, Massachusetts 01605, United States.

The three pan-genotypic HCV NS3/4A protease inhibitors (PIs) currently in clinical use-grazoprevir, glecaprevir, and voxilaprevir-are quinoxaline-based P2-P4 macrocycles and thus exhibit similar resistance profiles. Using our quinoxaline-based P1-P3 macrocyclic lead compounds as an alternative chemical scaffold, we explored structure-activity relationships (SARs) at the P2 and P4 positions to develop pan-genotypic PIs that avoid drug resistance. A structure-guided strategy was used to design and synthesize two series of compounds with different P2 quinoxalines in combination with diverse P4 groups of varying sizes and shapes, with and without fluorine substitutions. Read More

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Design, synthesis, and SAR study of novel 4,5-dihydropyrazole-Thiazole derivatives with anti-inflammatory activities for the treatment of sepsis.

Eur J Med Chem 2021 Aug 8;225:113743. Epub 2021 Aug 8.

Key Laboratory of Metabolism and Regulation for Major Diseases of Anhui Higher Education Institutes, College of Food and Biological Engineering, Hefei University of Technology, Hefei, China. Electronic address:

Systemic inflammatory response syndrome is a major feature of sepsis which is one of the major causes of death worldwide. It has been reported that 3,5-diaryl-4,5-dihydropyrazole and thiazole derivatives have many biological functions, especially in the aspect of anti-inflammation. According to the strategy of pharmacophore combination, we introduced thiazole moiety into dihydropyrazole skeleton to design and synthesize a novel series of 2-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-methylthiazole derivatives, and evaluated their anti-inflammatory activities for sepsis treatment. Read More

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A Multi-Catalytic Sensing for Hydrogen Peroxide, Glucose, and Organophosphorus Pesticides Based on Carbon Dots.

Front Chem 2021 12;9:713104. Epub 2021 Jul 12.

College of Materials Science and Engineering, Huaqiao University, Xiamen, China.

In this work, a facile one-pot hydrothermal route was employed to synthesize a series of fluorescent carbon dots (CDs) by using 20 natural amino acids, respectively, as the starting materials. It was found that the CDs synthesized using phenylalanine could possess the intrinsic peroxidase-like activity that could effectively catalyze a traditional peroxidase substrate like 3, 3', 5, 5'- tetramethylbenzidine (TMB) in the presence of HO to produce a blue solution; thereby, a catalytic sensing system for HO has been developed. On the basis of this catalytic reaction, together with the fact that glucose oxidase (GOx) can catalyze the hydrolysis of glucose to generate HO, a sensitive catalytic sensing system for glucose could be further established. Read More

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Transoesophageal echocardiography in cardiac arrest: A systematic review.

Resuscitation 2021 Aug 12. Epub 2021 Aug 12.

Teesside University, Middlesbrough, United Kingdom; Royal Victoria Infirmary, Newcastle upon Tyne, UK.

Aims: To identify, appraise and synthesize all available clinical evidence to evaluate the diagnostic role of transoesophageal echocardiography (TEE) during resuscitation of in-hospital (IHCA) and out-of-hospital cardiac arrest (OHCA) in the identification of reversible causes of cardiac arrest and cardiac contractility.

Methods: We conducted a systematic review following PRISMA guidelines. Medline, EMBASE, Web of Science Core Collection, Proquest Dissertations, Open Grey, CDSR, Cochrane Central, Cochrane Clinical Answers, and the clinicaltrials. Read More

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In Situ Synthesis of Robust Polyvinylpyrrolidone-Based Perovskite Nanocrystal Powders by the Fiber-Spinning Chemistry Method and Their Versatile 3D Printing Patterns.

ACS Appl Mater Interfaces 2021 Aug 12;13(33):39748-39754. Epub 2021 Aug 12.

State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemical Engineering, Jiangsu Key Laboratory of Fine Chemicals and Functional Polymer Materials, Nanjing Tech University, No. 5 Xin Mofan Road, Nanjing 210009, P. R. China.

All-inorganic halide perovskite nanocrystals (PNCs) have received increasing attention due to their excellent optical properties. However, the inherent instability and the large amount of volatile organic compounds during the production process have severely limited their applications. In this research, we employed the microfluidic electrostatic spinning method to synthesize polyvinylpyrrolidone (PVP)-based PNC (CsPbBr/PVP) powders directly by spinning chemistry, where the fibers serve as reactors. Read More

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Introducing A New Class of Sulfonyl Fluoride Hubs via Radical Chloro-Fluorosulfonylation of Alkynes.

Angew Chem Int Ed Engl 2021 Aug 11. Epub 2021 Aug 11.

Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University), State Key Laboratory of Photocatalysis on Energy and Environment, College of Chemistry, Fuzhou University, Fuzhou, 350108, China.

Sulfonyl fluorides have widespread applications in many important fields, including ligation chemistry, chemical biology, and drug discovery. Therefore, new methods to increase the synthetic efficiency and expand the available structures of sulfonyl fluorides are highly in demand. Here, we introduce a new and powerful class of sulfonyl fluoride hubs, β-chloro alkenylsulfonyl fluorides (BCASF), which can be constructed via radical chloro-fluorosulfonyl difunctionalization of alkynes under photoredox conditions. Read More

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