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About 338,693 results

The Ligand Free Palladium(II)-Catalyzed Regioselective 1,2-Addition of Enol Silanes to ...
https://doi.org/10.1021/acs.joc.1c00857
The Journal of Organic Chemistry; Polimera SR, A M Subbaiah M et. al.

Sep 24th, 2021 - In contrast to the conventional 1,4-addition process, regioselective 1,2-addition of silyl enol ethers to quinones can now be achieved via a palladium(II) enolate pathway that provides access to 4-hydroxy-4-(2-oxo-2-arylethyl)cyclohexa-2,5-dien-1-one derivatives. This quinone alkylation protocol proceeds under mild reaction conditions at ambient temperature under open air and does not require e...

Synthesis of 7-Chloroquinoline Derivatives Using Mixed Lithium-Magnesium Reagents.
https://doi.org/10.1021/acs.joc.1c01521
The Journal of Organic Chemistry; Murie VE, Nicolino PV et. al.

Sep 24th, 2021 - We have prepared a library of functionalized quinolines through the magnesiation of 7-chloroquinolines under mild conditions, employing both batch and continuous flow conditions. The preparation involved the generation of mixed lithium-magnesium intermediates, which were reacted with different electrophiles. Mixed lithium-zinc reagents allowed the synthesis of halogenated and arylated derivativ...

Ginger metabolites and metabolite-inspired synthetic products modulate intracellular ca...
https://doi.org/10.1152/ajplung.00271.2021
American Journal of Physiology. Lung Cellular and Molecul... Lukovic E, Perez-Zoghbi JF et. al.

Sep 23rd, 2021 - Asthma affects millions of people worldwide and its prevalence is increasing. It is characterized by chronic airway inflammation, airway remodeling, and pathologic bronchoconstriction, and it poses a continuous treatment challenge with very few new therapeutics available. Thus, many asthmatics turn to plant-based complementary products, including ginger, for better symptom control, indicating a...

A screen of kinase inhibitors reveals a potential role of Chk1 in regulating Hydra head...
https://doi.org/10.1387/ijdb.210087yl
The International Journal of Developmental Biology; Lee Y, Muddaluru V et. al.

Sep 23rd, 2021 - The cnidarian Hydra possesses remarkable regenerative capabilities which allows it to regrow lost or damaged body parts in a matter of days. Given that many key regulators of regeneration and development are evolutionarily conserved, Hydra is a valuable model system for studying the fundamental molecular mechanisms underlying these processes. In the past, kinase inhibitors have been useful tool...

The adult heart requires baseline expression of the transcription factor Hand2 to withs...
https://doi.org/10.1093/cvr/cvab299
Cardiovascular Research; Videira RF, Koop AMC et. al.

Sep 23rd, 2021 - Research on the pathophysiology of right ventricular (RV) failure has, in spite of the associated high mortality and morbidity, lagged behind compared to the left ventricle (LV).Previous work from our lab revealed that the embryonic basic helix-loop-helix transcription factor heart and neural crest derivatives expressed-2 (Hand2) is re-expressed in the adult heart and activates a 'fetal gene pr...

Inflammation during the life cycle of the atherosclerotic plaque.
https://doi.org/10.1093/cvr/cvab303
Cardiovascular Research; Libby P

Sep 23rd, 2021 - Inflammation orchestrates each stage of the life cycle of atherosclerotic plaques. Indeed, inflammatory mediators likely link many traditional and emerging risk factors with atherogenesis. Atheroma initiation involves endothelial activation with recruitment of leukocytes to the arterial intima, where they interact with lipoproteins or their derivatives that have accumulated in this layer. The p...

Hepatic global DNA Hypomethylation Phenotype in Rainbow Trout Fed Diets Varying in Carb...
https://doi.org/10.1093/jn/nxab343
The Journal of Nutrition; Liu J, Heraud C et. al.

Sep 23rd, 2021 - A high carbohydrate-low protein diet can induce hepatic global DNA hypomethylation in trout. The mechanisms remain unclear. We aimed to investigate whether increase in dietary carbohydrates (dHC) or decrease in dietary proteins (dLP) can cause hepatic global DNA hypomethylation, and to explore the underlying mechanisms in trout. Two feeding trials were conducted on juvenile males, both of which...

Quantitative Electrophysiological Evaluation of the Analgesic Efficacy of Two Lappaconi...
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Neuroscience Bulletin; Teng G, Zhang F et. al.

Sep 23rd, 2021 - Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development. Lappaconitine (LA), a potent analgesic drug extracted from the root of natural Aconitum species, has been clinically used for years because of its effective analgesic and non-addictive properties. However, being limited t...

Pembrolizumab-induced autoimmune haemolytic anemia in a patient with chronic lymphocyti...
https://doi.org/10.1136/bcr-2021-245350
BMJ Case Reports; Yun NK, Alrifai T et. al.

Sep 23rd, 2021 - We present a unique case of a patient with a long-standing history of indolent chronic lymphocytic leukaemia (CLL) who suddenly developed autoimmune haemolytic anaemia after starting immune checkpoint inhibitor therapy for bladder cancer. He had no clear indication to start CLL-directed treatment based on current clinical practice guidelines; however, targeted treatment of CLL with ibrutinib pr...

Evidence of Artemisinin-Resistant Malaria in Africa.
https://doi.org/10.1056/NEJMoa2101746
The New England Journal of Medicine; Balikagala B, Fukuda N et. al.

Sep 23rd, 2021 - In the six Southeast Asian countries that make up the Greater Mekong Subregion, Plasmodium falciparum has developed resistance to derivatives of artemisinin, the main component of first-line treatments for malaria. Clinical resistance to artemisinin monotherapy in other global regions, including Africa, would be problematic. In this longitudinal study conducted in Northern Uganda, we treated pa...

Multi-level inhibition of coronavirus replication by chemical ER stress.
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Nature Communications; Shaban MS, Müller C et. al.

Sep 22nd, 2021 - Coronaviruses (CoVs) are important human pathogens for which no specific treatment is available. Here, we provide evidence that pharmacological reprogramming of ER stress pathways can be exploited to suppress CoV replication. The ER stress inducer thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types including primary differentiated ...

Diversity-Oriented Synthesis of Spiropyrrolo1,2-aisoquinoline Derivatives via Diastereo...
https://doi.org/10.1021/acs.joc.1c01544
The Journal of Organic Chemistry; Toumi A, Boudriga S et. al.

Sep 22nd, 2021 - An efficient diastereoselective route is developed to get access to novel spiropyrrolo[1,2-a]isoquinoline-oxindole skeletons by a one-pot three-component [3 + 2] cycloaddition reaction of (Z)-5-arylidene-1,3-thiazolidine-2,4-diones, isatin derivatives, and 1,2,3,4-tetrahydroisoquinoline (THIQ). Interestingly, the regioselectivity of the reaction is both temperature- and solvent-dependent, allow...

Construction of a Pyrimidine Framework through 3 + 2 + 1 Annulation of Amidines, Ketone...
https://doi.org/10.1021/acs.joc.1c01847
The Journal of Organic Chemistry; Qin Z, Ma Y et. al.

Sep 21st, 2021 - An efficient, facile, and eco-friendly synthesis of pyrimidine derivatives has been developed. It involves a [3 + 2 + 1] three-component annulation of amidines, ketones, and one carbon source. N,N-Dimethylaminoethanol is oxidized through C(sp3)-H activation to provide the carbon donor. One C-C and two C-N bonds are formed during the oxidative annulation process. The reaction shows good toleranc...

Latent Class Analysis Reveals COVID-19-related ARDS Subgroups with Differential Respons...
https://doi.org/10.1164/rccm.202105-1302OC
American Journal of Respiratory and Critical Care Medicine; Sinha P, Furfaro D et. al.

Sep 21st, 2021 - Rationale Two distinct subphenotypes have been identified in acute respiratory distress syndrome (ARDS), but the presence of subgroups in ARDS associated with COVID-19 is unknown. The objective of this study was to identify clinically relevant, novel subgroups in COVID-19-related ARDS, and compare them to previously described ARDS subphenotypes. Methods Eligible participants were adults with CO...

A potential diagnostic serum immunological marker panel to differentiate between primar...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8452079
PloS One; Rankothgedera S, Atukorala I et. al.

Sep 21st, 2021 - Inflammation contributes to knee osteoarthritis (KOA) where many immunological mediators participate in its initiation and progression. Most clinicians manage primary (pKOA) and secondary osteoarthritis (sKOA) alike. Whether immunological profiles of pKOA and sKOA differ remains obscure. Hence, we aimed to differentially identify potential serum immunologic diagnostic markers of pKOA and of sKO...

Cost utility analysis of Remdesivir and Dexamethasone treatment for hospitalised COVID-...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8449700
BMC Health Services Research; Carta A, Conversano C

Sep 20th, 2021 - Sars-Cov-2 is a novel corona virus associated with significant morbidity and mortality. Remdesivir and Dexamethasone are two treatments that have shown to be effective against the Sars-Cov-2 associated disease. However, a cost-effectiveness analysis of the two treatments is still lacking. The cost-utility of Remdesivir, Dexamethasone and a simultaneous use of the two drugs with respect to stand...

Organoselenium-chitosan derivative: Synthesis via "click" reaction, characterization an...
https://doi.org/10.1016/j.ijbiomac.2021.09.053
International Journal of Biological Macromolecules; Nornberg AB, de Aquino TFB et. al.

Sep 20th, 2021 - The derivatization of chitosan (CS) is widely exploited to endow this polysaccharide with enhanced physicochemical and biological properties. Beyond the synthetic route, the nature of the compounds used to functionalize the CS-derivatives exerts a pivotal role in their final properties. Making use of a simple "click" reaction, we synthesized for the first time an organoselenium-CS derivative th...

Current neurologic treatment and emerging therapies in CDKL5 deficiency disorder.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8447578
Journal of Neurodevelopmental Disorders; Olson HE, Daniels CI et. al.

Sep 18th, 2021 - CDKL5 deficiency disorder (CDD) is associated with refractory infantile onset epilepsy, global developmental delay, and variable features that include sleep, behavioral disturbances, and movement disorders. Current treatment is primarily symptom-based and informed by experience in caring for this population. We describe medication and non-medication approaches to treatment of epilepsy and addit...

Usefulness of the prostate health index in predicting the presence and aggressiveness o...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8447777
BMC Urology; Kim JY, Yu JH et. al.

Sep 18th, 2021 - We aimed to evaluate the usefulness of the Beckman Coulter prostate health index (PHI) and to compare it with total prostate-specific antigen (PSA) levels and related derivatives in predicting the presence and aggressiveness of prostate cancer (PCa) in the Korean population. A total of 140 men who underwent their first prostate biopsy for suspected PCa were included in this prospective observat...

Click-to-lead design of a picomolar ABA receptor antagonist with potent activity in vivo.
https://doi.org/10.1073/pnas.2108281118
Proceedings of the National Academy of Sciences of the Un... Vaidya AS, Peterson FC et. al.

Sep 18th, 2021 - Abscisic acid (ABA) is a key plant hormone that mediates both plant biotic and abiotic stress responses and many other developmental processes. ABA receptor antagonists are useful for dissecting and manipulating ABA's physiological roles in vivo. We set out to design antagonists that block receptor-PP2C interactions by modifying the agonist opabactin (OP), a synthetically accessible, high-affin...