A novel class of 1,4-disubstituted 1,2,3-triazoles: Regioselective synthesis, antimicrobial activity and molecular docking studies
Sign Up to like & getrecommendations! Published in 2020 at "Arabian Journal of Chemistry"
DOI: 10.1016/j.arabjc.2020.10.026
Abstract: Abstract A Novel class of 1,4-disubstituted 1,2,3-triazoles have been synthesized in good to excellent yields via Cu(I) accelerated azide-alkyne click chemistry reaction strategy. The newly synthesized compounds were assessed for their in vitro antimicrobial activity… read more here.
Keywords: disubstituted triazoles; antimicrobial activity; chemistry; class disubstituted ... See more keywords
Synthesis and antibacterial evaluation of 13-substituted cycloberberine derivatives as a novel class of anti-MRSA agents.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.050
Abstract: A series of new 13-substituted cycloberberine (CBBR) derivatives were prepared and evaluated for their antibacterial activities against Gram-positive bacteria taking CBBR as the lead. Structure-activity relationship revealed that the introduction of a suitable electron-donating group… read more here.
Keywords: substituted cycloberberine; anti mrsa; derivatives novel; mrsa agents ... See more keywords
Pyrrole-2 carboxamides - A novel class of insect ryanodine receptor activators.
Sign Up to like & getrecommendations! Published in 2021 at "Pesticide biochemistry and physiology"
DOI: 10.1016/j.pestbp.2021.104798
Abstract: The ryanodine receptor (RyR) is an intracellular calcium channel critical to the regulation of insect muscle contraction and the target site of diamide insecticides such as chlorantraniliprole, cyantraniliprole and flubendiamide. To-date, diamides are the only… read more here.
Keywords: receptor; ryanodine receptor; novel class; pyrrole carboxamides ... See more keywords
A novel class of cardioprotective small-molecule PTP inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Pharmacological research"
DOI: 10.1016/j.phrs.2019.104548
Abstract: Ischemia/reperfusion (I/R) injury is mediated in large part by opening of the mitochondrial permeability transition pore (PTP). Consequently, inhibitors of the PTP hold great promise for the treatment of a variety of cardiovascular disorders. At… read more here.
Keywords: ptp opening; small molecule; cypd; novel class ... See more keywords
APPLICABILITY OF NOVEL, CLASS ACTIVATION MAPS (CAM) IN THE DEVELOPMENT OF ARTIFICIAL INTELLIGENCE-GUIDED, SINGLE AND 12-LEAD ECG TO DETECT ST-ELEVATION MYOCARDIAL INFARCTION
Sign Up to like & getrecommendations! Published in 2020 at "Journal of the American College of Cardiology"
DOI: 10.1016/s0735-1097(20)34101-2
Abstract: Convolutional Neural Networks (CNN) are seamlessly integrated into many fields, including image recognition. CAM are able to recognize specific regions of images for their classification. We applied CAM and discovered discriminative segments for the detection… read more here.
Keywords: applicability novel; guided single; class activation; activation maps ... See more keywords
A Novel Class IIb Bacteriocin-Plantaricin EmF Effectively Inhibits Listeria monocytogenes and Extends the Shelf Life of Beef in Combination with Chitosan.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.1c06269
Abstract: Plantaricin EmF separated and identified from L. plantarum 163 was a novel class IIb bacteriocin. The molecular masses of plantaricin Em and F were 1638 and 3702 Da, respectively, with amino acid sequences FNRGGYNFGKSVRH and… read more here.
Keywords: shelf life; class iib; novel class; plantaricin emf ... See more keywords
Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00338
Abstract: The activation of Homo sapiens Casein lysing protease P (HsClpP) by a chemical or genetic strategy has been proved to be a new potential therapy in acute myeloid leukemia (AML). However, limited efficacy has been… read more here.
Keywords: novel class; ring opening; strategy; opening strategy ... See more keywords
Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00517
Abstract: Leishmaniasis is a neglected tropical disease that is estimated to afflict over 12 million people. Current drugs for leishmaniasis suffer from serious deficiencies, including toxicity, high cost, modest efficacy, primarily parenteral delivery, and emergence of… read more here.
Keywords: novel class; discovery optimization; optimization tambjamines; antileishmanial agents ... See more keywords
Tetrahydropyrazolopyridinones as a Novel Class of Potent and Highly Selective LIMK Inhibitors
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.5c00974
Abstract: LIMKs are serine/threonine and tyrosine kinases that play critical roles in regulating actin filament turnover, affecting key cellular processes such as cytoskeletal remodeling, proliferation and migration. Aberrant LIMK overactivation has been implicated in several diseases,… read more here.
Keywords: class potent; novel class; selective limk; limk ... See more keywords
Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00232
Abstract: Autotaxin (ATX) catalyzes the hydrolysis of lysophosphatidylcholine (LPC) generating the lipid mediator lysophosphatidic acid (LPA). Both ATX and LPA are involved in various pathological inflammatory conditions, including fibrosis and cancer, and have attracted great interest… read more here.
Keywords: atx; fibrosis; autotaxin; hydroxamic acids ... See more keywords
Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01356
Abstract: Tuberculosis is the leading cause of death worldwide from infectious diseases. With the development of drug-resistant strains of Mycobacterium tuberculosis, there is an acute need for new medicines with novel modes of action. Herein, we… read more here.
Keywords: profiling hydantoins; identification profiling; dpre1; hydantoins novel ... See more keywords