Microbial Metabolite Inspired β-Peptide Polymers Displaying Potent and Selective Antifungal Activity.
Sign Up to like & getrecommendations! Published in 2022 at "Advanced science"
DOI: 10.1002/advs.202104871
Abstract: Potent and selective antifungal agents are urgently needed due to the quick increase of serious invasive fungal infections and the limited antifungal drugs available. Microbial metabolites have been a rich source of antimicrobial agents and… read more here.
Keywords: potent selective; antifungal activity; pdap; selective antifungal ... See more keywords
Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200577
Abstract: Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecule inhibitors lack selectivity or suffer from low bioactivity. To address this limitation, a… read more here.
Keywords: design synthesis; derivatives potent; quinazolin one; selective inhibitors ... See more keywords
Nucleobase Modified Adefovir (PMEA) Analogues as Potent and Selective Inhibitors of Adenylate Cyclases from Bordetella pertussis and Bacillus anthracis
Sign Up to like & getrecommendations! Published in 2018 at "ChemMedChem"
DOI: 10.1002/cmdc.201800332
Abstract: A series of 13 acyclic nucleoside phosphonates (ANPs) as bisamidate prodrugs was prepared. Five compounds were found to be non‐cytotoxic and selective inhibitors of Bordetella pertussis adenylate cyclase toxin (ACT) in J774A.1 macrophage cell‐based assays.… read more here.
Keywords: potent selective; adenylate cyclases; bacillus anthracis; bordetella pertussis ... See more keywords
Discovery of a Class of Potent and Selective Non‐competitive Sentrin‐Specific Protease 1 Inhibitors
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DOI: 10.1002/cmdc.202000067
Abstract: Sentrin‐specific proteases (SENPs) are responsible for the maturation of small ubiquitin‐like modifiers (SUMOs) and the deconjugation of SUMOs from their substrate proteins. Studies on prostate cancer revealed an overexpression of SENP1, which promotes prostate cancer… read more here.
Keywords: discovery class; potent selective; prostate cancer; sentrin specific ... See more keywords
Spirooxindol‐1,3‐oxazine Alkaloids: Highly Potent and Selective Antitumor Agents Evolved from Iterative Structure Optimization
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200162
Abstract: Spirooxindole‐1,3‐oxazines are a small and structurally unique class of spirooxindole alkaloids. To date, only four of these compounds have been isolated from natural sources, and their biological properties remained unknown thus far. Dioxyreserpine is a… read more here.
Keywords: highly potent; oxazine alkaloids; spirooxindol oxazine; alkaloids highly ... See more keywords
Design, Synthesis, and Optimization of Indole Acetic Acid Derivatives as Potent and Selective CRTH2 Receptor Antagonists: Discovery of ACT‐774312
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202300007
Abstract: Herein we report the structure‐activity relationship (SAR) studies and optimization of new highly potent and selective CRTH2 receptor antagonists as potential follow‐ups of our previous reported clinical candidate setipiprant (ACT‐129968) for the treatment of respiratory… read more here.
Keywords: act; acetic acid; selective crth2; crth2 receptor ... See more keywords
Identification of a potent and selective gametocytocidal antimalarial agent from the stem barks of Lophira lanceolata.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103321
Abstract: Bioassay-guided fractionation of the organic extract obtained from stem barks of the African plant Lophira lanceolata has led to the isolation of seven biflavonoids, including the new α'-chlorolophirone E (5) and 5'-chlorolophirone D (6). Among… read more here.
Keywords: agent; potent selective; stem barks; lophira lanceolata ... See more keywords
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2
Sign Up to like & getrecommendations! Published in 2021 at "Cell Chemical Biology"
DOI: 10.1016/j.chembiol.2021.04.020
Abstract: The COVID-19 pandemic has been disastrous to society and effective drugs are urgent needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (SCoV2) is indispensable for viral replication and represents a putative target for pharmacological intervention.… read more here.
Keywords: development potent; potent selective; like protease; papain like ... See more keywords
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.04.006
Abstract: A series of diverse small molecules have been designed and synthesized through structure-based drug design by taking advantage of fragment merging and elaboration approaches. Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and… read more here.
Keywords: potent selective; brd4 inhibitors; airway inflammation; brd4 ... See more keywords
4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.06.047
Abstract: Human Diphtheria toxin-like ADP-ribosyltranferases (ARTD) 10 is an enzyme carrying out mono-ADP-ribosylation of a range of cellular proteins and affecting their activities. It shuttles between cytoplasm and nucleus and influences signaling events in both compartments,… read more here.
Keywords: potent selective; benzamides potent; artd10; phenoxy benzyloxy ... See more keywords
Discovery of potent and selective inhibitors of the Escherichia coli M1-aminopeptidase via multicomponent solid-phase synthesis of tetrazole-peptidomimetics.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.11.074
Abstract: The Escherichia coli neutral M1-aminopeptidase (ePepN) is a novel target identified for the development of antimicrobials. Here we describe a solid-phase multicomponent approach which enabled the discovery of potent ePepN inhibitors. The on-resin protocol, developed… read more here.
Keywords: potent selective; discovery potent; escherichia coli; aminopeptidase ... See more keywords