Tertiary alkylamines as nucleophiles in substitution reactions at heteroaromatic halide during the synthesis of the highly potent pirinixic acid derivative 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS-121) [PDF]
, 2011 YS-121 [2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid] is the result of target-oriented structural derivatization of pirinixic acid.
Gabler, Matthias +3 more
core +1 more source
15–Lipoxygenase inhibition of Commelina benghalensis, Tradescantia fluminensis, Tradescantia zebrina
Asian Pacific Journal of Tropical Biomedicine, 2014 Objective: To evaluate the 15-lipoxygenase inhibitory activity of the methanol leaf extracts of Commelina benghalensis, Tradescantia fluminensis (T. fluminensis) and Tradescantia zebrina.
Cean Socorro M. Alaba +1 more
doaj +1 more source
A high throughput screen identifies potent and selective inhibitors to human epithelial 15-lipoxygenase-2. [PDF]
PLoS ONE, 2014 Lipoxygenase (LOX) enzymes catalyze the hydroperoxidation of arachidonic acid and other polyunsaturated fatty acids to hydroxyeicosatetraenoic acids with varying positional specificity to yield important biological signaling molecules.
J Brian Jameson +8 more
doaj +1 more source
Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase [PDF]
, 2014 Caulerpenyne (CYN) is a sesquiterpene from green algae with known inhibitory properties against soybean lipoxygenase. Here we introduce a detailed structure-activity study elucidating the inhibitory effects of CYN and a library of six synthetic CYN ...
Phillipp Richter +17 more
core +1 more source
Novel Human Lipoxygenase Inhibitors Discovered Using Virtual Screening with Homology Models [PDF]
, 2016 We report the discovery of new, low micromolar, small molecule inhibitors of human platelet-type 12- and reticulocyte 15-lipoxygenase-1 (12-hLO and 15-hLO) using structure-based methods.
Matthew P. Jacobson (174588) +4 more
core +5 more sources
Annals of Clinical and Translational Neurology, EarlyView.ABSTRACT Background Ischemic stroke, a major cause of mortality and long‐term disability, results from the abrupt cessation of cerebral blood flow due to vascular occlusion or rupture. Icosapent Ethyl (EPA‐EE), approved for hypertriglyceridemia, has anti‐inflammatory and antithrombotic properties that may lessen ischemic damage.
Mitra Mahmoudi Meymand +5 more
wiley +1 more source
Pakistan Journal of Pharmaceutical SciencesBackground: Synthesis of novel enzyme inhibitors and antioxidants is active research in pharmaceuticals sciences. Novel compounds with potential therapeutic value can be synthesized to help the body combat oxidative-stress related diseases.
Muneeb Yousuf +4 more
doaj +1 more source
Comparison of eight 15-lipoxygenase (LO) inhibitors on the biosynthesis of 15-LO metabolites by human neutrophils and eosinophils. [PDF]
PLoS ONE, 2018 Neutrophils and eosinophils are important sources of bioactive lipids from the 5- and the 15-lipoxygenase (LO) pathways. Herein, we compared the effectiveness of humans eosinophils and eosinophil-depleted neutrophils to synthesize 15-LO metabolites using
Anne-Sophie Archambault +10 more
doaj +1 more source
Inhibitors of Human 5-Lipoxygenase Potently Interfere With Prostaglandin Transport
Frontiers in Pharmacology, 2022 5-Lipoxygenase (5-LO) is the key enzyme in the formation of pro-inflammatory leukotrienes (LT) which play an important role in a number of inflammatory diseases.
Astrid S. Kahnt +14 more
doaj +1 more source
Arzneistofftarget-5-Lipoxygenase : ein neuer Enzymaktivierungsweg mit Einfluss auf die Wirksamkeit von Inhibitoren [PDF]
, 2005 Leukotriene (LT) sind bioaktive Lipidmediatoren, die in einer Vielzahl von Entzündungskrankheiten wie z.B. Asthma, Psoriasis, Arthritis oder allergische Rhinitis involviert sind.
Fischer, Lutz
core