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Adam A Wallace et al.
The journal of physical chemistry. A, 124(38), 7768-7775 (2020-08-28)
We report a photoelectron imaging study of gas-phase deprotonation of isoxazole in which spectroscopic data are compared to the results of electronic structure calculations for the anion products corresponding to each of three possible deprotonation sites. The observed photoelectron spectra
Laura E Jennings et al.
Bioorganic & medicinal chemistry, 26(11), 2937-2957 (2018-05-20)
Ligands for the bromodomain and extra-terminal domain (BET) family of bromodomains have shown promise as useful therapeutic agents for treating a range of cancers and inflammation. Here we report that our previously developed 3,5-dimethylisoxazole-based BET bromodomain ligand (OXFBD02) inhibits interactions
Afnan A Matti et al.
Bioorganic & medicinal chemistry letters, 23(21), 5931-5935 (2013-09-18)
Microwave accelerated reaction system (MARS) technology provided a good method to obtain selective and open isoxazole ligands that bind to and inhibit the Sxc- antiporter. The MARS provided numerous advantages, including: shorter time, better yield and higher purity of the
Nikolai V Rostovskii et al.
The Journal of organic chemistry, 82(1), 256-268 (2016-12-16)
4-Aminopyrrole-3-carboxylates and pyrazine-2-carboxylates were synthesized from 5-alkoxyisoxazoles and 1-sulfonyl-1,2,3-triazoles by tuning the Rh(II) catalyst and the reaction conditions. The reaction in chloroform at 100 °C under Rh
Sahaya Asirvatham et al.
Anti-inflammatory & anti-allergy agents in medicinal chemistry, 14(2), 128-137 (2015-08-13)
A series of newer 3-(4'-methoxyphenyl)-5-substituted phenylisoxazoles derivatives have been synthesized by reacting hydroxylamine hydrochloride with chalcones. The chalcones were formed by reacting different aromatic aldehydes with 4-methoxyacetophenone in presence of aqueos potassium hydroxide (KOH). The purity of all the synthesized
Cesira de Chiara et al.
Nature chemical biology, 16(6), 686-694 (2020-03-24)
The broad-spectrum antibiotic D-cycloserine (DCS) is a key component of regimens used to treat multi- and extensively drug-resistant tuberculosis. DCS, a structural analog of D-alanine, binds to and inactivates two essential enzymes involved in peptidoglycan biosynthesis, alanine racemase (Alr) and
Ting Geng et al.
The journal of physical chemistry. A, 124(20), 3984-3992 (2020-04-04)
The excited state relaxation pathways of isoxazole and oxazole upon excitation with UV-light were investigated by nonadiabatic ab initio dynamics simulations and time-resolved photoelectron spectroscopy. Excitation of the bright ππ*-state of isoxazole predominantly leads to ring-opening dynamics. Both the initially
Sebastian Markmiller et al.
Cell, 172(3), 590-604 (2018-01-27)
Stress granules (SGs) are transient ribonucleoprotein (RNP) aggregates that form during cellular stress and are increasingly implicated in human neurodegeneration. To study the proteome and compositional diversity of SGs in different cell types and in the context of neurodegeneration-linked mutations
Martin G Jaeger et al.
Nature genetics, 52(7), 719-727 (2020-06-03)
The Mediator complex directs signals from DNA-binding transcription factors to RNA polymerase II (Pol II). Despite this pivotal position, mechanistic understanding of Mediator in human cells remains incomplete. Here we quantified Mediator-controlled Pol II kinetics by coupling rapid subunit degradation
Sreejith J Nair et al.
Nature structural & molecular biology, 26(3), 193-203 (2019-03-06)
A crucial feature of differentiated cells is the rapid activation of enhancer-driven transcriptional programs in response to signals. The potential contributions of physicochemical properties of enhancer assembly in signaling events remain poorly understood. Here we report that in human breast
Scott Boitano et al.
PloS one, 9(6), e99140-e99140 (2014-06-14)
Protease-activated receptor-2 (PAR2) is a G-Protein Coupled Receptor (GPCR) activated by proteolytic cleavage to expose an attached, tethered ligand (SLIGRL). We evaluated the ability for lipid-tethered-peptidomimetics to activate PAR2 with in vitro physiological and Ca2+ signaling assays to determine minimal
Danilo Russo et al.
Water research, 169, 115203-115203 (2019-11-02)
The photodegradation process of methylisothiazolinone (MIT), benzisothiazolinone (BIT), and isoxazole (ISOX) in ultrapure water and synthetic wastewater by means of UV254 photolysis and by UV254/H2O2 advanced oxidation process were investigated in a microcapillary photoreactor designed for ultrafast photochemical transformation of
Nenad Joksimović et al.
Bioorganic chemistry, 105, 104343-104343 (2020-10-22)
Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also
Adam A Wallace et al.
The journal of physical chemistry. A, 125(1), 317-326 (2020-12-29)
Electron capture by the σ* LUMO of isoxazole triggers the dissociation of the O-N bond and the opening of the ring. Photodetachment of the resulting anion accesses a neutral structure, in which the O· and ·N bond fragments interact through
Mingxing Wang et al.
Journal of molecular graphics & modelling, 84, 18-28 (2018-05-25)
Studies on human genetics have implicated the voltage-gated sodium channel Nav1.7 as an appealing target for the treatment of pain. In this study, we put forward a ligand-based pharmacophore for the first time, which was generated by a set of
Ilaria Lampronti et al.
Oncology letters, 20(5), 151-151 (2020-09-17)
In order to develop potential anticancer agents stimulating apoptosis, novel 3,4-isoxazolediamide and 4,5,6,7-tetrahydro-isoxazolo-[4,5-c]-pyridine derivatives have been synthetized. The original structures of geldanamycin and radicicol, which are known natural heat shock protein (HSP) inhibitors, were deeply modified because both of them
Marina N Semenova et al.
ACS combinatorial science, 20(12), 700-721 (2018-11-20)
A series of both novel and reported combretastatin analogues, including diarylpyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles, were synthesized via improved protocols to evaluate their antimitotic antitubulin activity using in vivo sea urchin embryo assay and a panel of human cancer cells.
Chao Li et al.
Frontiers in pharmacology, 11, 1247-1247 (2020-09-29)
Cardiometabolic diseases are characterized as a combination of multiple risk factors for cardiovascular disease (CVD) and metabolic diseases including diabetes mellitus and dyslipidemia. Cardiometabolic diseases are closely associated with cell glucose and lipid metabolism, inflammatory response and mitochondrial function. Farnesoid
Margarita Gutiérrez et al.
The Journal of pharmacy and pharmacology, 65(12), 1796-1804 (2013-11-05)
Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of Alzheimer's disease. In this study, nine isoxazoles derivatives were tested for their in-vitro AChE activity. The molecular docking showed the interaction of the compounds with the active site.
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