keyword
MENU ▼
Read by QxMD icon Read
search

oxazolone

keyword
https://www.readbyqxmd.com/read/29400411/design-synthesis-and-biological-evaluation-of-novel-1-2-diaryl-4-substituted-benzylidene-5-4h-imidazolone-derivatives-as-cytotoxic-agents-and-cox-2-lox-inhibitors
#1
Phoebe F Lamie, John N Philoppes, Lucie Rárová
A new series of 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives 4a-l was synthesized. Their structures were confirmed by different spectroscopic techniques (IR, 1 H NMR, DEPT-Q NMR, and mass spectroscopy) and elemental analyses. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also normal human skin fibroblasts. Cyclooxygenase (COX)-1, COX-2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX-2 rather than COX-1, and the IC50 values (0...
February 5, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29395580/a-lamellar-body-mimetic-system-for-the-treatment-of-oxazolone-induced-atopic-dermatitis-in-hairless-mice
#2
Verónica Moner, Estibalitz Fernández, Ana Cristina Calpena, Adriana Garcia-Herrera, Mercedes Cócera, Olga López
BACKGROUND: Atopic dermatitis is a common skin disease characterized by a Th2 cell-dominant inflammatory infiltrate, elevated serum IgE levels and impaired epidermal barrier function. It is associated to abnormal epidermal lamellar body secretion, producing alteration in lipid composition and extracellular lamellar membrane organization. OBJECTIVES: The oxazolone-induced atopic dermatitis in hairless mice was used to evaluate in vivo the effect of the application of a lipid system that mimics the morphology, structure and composition of epidermal lamellar bodies...
January 30, 2018: Journal of Dermatological Science
https://www.readbyqxmd.com/read/29392979/characterization-of-acetylated-histidine-b1-ion-structure-a-competition-between-oxazolone-and-side-chain-imidazole-moiety
#3
Kranthikumar Yadav, J Laxmikanth Rao, R Srinivas, R Nagaraj, M V Jagannadham
The detection of post-translational modifications of proteins is an important comprehensive research area. Over the years, proteomic studies involving protein acetylation have attracted a great deal of attention. In the present study, we have focussed on the acetylation of histidine and the intrinsic stability of b1-ion of oxazolone ring and/or with side chain imidazole bicyclic product. The formation of oxazolone structure may occur when an amino moiety undergoes acetylation reaction and when it is present in the vicinity of the side chain imidazole moiety...
January 1, 2018: European Journal of Mass Spectrometry
https://www.readbyqxmd.com/read/29386485/juniperus-chinensis-fruits-attenuate-oxazolone-and-2-4-dinitrochlorobenzene-induced-atopic-dermatitis-symptoms-in-mice
#4
Jonghwan Jegal, No-June Park, Sang-A Park, Sim-Kyu Bong, Hyun Jegal, Su-Nam Kim, Min Hye Yang
Juniperus chinensis, commonly Chinese juniper, has been used for treating inflammatory diseases. This study aimed to investigate anti-atopic dermatitis (AD) effects of standardized J. chinensis fruits extract on murine oxazolone- and 2,4-dinitrochlorobenzene (DNCB)-induced models of AD. Ear swelling, epidermis thickening, and eosinophils infiltration in the oxazolone-mediated dermatitis of BALB/c mice were significantly reduced upon topical application of J. chinensis fruits 95% EtOH extract (JCE). Besides, transdermal administration of JCE to SKH-1 hairless mice inhibited the development of DNCB-induced AD-like skin lesions by suppressing transepidermal water loss and improving skin hydration...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29365216/insight-into-metal-removal-from-peptides-that-sequester-copper-for-methane-oxidation
#5
Arnaud Basle, Abdelnasser El Ghazouani, Jaeick Lee, Christopher Dennison
Methanobactins (Mbns) are modified peptides that sequester copper (Cu) methanotrophs use to oxidize methane. Limited structural information is available for this class of natural products, as is an understanding of how cells utilize Mbn-bound Cu. The crystal structure of Methylosinus sporium NR3K Cu(I)-Mbn provides further information about the structural diversity of Mbns and the first insight into their Cu-release mechanism. Nitrogen ligands from oxazolone and pyrazinedione rings chelate Cu(I) along with adjacent thioamides...
January 24, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29363669/histamine-drives-severity-of-innate-inflammation-via-histamine-4-receptor-in-murine-experimental-colitis
#6
J B Wechsler, A Szabo, C L Hsu, R A Krier-Burris, H A Schroeder, M Y Wang, R G Carter, T E Velez, L M Aguiniga, J B Brown, M L Miller, B K Wershil, T A Barrett, P J Bryce
Ulcerative colitis (UC) patients exhibit elevated histamine, but how histamine exacerbates disease is unclear as targeting histamine 1 receptor (H1R) or H2R is clinically ineffective. We hypothesized that histamine functioned instead through the other colon-expressed histamine receptor, H4R. In humans, UC patient biopsies exhibited increased H4R RNA and protein expression over control tissue, and immunohistochemistry showed that H4R was in proximity to immunopathogenic myeloperoxidase-positive neutrophils. To characterize this association further, we employed both the oxazolone (Ox)- and dextran sulfate sodium (DSS)-induced experimental colitis mouse models and also found upregulated H4R expression...
January 24, 2018: Mucosal Immunology
https://www.readbyqxmd.com/read/29353040/eupatilin-an-activator-of-ppar%C3%AE-inhibits-the-development-of-oxazolone-induced-atopic-dermatitis-symptoms-in-balb-c-mice
#7
Yujung Jung, Jin-Chul Kim, No-June Park, Sim-Kyu Bong, Sullim Lee, Hyun Jegal, Li Tai Jin, Sang Moo Kim, Yong Kee Kim, Su-Nam Kim
Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is the main lipophilic flavonoid obtained from the Artemisia species. Eupatilin has been reported to have anti-apoptotic, anti-oxidative and anti-inflammatory activities. Previously, we found that eupatilin increases transcriptional activity and expression of peroxisome proliferator-activated receptor α (PPARα) in a keratinocyte cell line and acts as an agonist of PPARα. PPARα agonists ameliorate atopic dermatitis (AD) and restore the skin barrier function...
January 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29330048/b-cell-activation-in-the-cecal-patches-during-the-development-of-an-experimental-colitis-model
#8
Taro Watabe, Takashi Nagaishi, Naoya Tsugawa, Yudai Kojima, Nisha Jose, Akinori Hosoya, Michio Onizawa, Yasuhiro Nemoto, Shigeru Oshima, Tetsuya Nakamura, Hajime Karasuyama, Takahiro Adachi, Mamoru Watanabe
Although previous studies have suggested that appendix seems to be involved in the colitis, the role of this in the pathogenesis remains unclear. In this study, we assessed the importance of appendiceal lymphoid follicles, specifically the cecal patches (CP) in mice, using an experimental colitis model. Treatment with oxazolone resulted in ulcerations particularly at CP with follicular expansion as well as colitis. The colitis was attenuated by either appendectomy or the absence of mature B cells. We therefore established an intravital imaging system accompanied by the fluorescence resonance energy transfer technology to analyze the dynamic immune response of CP B cells...
January 9, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29329002/integration-of-multi-scale-molecular-modeling-approaches-with-experiments-for-the-in-silico-guided-design-and-discovery-of-novel-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives-and-analysis-of-their-potential-restrictive-effects-on-cell
#9
Serdar Durdagi, Busecan Aksoydan, Ismail Erol, Isik Kantarcioglu, Yavuz Ergun, Gulay Bulut, Melih Acar, Timucin Avsar, George Liapakis, Vlasios Karageorgos, Ramin E Salmas, Barış Sergi, Sara Alkhatib, Gizem Turan, Berfu Nur Yigit, Kutay Cantasir, Bahar Kurt, Turker Kilic
AT1 antagonists is the most recent drug class of molecules against hypertension and they mediate their actions through blocking detrimental effects of angiotensin II (A-II) when acts on type I (AT1) A-II receptor. The effects of AT1 antagonists are not limited to cardiovascular diseases. AT1 receptor blockers may be used as potential anti-cancer agents - due to the inhibition of cell proliferation stimulated by A-II. Therefore, AT1 receptors and the A-II biosynthesis mechanisms are targets for the development of new synthetic drugs and therapeutic treatment of various cardiovascular and other diseases...
December 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29281784/determining-linear-free-energy-relationships-in-peptide-fragmentation-using-derivatization-and-targeted-mass-spectrometry
#10
Yuanyuan Shen, Reza Nemati, Lei Wang, Xudong Yao
The sequence complexity of proteome is utilized with rational, chemical derivatization for establishing the linear free energy relationship (LFER) to investigate collision-induced dissociation (CID) of peptides. The derivatization produces groups of peptides that have a varying designer residue of aliphatic amino acid at the N-terminus, but stay invariable for the rest of sequences that are naturally occurring, uncontrolled. Collisional fragmentation of the derivatized peptides is advantageously monitored by liquid chromatography-multiple reaction monitoring mass spectrometry...
December 27, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29258854/ameliorative-effects-of-juniperus-rigida-fruit-on-oxazolone-and-2-4-dinitrochlorobenzene-induced-atopic-dermatitis-in-mice
#11
Sullim Lee, No-June Park, Sim-Kyu Bong, Jonghwan Jegal, Sang-A Park, Su-Nam Kim, Min-Hye Yang
ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Juniperus rigida have been used in Korean traditional medicine for the treatment of inflammatory diseases in humans such as rheumatoid arthritis. AIM OF THE STUDY: This study aimed to investigate the anti-atopic properties of J. rigida fruit in in vivo murine atopic dermatitis (AD) models. METHODS AND RESULTS: BALB/c mouse ears ad SKH-1 hairless mice stimulated with oxazolone (4 weeks) and DNCB (3 weeks), respectively, were treated with the 1% Juniperus rigida fruit EtOH extract (JFE)...
December 16, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29236214/neural-network-modeling-of-ache-inhibition-by-new-carbazole-bearing-oxazolones
#12
Levent Cavas, Gamze Topcam, Cevher Gundogdu-Hizliates, Yavuz Ergun
Acetylcholine esterase (AChE) is one of the targeted enzymes in the therapy of important neurodegenerative diseases such as Alzheimer's disease. Many studies on carbazole- and oxazolone-based compounds have been conducted in the last decade due to the importance of these compounds. New carbazole-bearing oxazolones were synthesized from several carbazole aldehydes and p-nitrobenzoyl glycine as AChE inhibitors by the Erlenmeyer reaction in the present study. The inhibitory effects of three carbazole-bearing oxazolone derivatives on AChE were studied in vitro and the experimental results were modeled using artificial neural network (ANN)...
December 13, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/29225517/intestinally-restricted-janus-kinase-inhibition-a-potential-approach-to-maximize-the-therapeutic-index-in-inflammatory-bowel-disease-therapy
#13
David T Beattie, M Teresa Pulido-Rios, Fei Shen, Melissa Ho, Eva Situ, Pam R Tsuruda, Patrick Brassil, Melanie Kleinschek, Sharath Hegde
Background: An unmet need remains for safe and effective treatments to induce and maintain remission in inflammatory bowel disease (IBD) patients. The Janus kinase (JAK) inhibitor, tofacitinib, has demonstrated robust efficacy in ulcerative colitis patients although, like other systemic immunosuppressants, there may be safety concerns associated with its use. This preclinical study evaluated whether modulating intestinal inflammation via local JAK inhibition can provide efficacy without systemic immunosuppression...
2017: Journal of Inflammation
https://www.readbyqxmd.com/read/29206209/dioscorea-quinqueloba-ameliorates-oxazolone-and-2-4-dinitrochlorobenzene-induced-atopic-dermatitis-symptoms-in-murine-models
#14
Jonghwan Jegal, No-June Park, Sim-Kyu Bong, Hyun Jegal, Su-Nam Kim, Min Hye Yang
Dioscorea quinqueloba has been used for food substances, as well as in herbal medicines for allergic diseases such as asthma. This study aimed to investigate the anti-atopic dermatitis (AD) effects of the total extract of D. quinqueloba rhizomes and active fractionson murine oxazolone- and 2,4-dinitrochlorobenzene-induced models of AD. Specific AD symptoms, such as erythema, ear swelling, and epidermis thickening, were significantly reduced in the oxazolone-mediated AD BALB/c mice upon topical application of D...
December 5, 2017: Nutrients
https://www.readbyqxmd.com/read/29205369/regulatory-b-cells-induced-by-ultraviolet-b-through-toll-like-receptor-4-signalling-contribute-to-the-suppression-of-contact-hypersensitivity-responses-in-mice
#15
Xiaoming Liu, Haiyan Huang, Hongbin Gao, Xia Wu, Wei Zhang, Bo Yu, Xia Dou
BACKGROUND: Ultraviolet (UV) B irradiation is known to suppress contact hypersensitivity (CHS) responses in mouse models by suppressing immune responses. However, the cellular mechanisms responsible for UVB-induced systemic suppression remain unclear. Regulatory B cells have been reported to play an inhibitory role during CHS. It is presently unknown whether regulatory B cells contribute to the effect of UVB phototherapy. OBJECTIVE: To investigate the inductive effect of UVB on regulatory B cells and the underlying mechanisms by using a CHS mouse model...
December 5, 2017: Contact Dermatitis
https://www.readbyqxmd.com/read/29156380/structure-based-design-of-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives
#16
Busecan Aksoydan, Isik Kantarcioglu, Ismail Erol, Ramin Ekhteiari Salmas, Serdar Durdagi
Angiotensin II receptor type 1 (AT1) antagonists are the most recent drug class against hypertension. Recently first crystal structure of AT1 receptor is deposited to the protein data bank (PDB ID: 4YAY). In this work, several molecular screening methods such as molecular docking and de novo design studies were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan molecules at the binding site of the AT1 receptor...
October 18, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29116551/anti-inflammatory-effect-of-a-novel-locally-acting-a2a-receptor-agonist-in-a-rat-model-of-oxazolone-induced-colitis
#17
L Antonioli, A El-Tayeb, C Pellegrini, M Fornai, O Awwad, G Giustarini, G Natale, L Ryskalin, Z H Németh, C E Müller, C Blandizzi, R Colucci
Adenosine represents a powerful modulating factor, which has been shown to orchestrate the scope, duration, and remission of the inflammatory response through the activation of four specific receptors, classified as A1, A2A, A2B, and A3, all being widely expressed in a variety of immune cells. Several selective A2A receptor agonists have displayed anti-inflammatory effects, through the suppression of IL-12, TNF, and IFN-γ production by monocytes and lymphocytes, in the setting of chronic intestinal inflammation...
November 8, 2017: Purinergic Signalling
https://www.readbyqxmd.com/read/29057517/the-indane-diastereoisomers-ph2-and-ph5-divergence-between-their-effects-in-delayed-type-hypersensitivity-models-and-a-model-of-colitis
#18
Neil H Frankish, Brendan McHale, Helen Sheridan
OBJECTIVES: Compounds PH2 and PH5 are distereoisomers of novel indane compounds, synthesised as analogues of secondary metabolites of the fern, Onychium. In this study, we compare their effects on a variety of inflammatory models. METHODS: In an effort to extend our knowledge of their anti-inflammatory profile, we have investigated their activity in two models of delayed-type hypersensitivity (DTH); the methylated bovine serum albumin model (mBSA) and the oxazolone contact hypersensitivity (CHS) model, on IL2 release from Jurkat cells and in the dextran sulphate sodium (DSS) murine model of inflammatory bowel disease...
October 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29049008/exogenous-murine-antimicrobial-peptide-cramp-significantly-exacerbates-ovalbumin-induced-airway-inflammation-but-ameliorates-oxazolone-induced-intestinal-colitis-in-balb-c-mice
#19
Yang Li, Xiaojie Chu, Cunbao Liu, Weiwei Huang, Yufeng Yao, Ye Xia, Pengyan Sun, Qiong Long, Xuejun Feng, Kui Li, Xu Yang, Hongmei Bai, Wenjia Sun, Yanbing Ma
Cathelicidin has been reported to be multifunctional. The current study aimed to investigate the influences of exogenous cathelicidin-related antimicrobial peptide (CRAMP) on inflammatory responses in different disease models. In OVA-induced allergic airway inflammation, CRAMP significantly enhanced the infiltration of inflammatory cells and accumulation of proinflammatory Th2 cytokine IL-13 and IL-33 in bronchial alveolar lavage fluid (BALF), exacerbated lung tissue inflammation and airway goblet cell hyperplasia, and elevated OVA-specific IgE level in serum...
October 19, 2017: Human Vaccines & Immunotherapeutics
https://www.readbyqxmd.com/read/29043360/synthesis-photophysical-and-biological-properties-of-a-new-oxazolone-fluorescent-probe-for-bioimaging-an-experimental-and-theoretical-study
#20
Przemysław Krawczyk, Beata Jędrzejewska, Piotr Cysewski, Tomasz Janek
In this study, a new oxazolone derivative 4-{N,N-bis[2-phenyl-4-benzylidene-1,3-oxazol-5(4H)-one]amino}benzaldehyde (PB3) was synthesized and investigated as a fluorescent dye. The spectroscopic properties in different solvents were thoroughly studied. The experimental data were supported by quantum-chemical calculations using density functional theory. Measurements and theoretical calculations showed that the PB3 dye is characterized by non-monotonic solvatochromism, a strongly polar charge transfer excited state, a large Stokes' shift, a high fluorescence quantum yield and a high fluorescence lifetime...
October 31, 2017: Organic & Biomolecular Chemistry
keyword
keyword
69240
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"