Ethyl 5-methyl-4-oxo-3-phenyl-2-propyl­amino-3,4-dihydro­thieno[2,3-d]pyrimidine-6-carboxyl­ate

The title compound, C19H21N3O3S, was synthesized via the aza-Wittig reaction of functionalized imino­phospho­rane with phenyl isocyanate under mild conditions. In the mol­ecule, the fused thienopyrimidine ring system is essentially planar, with a maximum deviation of 0.072 (2) Å, and makes a dihedral angle of 60.11 (9)° with the phenyl ring. An intra­molecular C—H⋯O hydrogen bond is present. The crystal packing is stabilized by inter­molecular N—H⋯O and C—H⋯O hydrogen bonds

The development status of specialized nursing in ostomy care both in China and abroad

AbstractThe status of ostomy-specialized nurses' training and the specialized care for patients with permanent colostomy both in China and abroad are analyzed. Based on features and characteristics of the development of ostomy care outside China, problems in China's ostomy care are discussed to promote the sustainable development of this type of care

Co-targeting of DNA, RNA, and protein molecules provides optimal outcomes for treating osteosarcoma and pulmonary metastasis in spontaneous and experimental metastasis mouse models.

Metastasis is a major cause of mortality for cancer patients and remains as the greatest challenge in cancer therapy. Driven by multiple factors, metastasis may not be controlled by the inhibition of single target. This study was aimed at assessing the hypothesis that drugs could be rationally combined to co-target critical DNA, RNA and protein molecules to achieve "saturation attack" against metastasis. Independent actions of the model drugs DNA-intercalating doxorubicin, RNA-interfering miR-34a and protein-inhibiting sorafenib on DNA replication, RNA translation and protein kinase signaling in highly metastatic, human osteosarcoma 143B cells were demonstrated by the increase of γH2A.X foci formation, reduction of c-MET expression and inhibition of Erk1/2 phosphorylation, respectively, and optimal effects were found for triple-drug combination. Consequently, triple-drug treatment showed a strong synergism in suppressing 143B cell proliferation and the greatest effects in reducing cell invasion. Compared to single- and dual-drug treatment, triple-drug therapy suppressed pulmonary metastases and orthotopic osteosarcoma progression to significantly greater degrees in orthotopic osteosarcoma xenograft/spontaneous metastases mouse models, while none showed significant toxicity. In addition, triple-drug therapy improved the overall survival to the greatest extent in experimental metastases mouse models. These findings demonstrate co-targeting of DNA, RNA and protein molecules as a novel therapeutic strategy for the treatment of metastasis

3-[(E)-2-Chloro-3,3,3-trifluoro­prop-1-en-1-yl]-N-(2-fluoro­phen­yl)-2,2-dimethyl­cyclo­propane-1-carboxamide

The phenyl ring in the title compound, C15H14ClF4NO, makes a dihedral angle of 80.3 (3)° with the cyclo­propane ring. In the crystal, mol­ecules are linked by N—H⋯O hydrogen bonds into chains running along the a axis

Comparing the diagnostic values of circulating microRNAs and cardiac troponin T in patients with acute myocardial infarction

OBJECTIVE: Recent studies have shown that circulating microRNAs might be useful, novel biomarkers for the diagnosis of acute myocardial infarction. The aims of this study were to evaluate the expression of cardiac-specific miRNAs (miR-1, -133a, -208b, and -499) in patients with acute myocardial infarction and to compare the diagnostic values of these miRNAs with that of cardiac troponin T. METHODS: Sixty-seven plasma samples obtained from patients with acute myocardial infarction and 32 plasma specimens collected from healthy volunteers were analyzed in this study. The levels of cardiac-specific miRNAs (miR-1, -133a, -208b, and -499) were measured by quantitative reverse transcription-polymerase chain reaction, and the concentrations of plasma cardiac troponin T were measured using electrochemiluminescence-based methods and an Elecsys 2010 Immunoassay Analyzer. RESULTS: The levels of plasma miR-1, -133a, -208b, and -499 were significantly higher in acute myocardial infarction patients (all

Influence of different processing times on the quality of Polygoni Multiflora Radix by metabolomics based on ultra high performance liquid chromatography with quadrupole timeâ ofâ flight mass spectrometry

Peer Reviewedhttps://deepblue.lib.umich.edu/bitstream/2027.42/136757/1/jssc5378_am.pdfhttps://deepblue.lib.umich.edu/bitstream/2027.42/136757/2/jssc5378.pd

Synthesis of Enantiomers of Chiral Ester Derivatives Containing an Amide Group and their Chiral Recognition by ¹H NMR Spectroscopy

Enantiomers of Chiral Ester Derivatives Containing an Amide Group and Possessing One or Two Stereogenic Centers Were Prepared from L- and D-Α-Amino Acids, and Glycine with (S)- and (R)-Mandelic Acid for Probing their Chiral Recognition as a New Class of Chiral Guests by 1H NMR Spectroscopy, Since Chiral Ester Derivatives Have Been Rarely Used as Chiral Substrates for Chiral Recognition by 1H NMR Technology. the Results Indicated that These Chiral Ester Derivatives Have Been Successfully Differentiated in the Presence of Tetraaza Macrocyclic Chiral Solvating Agents (TAMCSAs) 1 A–1 C. in Order to Better Understand their Chiral Discriminating Behavior, Job Plots, Association Constants (Ka), and Theoretical Calculations of (S,S)-G1 and (R,R)-G1, as a Representative Example, Were Performed, respectively. in Order to Evaluate their Practical Application, the 1H NMR Spectra of G1 and G9 with Various Optical Purities Were Measured (Up to 98 % Ee). in This Work, a Practical Strategy Has Been Effectively Established for Chiral Recognition of Chiral Ester Derivatives Containing an Amide Group and Possessing One or Two Chiral Centers in the Presence of Tetraaza Macrocyclic Chiral Solvating Agents 1 A–1 C by Means of 1H NMR Spectroscopy

Effects of salidroside on rat CYP enzymes by a cocktail of probe drugs

Objective(s): In this study, we aimed to evaluate the effect of salidroside on the activities of the different drug-metabolizing enzymes CYP1A2, CYP2B6, CYP2C9, CYP2D6 and CYP3A4 in rats, in which a specific probe drug was used for each enzyme. Materials and Methods: After pretreatment with salidroside, five probe drugs were simultaneously administered to rats by gavage. The given dose was 2.0 mg/kg for phenacetin (CYP1A2 activity), 4.0 mg/kg for bupropion (CYP2B6 activity), 2.0 mg/kg for losartan (CYP2C9 activity), 8.0 mg/kg for metoprolol (CYP2D6 activity) and 1.0 mg/kg for midazolam (CYP3A4 activity). Then, an ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was used to analyze the concentrations of rats’ blood, which were collected at different corresponding times. Results: Our data showed that salidroside exhibited an inductive effect on CYP1A2, CYP2B6, CYP2C9 and CYP3A4 activities by changing the main pharmacokinetic parameters (t1/2, CL/F, Cmax and AUC(0-∞)) of the four probe drugs in rats. However, no significant changes in CYP2D6 activity were observed. Conclusion: In a word, the results displayed that salidroside could induce the activities of CYP1A2, CYP2B6, CYP2C9 and CYP3A4, which may influence the disposition of the drugs that are mainly metabolized by these pathways. Our research can provide the basis for the study of related herb-drug interactions in clinic