Search results for "Anilide"
showing 10 items of 40 documents
�ber die Wirkung von Metyrapon auf den mikrosomalen Arzneimittelabbau
1967
The inhibitor of adrenal steroid-11-β-hydroxylation, Metyrapone (SU 4885), also decreases the rate of drug hydroxylation reactions, both in vitro and in vivo. The follwing oxidative microsomal reactions were studied: O-demethylation of p-nitroanisole, N-demethylation of amidopyrine, and ring hydroxylation of acetanilide. In all three cases Metyrapone inhibits the formation of the reaction products. The inhibitor concentrations required for reduction of the initial reaction rates to one half are 7.5 · 10−4 M, 5 · 10−4m and 20 · 10−4 M, respectively. Steroid C-11-β-hydroxylation is reduced to one half by 2.5 · 10−4 M Metyrapone.
Analysis of serine proteases from marine sponges by 2-D zymography.
2007
Proteolytic activities isolated from the marine demosponges Geodia cydonium and Suberites domuncula were analyzed by 2-D zymography, a technique that combines IEF and zymography. After purification, a 200 kDa proteolytically active protein band was obtained from G. cydonium when analyzed in gelatin copolymerized 1-D zymograms. The enzymatic activity was quantified using alpha-N-benzoyl-D-arginine p-nitroanilide (BAPNA) as a substrate and corresponded to a serine protease. The protease activity was resistant to urea and SDS. DTT and 2-mercaptoethanol (2-ME) did not significantly change the protease activity, but induced a shift in molecular mass of the proteolytic band to lower M(r) values a…
Analysis of metabolism and genotoxicity of 5-nitro-3-thiophenecarboxanilides in bacterial, mammalian and human cells
1995
5-nitro-3-thiophenecarboxanilide (NTCA3) was clearly mutagenic in Salmonella typhimurium strains TA98, YG1021 (the strain with elevated nitroreductase) and YG1024 (the strain with elevated O-acetyltransferase) and only slightly mutagenic at the gpt locus in AS52 cells. Clastogenic activity in human lymphocytes was dependent on the length of exposure : detectable chromosome aberrations were observed following a 24 h treatment period, but not after 3 h exposure. S9 increased genotoxicity in both mammalian cells and human lymphocytes. Metabolites formed by incubation of NTCA3 with the different cell systems were examined. A time-course study in cell whole extracts showed that bacterial and mam…
CCDC 1972052: Experimental Crystal Structure Determination
2020
Related Article: Andreas Heilmann, Jamie Hicks, Petra Vasko, Jose M. Goicoechea, Simon Aldridge|2020|Angew.Chem.,Int.Ed.|59|4897|doi:10.1002/anie.201916073
ortho-Substituent effects inN-arylacetamides. NMR and molecular mechanics investigation
1995
1H, 13C, 15N and 17O NMR spectra of N-phenylacetamide (acetanilide) and 21 ortho-substituted acetanilides were measured and assigned. The observed NMR parameters are related to the Hammett substituent parameters and conformational characteristics of the acetamido moiety estimated by molecular mechanics calculations. Significant relationships were found for the 13C NMR chemical shifts of C-5 (para to substituent) and the direct spin–spin coupling constant, 1J(C, H), of C-3 (ortho to substituent) with Hammett substituent parameters. For 15N NMR chemical shifts of the amido nitrogen, no general correlation with the Hammett substituent parameters was found. The interactions between functionalit…
ChemInform Abstract: Ortho-Substituent Effects in N-Arylacetamides. NMR and Molecular Mechanics Investigation.
2010
1H, 13C, 15N and 17O NMR spectra of N-phenylacetamide (acetanilide) and 21 ortho-substituted acetanilides were measured and assigned. The observed NMR parameters are related to the Hammett substituent parameters and conformational characteristics of the acetamido moiety estimated by molecular mechanics calculations. Significant relationships were found for the 13C NMR chemical shifts of C-5 (para to substituent) and the direct spin–spin coupling constant, 1J(C, H), of C-3 (ortho to substituent) with Hammett substituent parameters. For 15N NMR chemical shifts of the amido nitrogen, no general correlation with the Hammett substituent parameters was found. The interactions between functionalit…
Nivolumab VERSUS Cabozantinib as Second-Line Therapy in Patients With Advanced Renal Cell Carcinoma: A Real-World Comparison
2022
Background: Tyrosine-kinase inhibitors (TKIs) still represent a first-line option for selected patients with metastatic Renal Cell Carcinoma (mRCC). We aimed to compare the real-world efficacy of nivolumab or cabozantinib as second-line therapy in specific mRCC subpopulations. Patients and Methods: We retrospectively collected data from 11 centers from Italy, Spain and US. Overall Survival (OS) and Progression-Free Survival (PFS) were analyzed using Kaplan-Meier curves. Cox proportional models were used at univariate and multivariate analyses. Results: We collected data from 343 patients with mRCC, 123 (36%) treated with cabozantinib and 220 (64%) with nivolumab. The median OS resulted long…
A role for peroxisome proliferator-activated receptor gamma in resveratrol-induced colon cancer cell apoptosis.
2014
Scope Resveratrol may function as a chemopreventive agent. A recent clinical study demonstrates a reduction in tumor cell proliferation in colorectal patients receiving repeated oral ingestion of resveratrol. However, gaps remain in our knowledge of the molecular mechanisms by which resveratrol exerts its chemopreventive effect. We have previously demonstrated that resveratrol induces apoptosis in colon cancer cells and that resveratrol can sensitize chemoresistant colon cancer cells to various drugs. Based on its ability to activate peroxisome proliferator-activated receptor gamma (PPARγ) in colon cancer cells, we sought to determine the implication of this nuclear transcription factor in …
Safety and tolerability of β3-adrenoceptor agonists in the treatment of overactive bladder syndrome - insight from transcriptosome and experimental s…
2016
We have reviewed the safety and tolerability of β3-adrenoceptor agonists, specifically mirabegron and solabegron, a newly emerging drug class for the treatment of the overactive bladder syndrome. We discuss them mechanistically in the context of expression and other preclinical data.Based on a systematic PubMed search, incidence of overall adverse events, hypertension, dry mouth, and constipation are comparable between mirabegron or solabegron and placebo. Hypertension is the most frequently observed adverse event, but has a similar incidence with mirabegron and placebo. Nevertheless, severe uncontrolled hypertension has become a contraindication for use of mirabegron based on observation o…
Studies in organic mass spectrometry. Part 23. Role of the aroyl group on the competitive fragmentation reactions of the molecular ion of aroylanilid…
1999
The 70 eV and mass-analysed ion kinetic energy (MIKE) spectra of some thiophenecarboxanilides and benzoylanilides (1–10) have been compared in order to investigate the role of the aroyl (or heteroaroyl) moiety on the abundance of the competitive fragmentation reactions occurring in their molecular ions (amide–bond cleavage and phenol radical ion formation). It has been shown that the electron ionisation induced decompositions with high (70 eV) and low (MIKE) internal energy excess are qualitatively similar, but remarkable quantitative differences have been observed that can be accounted for in terms of the different effectiveness in the transmission of electronic effects of substituents in …