Synthesis of Quinazolin-4(3<i>H</i>)‑ones via Amidine <i>N</i>‑Arylation

Pyrido­[4,3-<i>d</i>]­pyrimidin-4­(3<i>H</i>)-one (<b>1</b>) was prepared by reacting 2-trifluoromethyl-4-iodo-nicotinic acid (<b>2</b>) with amidine <b>9a</b> catalyzed by Pd₂(dba)₃ and Xantphos, followed by cyclization effected with HBTU and subsequent demethylation using PhBCl₂. The amidine arylation method was found applicable for the syntheses of quinazolin-4­(3<i>H</i>)-ones. Thus, reaction of 2-bromo or 2-iodo benzoate esters with amdidines afforded substituted quinazolin-4­(3<i>H</i>)-ones in 44–89% yields

The effect of high-fat diet on the plasma lipidome.

<p>Significant mean fold changes (P&lt;0.05) observed in plasma lipids from mice fed a high fat diet for 12 week (N = 6) relative to low fat fed animals (N = 8). Plasma lipids were analysed by LC ESI-MS/MS and absolute lipid levels were expressed relative to the low fat fed control group. Plasma samples were obtained from 5 hour fasted animals. BMP, bismonoacylglycerolphosphate; Cer, ceramide; DG, diacylglycerol; DHC, dihexosylceramide; LPC, lysophosphatidylcholine; MHC, monohexosylceramide; PC, phosphatidylcholine; PE, phosphatidylethanolamine; PG, phosphatidylglycerol; SM, sphingomyelin; Sph, sphingosine; TG, triacylglycerol; THC, trihexosylceramide.</p

Time course changes in metabolic parameters measured in mice fed a high fat diet.

<p>Body mass (A), fat mass (B), fasting blood glucose (C), plasma insulin (D), blood glucose during an intraperitoneal glucose tolerance test (E) and blood glucose area under the curve during an intraperitoneal glucose tolerance test (F) were measured in mice (N = 11) following a 5 hour fast at baseline (time 0) and after 1, 3 and 6 weeks of high fat feeding. Data are presented as mean ± SEM. *P&lt;0.05 versus baseline; ^†P&lt;0.05 versus week 1; ^‡P&lt;0.05 versus week 3.</p

Tissue lysophosphatidylcholine levels in low and high fat fed mice.

<p>Liver (A), skeletal muscle (B) and adipose tissue (C) lysophosphatidylcholine (LPC) levels measured by LC ESI-MS/MS in mice fed a low (N = 8) or high fat diet (HFD, N = 6). Tissues were collected from 5 hour fasted animals. Data are presented as mean ± SEM. *P&lt;0.05 versus low fat.</p

Subject characteristics.

<p>Samples were obtained following an overnight (10–12 hour) fast. Data are mean ± SEM.</p>a<p>P&lt;0.05 vs lean;</p>b<p>P&lt;0.05 vs obese non-diabetic.</p

Relationship between plasma lysophosphatidylcholine (LPC), adiposity and indices of insulin resistance in high fat fed mice (A–D) and lean, obese and obese type 2 diabetic humans (E–H).

<p>The association between circulating LPC and percent body fat (A), blood glucose (B), plasma insulin (C) and HOMA-IR (D) in high fat fed mice. The association between circulating LPC and BMI (E), blood glucose (F), plasma insulin (G) and HOMA-IR (H) in the human cohort. Data are presented as line of best fit with 95% confidence intervals.</p

Plasma LPC levels in lean, obese non-diabetic and obese type 2 diabetic individuals.

<p>Samples were obtained following an overnight (10–12 hour) fast. Data are mean ± SEM.</p>a<p>P&lt;0.05 vs lean;</p>b<p>P&lt;0.01 vs lean;</p>c<p>P = 0.052 vs lean;</p>d<p>P = 0.06 vs lean.</p

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05 novembre 19201920/11/05 (A49).Appartient à l’ensemble documentaire : PoitouCh

Metabolic parameters of C57Bl/6 mice fed a low or high fat diet for 12 wk.

<p>All measurements were made in 5 hour fasted mice. Data are mean ± SEM.</p>a<p>P&lt;0.05 vs Chow;</p>b<p>P&lt;0.001 vs Chow. LFD, low fat diet; HFD, high fat diet.</p

Additional file 2: of Impact of flanking chromosomal sequences on localization and silencing by the human non-coding RNA XIST

Location of XIST RNA signal for each integration site with and without DOX treatment. The numbers shown are based on three independent experiments for the DOX results and one experiment for the No DOX results, with ≥50 cells counted for each integration site in each experiment. (PDF 57 kb