Publications by authors named "Masanori Ichikawa"

Article Synopsis
  • The study analyzed discrepancies in fatty acid compositions measured by gas chromatography (GC) and near-infrared fiber-optic method (NIR) in bovine fat, focusing on refractive index values.
  • Using intermuscular fat from 45 crossbreeds, the researchers found that both SFA and MUFA measurements had strong correlations (≥ 0.8) between GC and NIR and with refractive index.
  • The findings suggested that measurement errors lead to significant differences (over 3%) between GC and NIR, and reanalyzing GC samples using refractive index could enhance accuracy by slightly reducing these discrepancies.
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  • Researchers synthesized new BRS-3 agonist compounds to target peripheral systems, with a focus on reducing obesity without affecting the central nervous system.
  • They introduced a labile carboxylic ester to enhance the potency and safety of these compounds during testing.
  • The compound phenol ester 17c was identified as the most promising candidate, effectively suppressing food intake in mice and exhibiting no significant adverse effects on heart rate or blood pressure in dogs, facilitating the development of safer anti-diabetes and obesity drugs.
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  • Researchers developed a new series of compounds called trifluoromethyltriazolobenzoxazepines that inhibit squalene synthase.
  • Through structure-activity studies and optimizing pharmacokinetics, they identified a particularly effective compound, DF-461 (compound 23), with strong inhibitory activity against squalene synthase.
  • DF-461 demonstrated high liver selectivity, effectively reduced cholesterol synthesis in rats, and showed promising results for lowering plasma lipids in non-rodent studies.
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Article Synopsis
  • The article discusses the development of benzhydrol derivatives that are powerful inhibitors of squalene synthase but failed to show adequate effectiveness for clinical use.
  • The research then shifted towards creating a more effective compound by utilizing a benzoxazepine structure.
  • The newly designed pyrrolobenzoxazepine derivatives demonstrated improved in vitro and in vivo activity compared to the initial compounds.
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We have recently reported the discovery of the new benzhydrol template, which has a highly potent inhibitory activity for squalene synthase, as typified by compound 1 (SSI IC(50)=0.85 nM). However, it was composed of a pair of easy rotatable atropisomers.

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To obtain small and efficient squalene synthase inhibitors, a flexible 2-aminobenzhydrol open form structure was designed and showed potent inhibitory activity comparable to 4,1-benzoxazepin compounds. Further chemical modification led to the discovery of a novel template with a strong squalene synthase inhibitory activity, and its basic structure-activity relationship was revealed. The X-ray crystallographic data of compound 12 bound to the active site of squalene synthase provided an important insight into the binding mode of this alternative template that formed 11-membered ring conformations with an intramolecular hydrogen bond.

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In an effort to find accurate alternatives to the usual confidence intervals based on normal approximations, this paper compares four methods of generating second-order accurate confidence intervals for non-standardized and standardized communalities in exploratory factor analysis under the normality assumption. The methods to generate the intervals employ, respectively, the Cornish-Fisher expansion and the approximate bootstrap confidence (ABC), and the bootstrap-t and the bias-corrected and accelerated bootstrap (BC(a)). The former two are analytical and the latter two are numerical.

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