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Yuichi Hashimoto - One of the best experts on this subject based on the ideXlab platform.
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Structural Development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility.
Bioorganic & medicinal chemistry letters, 2017Co-Authors: Sayaka Nomura, Yuichi Hashimoto, Makoto Makishima, Kaori Endo-umeda, Shinya Fujii, Minoru IshikawaAbstract:Abstract LXRβ-selective agonists are promising candidates to improve atherosclerosis without increasing plasma or hepatic TG levels. We have reported a series of tetrachlorophthalimide analogs as an LXRβ-selective agonist. However, they exhibited poor aqueous solubility probably due to its high hydrophobicity and highly rigid and plane structure. In this report, we present further Structural Development of tetrachloro(styrylphenyl)phthalimides as the LXRβ-selective agonists with improved aqueous solubility.
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Structural Development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton.
Bioorganic & medicinal chemistry, 2010Co-Authors: Masahiko Nakamura, Yuichi Hashimoto, Hiroyuki Miyachi, Atsushi Aoyama, Mohammed T.a. Salim, Mika Okamoto, Masanori Baba, Hiroshi AoyamaAbstract:Abstract A phenanthridinone skeleton was derived from our previous researches on thalidomide and retinoids as a multi-template for generation of anti-viral lead compounds. Structural Development studies focusing on anti-hepatitis C virus activity afforded 5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6(5 H )-one ( 10 ) and 5-butylbenzo[ b ]phenanthridin-6(5 H )-one ( 39 ), which showed EC 50 values of approximately 3.7 and 3.2 μM, respectively.
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Structural Development studies of nuclear receptor ligands
Pure and Applied Chemistry, 2007Co-Authors: Shinnosuke Hosoda, Yuichi HashimotoAbstract:Studies in our laboratory are focused on Structural Development studies of biologi- cal response modifiers (BRMs), including nuclear receptor (NR) ligands, which act directly on cells at the gene expression level, and thalidomide (and related molecules), which modu- lates a variety of physiological processes. Our studies on the molecular design of ligands for retinoic acid receptor (RAR), androgen receptor (AR), vitamin D receptor (VDR), farnesoid X receptor (FXR), and peroxisome proliferator-activated receptor (PPAR) are reviewed.
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Structural Development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors.
Chemical & pharmaceutical bulletin, 2007Co-Authors: Tomomi Noguchi-yachide, Hiroyuki Miyachi, Hiroshi Aoyama, Atsushi Aoyama, Makoto Makishima, Yuichi HashimotoAbstract:Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure–activity studies and further Structural Development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 μM for LXRα and LXRβ, respectively.
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Thalidomide as a nitric oxide synthase inhibitor and its Structural Development
Chemical & pharmaceutical bulletin, 2004Co-Authors: Rumiko Shimazawa, Hiroko Sano, Aya Tanatani, Hiroyuki Miyachi, Yuichi HashimotoAbstract:Thalidomide has been found to exhibit weak nitric oxide synthase (NOS)-inhibitory activity. Structural Development studies of thalidomide showed that some N-2,6-dimethylphenylhomophthalimide analogs possess NOS-inhibiting activity.
J R Helliwell - One of the best experts on this subject based on the ideXlab platform.
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quantifying the impact of microbes on soil Structural Development and behaviour in wet soils
Soil Biology & Biochemistry, 2014Co-Authors: J R Helliwell, Anthony J Miller, W R Whalley, Sacha J Mooney, Craig J SturrockAbstract:There is evidence that microbial populations play an important role in altering soil pore geometry, but a full understanding of how this affects subsequent soil behaviour and function is still unclear. In particular the role of microorganisms in soil Structural evolution and its consequence for pore morphological Development is lacking. Using a combination of bio-chemical measurements and X-ray Computed Tomography (CT) imaging, a temporal comparison of microscale soil Structural Development in contrasting soil environments was made. The aim was to quantify the effect of microbial activity in the absence of other features likely to cause soil deformation (e.g. earthworms, roots etc.) on soil Structural Development in wet soils, defined by changes in the soil porous architecture i.e. pore connectivity, pore shape and pore volume during a 24 week period. Three contrasting soil textures were examined and changes compared between field soil, sterilised soil and a glucose enhanced soil treatment. Our results indicate that soil biota can significantly alter their microhabitat by changing soil pore geometry and connectivity, primarily through localised gaseous release. This demonstrates the ability of microorganisms to modify soil structure, and may help reveal the scope by which the microbial-rich rhizosphere can locally influence water and nutrient delivery to plant roots.
Craig J Sturrock - One of the best experts on this subject based on the ideXlab platform.
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quantifying the impact of microbes on soil Structural Development and behaviour in wet soils
Soil Biology & Biochemistry, 2014Co-Authors: J R Helliwell, Anthony J Miller, W R Whalley, Sacha J Mooney, Craig J SturrockAbstract:There is evidence that microbial populations play an important role in altering soil pore geometry, but a full understanding of how this affects subsequent soil behaviour and function is still unclear. In particular the role of microorganisms in soil Structural evolution and its consequence for pore morphological Development is lacking. Using a combination of bio-chemical measurements and X-ray Computed Tomography (CT) imaging, a temporal comparison of microscale soil Structural Development in contrasting soil environments was made. The aim was to quantify the effect of microbial activity in the absence of other features likely to cause soil deformation (e.g. earthworms, roots etc.) on soil Structural Development in wet soils, defined by changes in the soil porous architecture i.e. pore connectivity, pore shape and pore volume during a 24 week period. Three contrasting soil textures were examined and changes compared between field soil, sterilised soil and a glucose enhanced soil treatment. Our results indicate that soil biota can significantly alter their microhabitat by changing soil pore geometry and connectivity, primarily through localised gaseous release. This demonstrates the ability of microorganisms to modify soil structure, and may help reveal the scope by which the microbial-rich rhizosphere can locally influence water and nutrient delivery to plant roots.
Wang Zhong - One of the best experts on this subject based on the ideXlab platform.
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Structural Development of wheat nutrient transfer tissues and their relationships with filial tissues Development
Protoplasma, 2015Co-Authors: Yu Xurun, Shao Shanshan, Xiong Fei, Zhou Liang, Yu Heng, Zhang Jing, Chen Xinyu, Wang ZhongAbstract:Nutrients from spikelet phloem are commonly delivered to endosperm via caryopsis nutrient transfer tissues (NTTs). Elucidation of NTTs Development is paramount to developing an understanding of the control of assimilate partitioning. Little information was available on the Structural Development of the entire NTTs and their functions, particularly those involved in the relationship between Development of NTTs and growth of filial tissues including endosperm and embryo. In this study, wheat caryopses at different Development stages were collected for observation of the NTTs by light microscopy, stereoscopic microscopy, and scanning electron microscopy. The cytological features of NTTs in the developing wheat caryopsis were clearly elucidated. The results were as follows: NTTs in the wheat caryopsis include maternal transfer tissues that are composed of vascular bundle, chalaza and nucellar projection transfer cells, and endosperm transfer tissues that consist of the aleurone transfer cells, starchy endosperm transfer cells, and endosperm conducting cells. The initiation, Development, and apoptosis of these NTTs revealed the pattern of temporal and spatial gradient and were closely coordinated with endosperm and embryo Development. These results may give us a further understanding about the functions of NTTs and their relationships with endosperm and embryo Development.
Peter Fratzl - One of the best experts on this subject based on the ideXlab platform.
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Structural Development of the mineralized tissue in the human l4 vertebral body
Journal of Structural Biology, 2001Co-Authors: Paul Roschger, B M Grabner, S Rinnerthaler, Andrea Berzlanovich, W Tesch, Michaela Kneissel, Klaus Klaushofer, Peter FratzlAbstract:Abstract Knowledge of the Structural Development of the human vertebrae from non-weight-bearing before birth to weight-bearing after birth is still poor. We studied the mineralized tissue of the developing lumbar L4 vertebral body at ages 15 weeks postconception to 97 years from the tissue level (trabecular architecture) to the material level (micro- and nanostructure). Trabecular architecture was investigated by 2D histomorphometry and the material level was examined by quantitative backscattered electron imaging (for typical calcium content, CaMaxFreq) and scanning small-angle X-ray scattering (for mean mineral particle thickness). During early Development, the trabecular orientation changed from a radial to a vertical/horizontal pattern. For bone area per tissue area and trabecular width in postnatal cancellous bone, the maximum was reached at adolescence (20 years), while for trabecular number the maximum was reached at childhood (≈1 year). CaMaxFreq was lower in early bone (≈21 wt%) than in mineralized cartilage (≈29 wt%) and adolescent bone (≈23 wt%). In conclusion, the changes at the tissue level were observed to continue throughout life while the Development of bone at the material level (CaMaxFreq, mineral particle thickness and orientation) is essentially complete after the first years of life. CaMaxFreq and mean particle thickness increase rapidly during the first years and reach saturation. Remarkably, when these parameters are plotted versus logarithm of age, they appear linear.
