A5088595957- Aldose Reductase and Taurine
- Radiation Effects and Dosimetry
- Receptor Mechanisms and Signaling
- Plant-based Medicinal Research
- Chemical Synthesis and Analysis
- Prenatal Substance Exposure Effects
- Gout, Hyperuricemia, Uric Acid
- Alcohol Consumption and Health Effects
- Surgical Sutures and Adhesives
- Folate and B Vitamins Research
- Synthesis and Biological Evaluation
- Diabetes Treatment and Management
- Neonatal Health and Biochemistry
- Neuropeptides and Animal Physiology
- Biochemical and Molecular Research
- Cholinesterase and Neurodegenerative Diseases
- Peptidase Inhibition and Analysis
- Molecular spectroscopy and chirality
- Metal complexes synthesis and properties
- Neuroscience and Neuropharmacology Research
- Fish Biology and Ecology Studies
- Biochemical effects in animals
- Bioactive Compounds and Antitumor Agents
- Chemical synthesis and alkaloids
- Cannabis and Cannabinoid Research
Riso Kagaku (Japan)
1998-2016
Monash University
2004-2005
Inserm
2004-2005
Centre National de la Recherche Scientifique
2004-2005
Institut de Biologie Moléculaire et Cellulaire
2005
Institut de génétique et de biologie moléculaire et cellulaire
2005
Parks Victoria
2004
Maruwa Foods and Biosciences (Japan)
2000
National Archives and Records Administration
2000
Gifu Pharmaceutical University
1998-1999
We collected and completely sequenced 28,469 full-length complementary DNA clones from Oryza sativa L. ssp. japonica cv. Nipponbare. Through homology searches of publicly available sequence data, we assigned tentative protein functions to 21,596 (75.86%). Mapping the cDNA genomic revealed that there are 19,000 20,500 transcription units in rice genome. Protein informatics analysis against InterPro database existence proteins presented but not Arabidopsis. Sixty-four percent our cDNAs...
Abstract The X‐ray structures of human aldose reductase holoenzyme in complex with the inhibitors Fidarestat (SNK‐860) and Minalrestat (WAY‐509) were determined at atomic resolutions 0.92 Å 1.1 Å, respectively. hydantoin succinimide moieties interacted conserved anion‐binding site located between nicotinamide ring coenzyme active residues Tyr48, His110, Trp111. Minalrestat's hydrophobic isoquinoline was bound an adjacent pocket lined by Trp20, Phe122, Trp219, bromo‐fluorobenzyl group inside...
The single-crystal structure of anagliptin, N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide, was determined. Two independent molecules were held together by intermolecular hydrogen bonds, and the absolute configuration 2-cyanopyrrolidine ring delivered from l-prolinamide confirmed to be S. interactions anagliptin with DPP-4 clarified co-crystal solved at 2.85 Å resolution. Based on determined X-ray crystallography,...
Structure determination of porcine aldehyde reductase holoenzyme in complex with the potent aldose inhibitor fidarestat was carried out to explain difference potency for and reductases. The hydrogen bonds between active-site residues Tyr50, His113, Trp114 are conserved two enzymes. In reductase, Leu300 forms a bond through its main-chain nitrogen atom exocyclic amide group inhibitor, which when replaced Pro cannot form bond, thus causing loss binding energy. Furthermore, side chain Trp220...
In this study, we developed a highly sensitive assay for xanthine oxidoreductase (XOR) activity utilizing combination of [(13) C2 ,(15) N2 ]xanthine and liquid chromatography (LC)/triple quadrupole mass spectrometry (TQMS). assay, the amount ]uric acid (UA) produced by XOR was determined using LC/TQMS. For synthesized as substrate, ]UA an analytical standard, C3 N3 internal standard. The calibration curve obtained LC/TQMS under selected reaction monitoring mode evaluated, results indicated...
The absolute configuration of the aldose reductase (AR) inhibitor, (+)-(2S,4S)-6-fluoro-2',5'-dioxospiro¿chroman-4, 4'-imidazolidine-2-carboxamide (fidarestat), was established indirectly by single-crystal X-ray analysis (+)-(2S, 4S)-8-bromo-6-fluoro-2',5'-dioxospiro¿chroman-4, 4'-imidazolidine-2-carboxylic acid (1). crystal structure human AR complexed with fidarestat determined, and specific inhibition activity discussed on basis three-dimensional interactions between them. clarified that...
Structure of the Leu300Pro mutant human aldose reductase (ALR2) in complex with inhibitor fidarestat is determined. Comparison hALR2-fidarestat and porcine aldehyde (ALR1)-fidarestat indicates that hydrogen bond between Leu300 amino group wild-type exocyclic amide key determinant for specificity ALR2 over ALR1. Thermodynamic data also suggest an enthalpic contribution as predominant difference binding energy wild-type. An additional selectivity-determining feature interaction side chain...
Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery 4b as a highly selective, potent inhibitor DPP-IV. In vivo studies in Wistar/ST rats showed that was converted into strongly active metabolite 4l high yield, resulting good efficacy for antihyperglycemic activity.
Structure determinations of human aldose reductase holoenzyme in complex with the 2S4R-, 2R4S- and 2R4R-isomers potent inhibitor Fidarestat ((2S,4S)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazoline]-2-carboxamide) were carried out order to elucidate binding modes responsible for differences their inhibitory potencies. In structure 2R4S-isomer cyclic imide moiety formed hydrogen bonds side-chains Trp111, Tyr48 His110. attempt determine least 2R4R-isomer this ligand was not observed,...
Several novel tricyclic compounds with a unique amine moiety (1, 2a--i) were designed and prepared based on the structure of triperiden for development anti-influenza virus agents. An in vitro antiviral assay showed that 1-(1-azabicyclo[3.3.0]octan-5-yl)-1-(4-fluorophenyl)-1-(2-tricyclo[3.3.1.1(3.7)]decyl)methan-1-ol hydrochloride (2f) has potent A activity. Furthermore, since 2f was well tolerated mice, is promising as agent humans.
In order to discover a medicine effective against Alzheimer's disease, we synthesized series of quinoline derivatives having characteristic 1-azabicyclo[3.3.0]octane amine ring, and performed pharmacological evaluation them. Acetylcholine esterase inhibitory activities these were unexpectedly weak. Tests for central nervous muscarinic cholinergic receptor binding affinity indicated that compounds had higher affinities M1 receptors than M2 receptors. A naphthalene substituted with the ring...
Abstract The photochemical synthesis of indole derivatives starting from the indoline‐2‐thiones 1 is described. Irradiation in presence alkenes 3 gave 2‐alkyl‐3 H ‐indoles 4 – 7 or 2‐alkylindoles 8 22 through ring cleavage intermediates, spirocyclic amino‐thietanes, initially derived by [2 + 2] cycloaddition CS bond and CC . trialkylamines 26 desulfurization products 27 32 unexpected 3‐alkylindoles 33 40 N ‐Acylindoline‐2‐thiones 11 ‐ p yielded deacylated products, 1a b , ethyl esters 43...
A useful pharmaceutical intermediate, 5-nitromethyl-1-azabicyclo[3.3.0]octane (1), was prepared in one step from 1,7-dichloro-4-heptanone (4) under mild conditions. Catalytic hydrogenation of 1 over Raney Ni the presence sodium hydroxide afforded 5-aminomethyl-1-azabicyclo[3.3.0]octane (2) high yield. Piracetam analogues 20-23, which were pyrrolidine derivatives involving a 1-azabicyclo[3.3.0]octane ring, synthesized. Pharmacological tests showed that...
Abstract 5‐Cyano‐1‐azabicyclo[3.3.0]octane ( 1 ) was prepared in one step from 1,7‐dichloro‐4‐heptanone 4 under mild conditions. The application of this method for the preparation 5‐cyano‐4,6‐dimethyl‐1‐azabicy‐clo[3.3.0]octane 11 gave two diastereomers equilibrium. NMR measurements and its reduced compound 15 showed that major isomer is cis‐exo form, minor trans form. Molecular orbital calculations indicated form more stable than agreement with experimental results. Furthermore,...
In order to develop drugs effective against Alzheimer's disease, we synthesized a series of aniline derivatives having characteristic cyclic amine, 1-azabicyclo[3.3.0]octane ring, and evaluated their binding affinity for the central muscarinic cholinergic receptor. Among these compounds which showed high M1 receptor, N-[2-(1-Azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline (9f fumarate, SK-946) highest affinity. The ability this compound improve cognitive function was assessed using passive...
5-Substituted methyl-I-azabicyclo[3.3.0]octane, which is a useful intermediate for drugs, was readily synthesized from 1,7-dichloro-4-heptanone without isolating unstable intermediates.5-Substituted methyl-I-azabicyclo[3.3.0]octanederivatives such as 5-cyanomethyl-I-azabicyclo[3.3.0]octane ( I ) are intermediary materials preparing various medicines 1
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”
The radioresistances of 16 species and 39 strains bacilli spores grown on tryptone glucose extract agar, nutrient agar yeast were illustrated in Fig. 2 by the dose to give 10-4 survival which was obtained from dose-survival curves (Fig. 1). In some cases, varied radioresistance same strain different growing media observed.Significance concentration level metals spore production radioresistanceof investigated using Bacillus megaterium IMF 1166. A little, crop observed without addition...
栽培方法の違いが生食向きホウレンソウの成分に与える影響を明らかにするため, 成分分析, 官能検査を行った。1) 水耕, 土耕の栽培法の違いでおかめ, リード, TG-1, S-20の4品種を一括して成分を比べると, 水分は水耕で. ビタミンCは土耕で有意に高く食物繊維, シュウ酸は差を見いだせなかった。2) 水耕のTG-1とS-20ではおかめやリードに比べ水分が多く, 食物繊維, シュウ酸が少なく, 土耕との成分差が大きく品種間の差も見られた。3) 栽培法の違いをより明らかにするため, 新たにガラス室内に土耕試験区を設け比較した結果, これまでの栽培法の露地土耕とガラス室内水耕に比べ食物繊維, とくにシュウ酸含量に顕著な差違が見られた。4) 味および総合評価において, おかめでは水耕が土耕より優れており, TG-1では水耕が劣っていることがわかった。5) 露地とガラスハウス内の栽培を一括するとビタミンCが露地で多く, 他の成分には有意な差は認められなかった。以上の結果はホウレンソウの生食にはおかめの水耕が適し, TG-1はガラスハウス内土耕が適しているということを示している。