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411.
Fujisawa T Odake S Ogawa Y Yasuda J Morita Y Morikawa T 《Chemical & pharmaceutical bulletin》2002,50(2):239-252
Fibroblast collagenase (MMP-1), a member of the matrix metalloproteinases family, is believed to be a pathogenesis of arthritis, by cleaving triple-helical type II collagen in cartilage. From the similarity of the active site zinc binding mode with hydroxamate, we designed and synthesized alpha-mercaptocarbonyl possessing compounds (3-5), which incorporated various peptide sequences as enzyme recognition sites. The P4-P1 peptide incorporating compound (3) exhibited as potent inhibition as the hydroxamate (1) and the carboxylate (2) type inhibitors, with an IC50 of 10(-6) M order against MMP-1. But the inhibitor (3) related compounds (6-8) displayed decreased or no inhibitory potencies. These results suggest that the existence of both the carbonyl and thiol groups might be critical for the inhibition, and the distance between the two functional groups is important for inhibitory potency. For Pn' peptide incorporating compounds (4a-k), except for 4h and 4k, all compounds showed IC50 values under sub-nanomolar. Among them, for potent inhibition, Leu was better than Phe and Val as the P1' amino acid, and the P2' position amino acid was necessary, and preferentially Phe. Insertion of the Pn peptide into 4d or 4k, giving compounds 5a-c, did not increase the activities of 4d and 4k. Substitution of the mercapto group with other functional groups lost the activity of compound 4a. The stereochemical preference at the thiol-attached position was also determined by preparation of both isomers of 4a. It was found that the S configuration compound (36b) is approximately 100 times more potent than the corresponding R-isomer (36a). 相似文献
412.
Concentrations of arsenic and bromine dissolved in hot spring waters have been determined by neutron activation analysis using 0.5 cm3 of sample waters without any chemical pretreatment. The samples prepared for neutron irradiation were simply pieces of filter papers which were infiltrated with samples. With the results of satisfactorily high accuracy and precision, this analytical method was found to be very convenient for the determinations of arsenic and bromine dissolved in water at ppm to sub-ppm levels.This revised version was published online in November 2005 with corrections to the Cover Date. 相似文献
413.
Kita Y Futamura J Ohba Y Sawama Y Ganesh JK Fujioka H 《The Journal of organic chemistry》2003,68(15):5917-5924
The Lewis acid treatment of 2,3-epoxysulfonates with 2,3-dialkyl substituents or 2-alkyl-3-aryl substituents produced the rearrangement products via C3-cleavage of the oxirane ring in high yields. On the other hand, 2-aryl-3-alkyl-2,3-epoxysulfonates produced the products via C2-cleavage of the oxirane ring. The sulfonyloxy groups of the alpha-sulfonyloxy ketones, having a chiral benzylic quaternary carbon center obtained by the rearrangement of 2-alkyl-3-aryl-2,3-epoxysulfonates, were reductively eliminated to give the ketones with a chiral benzylic quaternary carbon center. The method was applied to the formal synthesis of (-)-aphanorphine and total syntheses of (-)-alpha-herbertenol and (-)-herbertenediol. 相似文献
414.
T. Honda T. Oi T. Ossaka T. Nozaki H. Kakihana 《Journal of Radioanalytical and Nuclear Chemistry》1989,133(2):301-315
Determination of the rare earth elements (REE's) in acidic hot spring and crater lake waters by neutron activation analysis (NAA), in which activation was performed mostly by epithermal neutrons (epithermal NAA) was investigated. Nine REE's, La, Ce, Sm, Eu, Tb, Ho, Tm, Yb and Lu, out of fourteen naturally existing REE's were determined at ppb levels with satisfactory precision. The epithermal NAA was found to be more effective in the determination of Sm, Tb, Ho and Yb than normal NAA, in which activation was performed mainly by thermal neutrons. Combined use of the epithermal and normal NAA's enabled the determination of eleven REE's, La, Ce, Sm, Eu, Gd, Tb, Dy, Ho, Tm, Yb and Lu. 相似文献
415.
416.
Y. Kikawada H. Fuji Y. Ohno T. Oi 《Journal of Radioanalytical and Nuclear Chemistry》2008,278(2):323-326
The contents of arsenic in soils collected in the Kusatsu hot spring area, Gunma, Japan, were determined by INAA, with the
average content of 36 mg/kg, which was obviously higher than that reported for the Japanese crust. The remarkably high contents
of arsenic, 170 and 130 mg/kg, were observed in the soils collected near the discharge point of the surplus hot spring water.
The distribution of arsenic in the ground suggests that arsenic originated from hot springs has been diffusing into the ground
accompanying the penetration of the hot spring water. 相似文献
417.
M. Oi 《Physics of Atomic Nuclei》2007,70(9):1577-1581
An unexpected strong anharmonicity was observed in the wobbling spectrum in 163Lu. In an attempt to understand what causes the deviation from the original wobbling model by Bohr and Mottelson, an analysis
is presented using several different approaches, such as exact diagonalization, a semiclassical model to deal with anharmonic
wobbling motion, and a microscopic method based on the self-consistent cranking calculation.
The text was submitted by the author in English. 相似文献
418.
419.
Tomoki Yabutani Yasuhiro Utsunomiya Yukiko Kado Yuji Tani Hideyuki Kishimoto Akinori Fukuda Junko Motonaka 《Analytical sciences》2006,22(7):1021-1024
We present a new multielement masking method using magnesium hydroxide coprecipitation for the selective determination of Pb by differential pulse anodic stripping voltammetry (DPASV). The recovery of Pb in the masking method was over 95%, while interfering ions (Cd(2+), Co(2+), Cu(2+), Fe(3+), Mn(2+), and Ni(2+)) could be removed at 100% from the analytical sample. A linear regression was obtained in the Pb concentration from 10 to 1000 microg kg(-1) in the existence of 100 microg kg(-1) of the interfering ions. When this method was applied to the determination of Pb in a natural water-standard reference material (NIST 1640), the determined value for Pb in this work (25.4 +/- 4.1 microg kg(-1)) almost agreed with the certified value (27.89 +/- 0.14 microg kg(-1)). 相似文献
420.
Kenta Itahashi Satoshi Itoh Nobuhisa Fukunishi Hans Geissel Ryugo S. Hayano Satoru Hirenzaki Masahiko Iwasaki Paul Kienle Rie Kimura Karl Lindberg Chiara Nociforo Hiroaki Ohnishi Shinji Okada Naoya Ono Haruhiko Outa Masaharu Sato Ken Suzuki Takatoshi Suzuki Hideyuki Tatsuno Per–Erik Tegnér Masanori Wakasugi Helmut Weick Junko Yamagata–Sekihara Toshimitsu Yamazaki Yasushige Yano Irina Zartova 《Hyperfine Interactions》2009,193(1-3):27-31
We are preparing for a high resolution spectroscopy of the 1s and 2s pionic states of 121Sn in the 122Sn(d,3He) reaction at the incident deuteron energy of ~500 MeV. The measurement will provide accurate information on the strong interaction between the pion and the nucleus, which leads to quantitative determination of the magnitude of the quark condensate at the normal nuclear density. 相似文献