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941.
942.
943.
Nishida H Miyazaki Y Kitamura Y Ohashi M Matsusue T Okamoto A Hosaka Y Ohnishi S Mochizuki H 《Chemical & pharmaceutical bulletin》2001,49(10):1237-1244
Intravascular clot formation is an important factor in a number of cardiovascular diseases. Therefore, the prevention of blood coagulation has become a major target for new therapeutic agents. One attractive approach is the inhibition of factor Xa (FXa), which is a key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen, prothrombin. We have investigated 1-arylsulfonyl-3-piperazinone derivatives, containing a 4-(piperidino)pyridine group in place of guanidino and/or amidino groups, and discovered compound M55113 (30a: 4-[(6-Chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]methyl]piperazinone), as a potent inhibitor of FXa (IC50=0.06 microM) with high selectivity for FXa over trypsin and thrombin. 相似文献
944.
de Kort M Regenbogen AD Valentijn AR Challiss RA Iwata Y Miyamoto S van der Marel GA van Boom JH 《Chemistry (Weinheim an der Bergstrasse, Germany)》2000,6(15):2696-2704
The synthesis, biological evaluation, and molecular modeling of two conformationally restricted analogues of adenophostinA (1), denominated as spirophostin (3R)-10 and (3S)-11, as novel ligands for the D-myo-inositol 1,4,5-trisphosphate receptor (IP3R), is presented. These diastereoisomeric spiroketals are synthesized by spiroketalization of D-glucose derivatives (2S)-15 and (2R)-16, separation of the protected isomers (3R)-19 and (3S)-20, followed by phosphorylation and deprotection. The spirophostins (3R)-10 and (3S)-11 display comparable biological activity, with a 3H-IP3-displacing and Ca2+-releasing potency less than IP3 and adenophostin A. 相似文献
945.
Antimicrobial activity studies of the binuclear metal complexes derived from tridentate Schiff base ligands 总被引:1,自引:0,他引:1
Tümer Mehmet Köksal Hüseyin Sener M. Kasim Serin Selahattin 《Transition Metal Chemistry》1999,24(4):414-420
Three novel tridentate Schiff base ligands derived fromthe 3-hydroxysalicylaldehyde (H2L1), 4-hydroxysalicylaldehyde (H2L2) and 5-bromosalicylaldehyde (H2L3) with a new amine N-(pyridyl)-2-hydroxy-3-methoxy-5-aminobenzylamine (2) have been prepared. The ligands and their metal complexes have been characterized by elemental analyses, conductivity and magnetic susceptibility measurements, i.r., electronic absorption and 1H and 13C n.m.r. spectroscopy. All complexes are binuclear and, in some, the H2O molecules are coordinated to the metal ion. Antimicrobial activities of the ligands and their complexes have been tested against to the Bacillus subtilis IMG 22 (bacteria), Micrococcus luteus LA 2971 (bacteria) Saccharamyces cerevisiae WET 136 (yeast), and Candida albicans CCM 314 (yeast). Thermal properties of all complexes have been studied by t.g. and d.t.a techniques. 相似文献
946.
M. Ebihara Y. S. Chung W. Chueinta B.-F. Ni T. Otoshi Y. Oura F. L. Santos F. Sasajima Sutisna A. K. B. H. Wood 《Journal of Radioanalytical and Nuclear Chemistry》2006,269(2):259-266
Summary Seven Asian countries have been collaborating in collecting airborne particulate matter (APM) in their individual countries
and analyzing them by neutron activation analysis as a common analytical tool. APM samples were collected into two fractions
of fine and coarse grains (PM2 and PM2-10, respectively). Analytical data were compared from several viewpoints such as particulate
sizes, locality of sampling sites (either urban or rural) and geographical location of participating countries. Chemical composition
and their monthly variations as well as mass concentrations appear to be highly characteristic for individual sampling sites,
suggesting that NAA data are suitable for evaluating the air quality in each site. 相似文献
947.
948.
Chang-Kyu Kim A. Takaku M. Yamamoto H. Kawamura K. Shiraishi Y. Igarashi S. Igarashi H. Takayama N. Ikeda 《Journal of Radioanalytical and Nuclear Chemistry》1989,131(1):131-137
Ammonium uranates (AU) obtained by the addition of aqueous NH4 OH to a solution of UO2 (NO3)2 or the equilibrium reaction of UO3 · 2H2 O with the vapour over concentrated NH4 OH have been studied by X-ray diffraction (XRD) analysis, diffuse reflectance Fourier transform infrared spectrometry (DR-FTIR) and chemical analysis. Ammonia can be present as either NH3 or NH
4
+
. For precipitates obtained at a pH of 3.7, ammonia in the form of NH3 is predominant. For ammonium uranate obtained by reaction over concentrated NH4OH, most of the ammonia is bonded as NH
4
+
. The reaction mechanism and structures of the products are also discussed. 相似文献
949.
Resolution of enantiomers by HPLC on cellulose derivatives 总被引:4,自引:0,他引:4
Summary Various polysaccharide derivatives, particularly cellulose derivatives, were synthesized and used as chiral stationary phases
for optical resolution by HPLC after being adsorbed on macroporous silica gel. Cellulose triacetate (CTA-II), which was synthesized
under homogeneous conditions, showed a chiral recognition ability for many racemates. Other cellulose derivatives such as
cellulose tribenzoate (OB), cellulose-trisphenylcarbamate (OC), cellulose tribenzyl ether (OE), and cellulose tricinnamate
(OK) also showed unique chiral recognition. Among other polysaccharide derivatives, curdlan triacetate was also exhibited
an effective chiral recognition.
Presented at the 15th International Symposium on Chromatography, Nürnberg, October 1984 相似文献
950.
A. Müller-Groeling G. Soff 《Zeitschrift für Physik D Atoms, Molecules and Clusters》1988,9(3):223-228
Employing the semiclassical approximation we calculate within the coupled-state formalism the ionization probability in antiproton-hydrogen (p+H) collisions. In particular we investigate the adiabatic ionization at the distance of closest approach in almost central collisions. Striking differences in the electron excitation probability compared with proton-hydrogen (p+H) collisions are predicted. 相似文献