The polytopal association scheme

Summary The polytopal association scheme for PBIB designs is introduced and studied utilizing the concept of clustering of treatments.     

Cabibbo angle and quark masses in a four-quark model of quantum flavordynamics

The Cabibbo angle is related through spontaneous symmetry breaking to the masses of the light quarks in an illustrative model of quantum flavordynamics based on the SU_2L × SU_2R × U₁ flavor gauge group and on four quark flavors. The agreement with experiment is quite good.     

Magnetic moments ofb-quark baryons in broken SU(5) symmetry

The magnetic moments ofb-quark baryons within the framework of five quark models are derived. Also the transition magnetic moments of variousb-quark baryons are calculated.     

Direct observation of the modulation of the 4f-electron orbital state by strong p-f mixing in CeSb

Low-temperature x-ray diffraction experiment has been carried out to investigate the 4 f-electron state of the low carrier density system CeSb which shows complicated magnetic phase diagrams at low temperatures. The scattering pattern of the satellite peaks observed in the magnetically ordered state AFP3 is explained well by the model which takes into account both the lattice and charge modulations corresponding to the complex magnetic structure. The present result gives direct evidence for the strong modulation of the 4 f-electron orbital state in CeSb due to the combined effect of the strong p-f mixing and carrier localization.     

2-hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide (DRF-4367): an orally active COX-2 inhibitor identified through pharmacophoric modulation

Analogs of 1,5-diarylpyrazoles with a novel pharmacophore at N1 were designed, synthesized and evaluated for the in-vitro cyclooxygenase (COX-1/COX-2) inhibitory activity. The variations at/around position-4 of the C-5 phenyl ring in conjunction with a CF3 and CHF2 groups at C-3 exhibited a high degree of potency and selectivity index (SI) for COX-2 inhibition. The in-vivo evaluation of these potent compounds with a few earlier ones indicated the 4-OMe-phenyl analog and the 4-NHMe-phenyl analog with a CF3, and the 4-OEt-phenyl analog with a CHF2 group at C-3 to possess superior potency than celecoxib. In addition to its impressive anti-inflammatory, antipyretic, analgesic and anti-arthritic properties, compound (DRF-4367) was found to possess an excellent pharmacokinetic profile, gastrointestinal (GI) safety in the long-term arthritis study and COX-2 potency in human whole blood assay. Thus, compound was selected as an orally active anti-inflammatory candidate for pre-clinical evaluation.     

Detachable immobilization of liposomes on polymer gel particles

Immobilization of liposomes on hydrophobized Sephacryl gel and controlled detachment of the liposomes from the gel were examined. The gel was chemically modified and bore octyl, hexadecyl or cholesteryl moiety via disulfide linkage as anchors to liposomal bilayer membrane. Upon interaction with the gel, egg phosphatidylcholine liposomes were successfully immobilized onto the gel. The gel with cholesteryl moiety showed 1.7 times higher liposome immobilization per anchor moiety than the gels with the alkyl moieties. The immobilization of liposomes on the gel was stable, and no significant spontaneous detachment of phospholipid or leakage of fluorescein isothiocyanate-conjugated dextran encapsulated in the immobilized liposomes was observed in 24h. Reductive cleavage of the disulfide linkage by dithiothreitol resulted in detachment of the liposomes from the gel. The majority of the detached liposomes were found encapsulating the dextran derivative, and these liposomes should have kept their structural integrity throughout the immobilization and the detachment processes. The release of the liposomes was insignificant until the ratio of the dithiothreitol to the hydrophobic anchor reached a threshold. The presence of the threshold suggests that the immobilization of liposomes should require a certain minimum number of the hydrophobic moieties anchored in the liposomal membrane. By applying the present immobilization-detachment system, preparation of liposomes encapsulating the dextran derivative without using costly gel filtration or ultracentrifugation procedure was successfully demonstrated.