Pyrrolopyridine analogs of nalidixic acid. 1. Pyrrolo[2,3-b]pyridines

A series of 4,7-dihydro-4-oxo-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acids was synthesized from ethyl 5-methyl(or 5H)-2-aminopyrrole-3-carboxylate. The starting pyrroles were obtained by reaction of carbethoxyacetamidine with bromoacetone or chloroacetaldehyde. One compound ( 10 ) showed antibacterial activity in vitro.     

Conversion of 3-benzoyl-1-methyl-4-phenyl-γ-piperidol by arylamines and arylhydrazines. Synthesis of 3-arylamino-1-oxo-1-phenylpropanes and 1,3-diarylpyrazoles and their fragmentation under electron impact

It has been established that on heating, 3-benzoyl-4-hydroxy-1-methyl-4-phenylpiperidine is ring-opened in the presence of arylamines by a type of retroaldol reaction, with subsequent transamination of the intermediate Mannich base and the formation of 3-arylamino-1-oxo-1-phenylpropanes. When using arylhydrazines this γ-piperidol is recyclized with the formation of 1,3-diarylpyrazoles and their 4,5-dihydro derivatives. The mass spectral behavior of a series of 3-arylamino-substituted 1-phenylpropanones has been studied. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1486–1495, October, 2007.     

用硼酸作催化剂一锅法合成双（二氢化嘧啶酮-4-基）苯

A simple effective synthesis of bis(dihydropyrimidinone-4-yl)benzene derivatives, using boric acid as catalyst,from isophthalic aldehyde or terephthalic aldehyde, 1,3-dicarbonyl compounds and urea or thiourea in glacial acetic acid was described. As the expansion of the classical Biginelli reaction, this method has the advantage of excellent yields 83%-94% and short reaction time 0.5-1.5 h.     

Optical sensor for the detection of caspase-9 activity in a single cell

We demonstrate for the first time, the application and utility of a unique optical sensor having a nanoprobe for monitoring the onset of the mitochondrial pathway of apoptosis in a single living cell by detecting enzymatic activities of caspase-9. Minimally invasive analysis of single live MCF-7 cells for caspase-9 activity is demonstrated using the optical sensor which employs a modification of an immunochemical assay format for the immobilization of nonfluorescent enzyme substrate, Leucine-GlutamicAcid-Histidine-AsparticAcid-7-amino-4-methylcoumarin (LEHD-AMC). LEHD-AMC covalently attached on the nanoprobe tip of an optical sensor is cleaved during apoptosis by caspase-9 generating free AMC. An evanescent field is used to excite cleaved AMC and the resulting fluorescence signal is detected. By quantitatively monitoring the changes in fluorescence signals, caspase-9 activity within a single living MCF-7 cell was detected. By comparing of the fluorescence signals from apoptotic cells induced by photodynamic treatment and nonapoptotic cells, we successfully detected caspase-9 activity, which indicates the onset of apoptosis in the cells.     

Thermodynamics of binding of 2-methoxy-3-isopropylpyrazine and 2-methoxy-3-isobutylpyrazine to the major urinary protein

In the present study we examine the thermodynamics of binding of two related pyrazine-derived ligands to the major urinary protein, MUP-I, using a combination of isothermal titration calorimetry (ITC), X-ray crystallography, and NMR backbone (15)N and methyl side-chain (2)H relaxation measurements. Global thermodynamics data derived from ITC indicate that binding is driven by favorable enthalpic contributions, rather than the classical entropy-driven hydrophobic effect. Unfavorable entropic contributions from the protein backbone and side-chain residues in the vicinity of the binding pocket are partially offset by favorable entropic contributions at adjacent positions, suggesting a "conformational relay" mechanism whereby increased rigidity of residues on ligand binding are accompanied by increased conformational freedom of side chains in adjacent positions. The principal driving force governing ligand affinity and specificity can be attributed to solvent-driven enthalpic effects from desolvation of the protein binding pocket.     

The co-production approach to service: a theoretical background

The paper develops a theoretical background on the co-production approach as an extension of operations management principles, in which co-production function assumes well-defined functional form with the input presence of both firm and customers. The co-production approach not only views a customer as a co-producer, but also conducts strategic trade-offs between a firm and customers in service systems. Moreover, the value and the process of value co-creation are also explored under the co-production approach. The experimental study with a hypothetical service system indicates that the co-production function is feasible under economic and institutional considerations, and the co-production approach generalizes both the firm approach and the customer approach. Furthermore, the co-production approach creates many rich opportunities for future research on service operations management.     

A splitting algorithm for equilibrium problem given by the difference of two bifunctions

In this paper, we introduce a splitting algorithm for solving equilibrium problems given by the difference of two bifunctions in a real Hilbert space. Under suitable assumptions on component bifunctions, we prove strong convergence of the proposed algorithm. In contrast to most existing projection-type methods for equilibrium problems, our algorithm does not require any convexity or monotonicity conditions on the resulting bifunction. Some numerical experiments and comparisons are given to illustrate the efficiency of the proposed algorithm.