Fluorometric investigation of the interaction of bovine serum albumin with surfactants and 6-mercaptopurine

Fluorescence quenching in solutions of bovine serum albumin has been investigated in the presence of 6-mercaptopurine and ionic surfactants. Spectroscopic analysis of the emission quenching at different temperatures revealed that the quenching mechanism of bovine serum albumin by 6-mercaptopurine was dynamic quenching mechanism. The Stern–Volmer quenching model has been successfully applied, and the activation energy of the interaction between 6-mercaptopurine and bovine serum albumin as much as 4.26 kJ mol⁻¹ was calculated. The distance r between donor (bovine serum albumin) and acceptor (6-mercaptopurine) was obtained according to fluorescence resonance energy transfer (FRET). The result of synchronous fluorescence spectra shows that the conformation of bovine serum albumin has been changed at the present of 6-mercaptopurine.     

Efficient solid-phase synthesis of 4,5-dihydro-1,2,4-triazin-6(1H)-ones

A new and easy protocol for the formation of substituted 4,5-dihydro-1,2,4-triazin-6(1H)-ones was developed on solid support. The heterocyclic compounds were formed by nucleophilic reaction of hydrazine on thioamide esters. As cyclization was concomitant with cleavage from the support, substituted 4,5-dihydrotriazinones were obtained in high purity.     

Binding Ensembles of p53-MDM2 Peptide Inhibitors by Combining Bayesian Inference and Atomistic Simulations

Designing peptide inhibitors of the p53-MDM2 interaction against cancer is of wide interest. Computational modeling and virtual screening are a well established step in the rational design of small molecules. But they face challenges for binding flexible peptide molecules that fold upon binding. We look at the ability of five different peptides, three of which are intrinsically disordered, to bind to MDM2 with a new Bayesian inference approach (MELD × MD). The method is able to capture the folding upon binding mechanism and differentiate binding preferences between the five peptides. Processing the ensembles with statistical mechanics tools depicts the most likely bound conformations and hints at differences in the binding mechanism. Finally, the study shows the importance of capturing two driving forces to binding in this system: the ability of peptides to adopt bound conformations (ΔGconformation) and the interaction between interface residues (ΔGinteraction).     

2,2,4-Trimethylhydroquinolines in the Bischler-Melau Reaction

8-R-1-Aryl-4,4,6-trimethyl-4H-pyrrolo[3,2,1-ij]quinolines have been synthesized by the Bischler-Melau reaction in the series of 6-R-2,2,4-trimethylhydroquinolines.     

Additive telluromolybdates. Structure and catalysis in oxidation

Additive telluromolybdates, MoO₃·2TeO₂ and M^IIO·TeO₂·MoO₃ (M^IITeMoO₆; M^II = Co, Mn, Zn), converted ethyl lactate selectively to pyruvate in a vaporphase fixedbed flow system at 250–300 °C. A synergy in activity was observed for binary TeO₂–MoO₃, and crystalline Te₂MoO₇ was suggested as the active species. The Rietveld analysis of powder XRD patterns of ternary CoTeMoO₆ revealed the layer structure quite different from that of the reference Te₂MoO₇, but tellurium was again located adjacent to molybdenum linked through lattice oxygen.     

1-(2,6-二氯-4-硝基苯)-3-(4-硝基苯)-三氮烯与铜的显色反应研究及其应用

研究了新试剂1-(2,6-二氯-4-硝基苯)-3-(4-硝基苯)-三氮烯(DCNPNPT)与铜(Ⅱ)显色反应。在表面活性剂Tween-80存在下,pH 9.0～10.0范围内,铜(Ⅱ)与DCNPNPT形成1:4黄色配合物,其最大吸收波长为460nm,用双峰双波长法测定,表观摩尔吸光系数为1.I×10~5L·mol~(-1)·cm~(-1)。铜(Ⅱ)含量在0～240μg·L~(-1)范围内符合比耳定律。拟定方法用于铜矿和环境水标样中铜的测定,结果满意。     

A Minor New Flavone from Scutellaria baicalensis Georgi

A new flavone,6,2′-dihydroxy-5,7,8,6′-tetramethoxyflavone,was isolated from the roots of Scutellaria baicalensis. Its structure was established on the basis of spectral evidences.     

Photo-initiated base-formation in a polymer matrix

It was found that amines were formed efficiently by the photolysis of O-acyloximes followed by hydrolysis in polystyrene films and the relationship between structures of O-acyloximes and yields of amines were investigated. O-phenylacetyl acetophenone oxime (PaApO), O-pivaloyl acetophenone oxime (PApO), and O-benzoyl acetophenone oxime (BApO) as monofunctional O-acyloximes and O,O′-succinyl diacetophenone oxime (SDApO) and O,O′-glutaryl diacetophenone oxime (GDApO) as bifunctional O-acyloximes were examined. The yields of amines for PaApO and SDApO under N₂ were ca. 70%, which was the highest among O-acyloximes examined in this experiment. On the other hand, the yields for PApO, BApO, and GDApO were less than 15% and it was verified that the hydrogen abstraction by imino radicals via 6-membered cyclic intermediates resulted in the lowering of yields. Although the effect of oxygen under photolysis on the yields of amine for PaApO was negligible under 50% conversion of PaApO, the yield decreased with further increase in the conversion and was 50% at 90% conversion. © 1994 John Wiley & Sons, Inc.     

离子液体介质中FeCl3•6H2O催化下芳香醛与5,5-二甲基-1,3-环己二酮的缩合反应

考察了在离子液体1-正丁基-3-甲基咪唑四氟硼酸盐([bmim][BF₄])介质中, 芳香醛与5,5-二甲基-1,3-环己二酮的缩合反应. 实验结果表明, 在催化量的FeCl₃•6H₂O存在下, 该反应可高产率地生成氧杂蒽二酮类化合物3; 而在TMSCl/FeCl₃•6H₂O复合催化体系的催化下, 则得到氧杂蒽二酮类化合物的开环衍生物4, 反应具有非常好的选择性. 该论文提供的方法操作简单、产率高、选择性好而且对环境友好. 在反应结束后, 所用催化剂及离子液体都很容易回收, 并能有效重复使用.