Synthesis and Antimicrobial Studies of Some Quinolinylpyrimidine Derivatives

The quinolinylpyrimidine derivatives were prepared by the condensation of quinolinyl chalcones with urea (or thiourea) under basic conditions by using both conventional and microwave heating. Their IR, ¹H NMR, ¹³C NMR, mass spectra and CHN analyses confirmed the prepared compounds. The newly prepared quinolinylpyrimidine derivatives were screened for antimicrobial activities against the bacterial strains viz. S. aureus, Shigella, Salmonela, P. aeroginosa, B. Subtilus and E. coli and found considerably active against S. aureus, P. aeroginosa and E. coli.     

Preparation of ethambutol-copper(II) complex and fabrication of PVC based membrane potentiometric sensor for copper

Copper(II) complex of ethambutol (I) was prepared and used in the fabrication of Cu(2+) selective ISE membrane. The membrane having Cu(II)-ethambutol complex (I) as electroactive material, along with sodium tetraphenylborate (NaTPB) as anion discriminator, dioctylphthalate (DOP) as plasticizer in poly(vinyl chloride) (PVC) matrix in the percentage ratio 6:2:190:200 (I:NaTPB:DOP:PVC) (w/w) gave a linear response in the concentration range 7.94x10(-6) to 1.0x10(-1) M of Cu(2+) with a slope of 29.9+/-0.2 mV per decade of activity and a fast response time of 11+/-2 s. The sensor works well in the pH range 2.1-6.3 and could be satisfactorily used in presence of 40% (v/v) methanol, ethanol and acetone and is selective for copper over a large number of cations with slight interference from Na(+) and Co(2+) if present at a level 1.5x10(-5) and 6.5x10(-5) M, respectively. It works well over a period of 6 months and can also be used as indicator electrode for the end point determination in the potentiometric titration of Cu(2+) against EDTA as well as in the determination of Cu(2+) in real samples.     

Metallo-tetraazaporphyrin based anion sensors: regulation of sensor characteristics through central metal ion coordination

The iron(III) and cobalt(III) complexes of 2,3,7,8,12,13,17,18-octakis(benzylthio)-5,10,15,20-tetraazaporphyrin, (OBTAP) were synthesized and incorporated into PVC matrix as ionophores to fabricate anion selective membrane electrodes that exhibit selective potentiometric response to azide and nitrite ions, respectively. The membrane of [Fe(OBTAP)]⁺ (III) with a composition of 6:190:200 (III:DBP:PVC) (w/w), and of [Co(OBTAP)]⁺ (IV) with a composition of 10:148:200 (IV:DOP:PVC) (w/w), i.e. 1a and 2b, respectively (where DBP:dibutylphthalate and DOP=dioctylphthalate) gave the best performance. The membrane 1a showed a slope of 29.2±0.2 mV per decade of activity for N₃⁻ in the working concentration range of 8.9×10⁻⁶ to 1.0×10⁻¹ M. The membrane 2b showed a slope of 30.0±0.2 mV per decade of activity for NO₂⁻ in the working concentration range of 1.1×10⁻⁵ to 1.0×10⁻¹ M. The membranes worked satisfactorily in the pH range of 4.3-10.5 (1a) and 2.8-6.4 (2b) and had fast response time of 12±2 and 13±2 s, respectively. Electrodes exhibited a high degree of selectivity for N₃⁻ and NO₂⁻, respectively, over several other monovalent and bivalent anions. Only SCN⁻ and S²⁻ (at >1.0×10⁻⁴ M) cause moderate interference for electrode 1a and Cl⁻ and S²⁻ (at >1.0×10⁻⁵ M) for electrode 2b. They gave reproducible results with the relative standard deviation in the observed values of potentials (σ) of 1.96 and 1.80 mV for electrodes 1a and 2b, respectively, from the least-squares fit line. The 90% confidence limit lies within ±0.2 mV per decade of activity. Reproducible results were obtained over a period of 5 months. Their performance in non-aqueous solvent mixtures having up to 50% (v/v) methanol, ethanol and acetone were evaluated and were found satisfactory. The proposed sensors are superior in terms of detection limit and response time in comparison to the reported ones.     

On-column derivatization of the antibiotics teicoplanin and ristocetin coupled to affinity capillary electrophoresis

Binding constants between the glycopeptides teicoplanin (Teic) and ristocetin (Rist) and their derivatives to D-Ala-D-Ala terminus peptides were determined by on-column receptor synthesis coupled to partial-filling affinity capillary electrophoresis (PFACE) or affinity capillary electrophoresis (ACE). In these techniques, the column is first partially filled with increasing concentrations of D-Ala-D-Ala terminus peptides. This is followed by plugs of buffer, antibiotic and two noninteracting standards, and acetic and/or succinic anhydride (and buffer in the case of ACE). The order of the reagent plugs containing the antibiotic and anhydride varies with the charge of the glycopeptide. Upon electrophoresis, the antibiotic reacts with the anhydride yielding a derivative of Teic or Rist. Continued electrophoresis results in the overlap of the derivatized antibiotic and the plug of D-Ala-D-Ala peptide. Analysis of the change in the relative migration time ratio (RMTR) of the new glycopeptide relative to the standards, as a function of the concentration of the D-Ala-D-Ala ligand yields a value for the binding constant K(b). The techniques described here can be used to assess how the derivatization of drugs alters their affinities for target molecules.     

Decision Rules Derived from Optimal Decision Trees with Hypotheses

Conventional decision trees use queries each of which is based on one attribute. In this study, we also examine decision trees that handle additional queries based on hypotheses. This kind of query is similar to the equivalence queries considered in exact learning. Earlier, we designed dynamic programming algorithms for the computation of the minimum depth and the minimum number of internal nodes in decision trees that have hypotheses. Modification of these algorithms considered in the present paper permits us to build decision trees with hypotheses that are optimal relative to the depth or relative to the number of the internal nodes. We compare the length and coverage of decision rules extracted from optimal decision trees with hypotheses and decision rules extracted from optimal conventional decision trees to choose the ones that are preferable as a tool for the representation of information. To this end, we conduct computer experiments on various decision tables from the UCI Machine Learning Repository. In addition, we also consider decision tables for randomly generated Boolean functions. The collected results show that the decision rules derived from decision trees with hypotheses in many cases are better than the rules extracted from conventional decision trees.     

Tilianin: A Potential Natural Lead Molecule for New Drug Design and Development for the Treatment of Cardiovascular Disorders

Cardiovascular disorders (CVDs) are the leading risk factor for death worldwide, and research into the processes and treatment regimens has received a lot of attention. Tilianin is a flavonoid glycoside that can be found in a wide range of medicinal plants and is most commonly obtained from Dracocephalum moldavica. Due to its extensive range of biological actions, it has become a well-known molecule in recent years. In particular, numerous studies have shown that tilianin has cardioprotective properties against CVDs. Hence, this review summarises tilianin’s preclinical research in CVDs, as well as its mechanism of action and opportunities in future drug development. The physicochemical and drug-likeness properties, as well as the toxicity profile, were also highlighted. Tilianin can be a natural lead molecule in the therapy of CVDs such as coronary heart disease, angina pectoris, hypertension, and myocardial ischemia, according to scientific evidence. Free radical scavenging, inflammation control, mitochondrial function regulation, and related signalling pathways are all thought to play a role in tilianin’s cardioprotective actions. Finally, we discuss tilianin-derived compounds, as well as the limitations and opportunities of using tilianin as a lead molecule in drug development for CVDs. Overall, the scientific evidence presented in this review supports that tilianin and its derivatives could be used as a lead molecule in CVD drug development initiatives.     

Li5ReN4, ein Lithium–Nitridorhenat(VII) mit anti‐Flußspat‐Überstruktur

Li₅ReN₄, a Lithium Nitridorhenate(VII) with Anti Fluorite Superstructure At 673 K Li₃N reacts with Re powder under N₂ to pale yellow, microcrystalline Li₅ReN₄. The structure determination is based on X‐ray powder data: Spacegroup Pmmn (No. 59), Z = 2, a = 6.719(1) Å, b = 6.627(1) Å, c = 4.893(1) Å. The compound crystallizes in an anti‐type of a fluorite superstructure. In comparison to the aristo‐type – CaF₂ – in Li₅ReN₄ tetrahedral interstices of a ccp nitrogen partial structure are unoccupied. The distribution of these vacancies is related with its orthorhombic distortion. Under aspects of crystal chemistry the tetragonally crystallizing compounds Li₆MN₄ with M = Mo, W result by partially filling up such vacancies.     

Counting Closed Orbits of Hyperbolic Diffeomorphisms

In this paper we count closed orbits of a hyperbolic diffeomorphism restricted to a basic set. In fact we shall be dealing with two types of extensions of a hyperbolic diffeomorphism: a finite group extension (also called G-extensions) and also an automorphism extension (also called (G, ρ)-extensions). In particular we present Chebotarev type theorems and prime orbit theorem for such diffeomorphisms. These counting results are in the form of an asymptotic formula derived in complete analogy with the number theoretic result. The main difficulty is extending the domain of analyticity of the zeta and L-functions and this is overcome by resorting to symbolic dynamics. Unlike the case of a flow, the proof of this extension result does not rely on the properties of the Ruelle–Perron–Frobenius operator. Also the counting results do not use any tauberian theorems. Received: January 7, 2005.     

Dynamics of the Hantavirus infection through variational iteration method

This paper studies the dynamics of the Hantavirus infection model, which was originally developed by Abramson and Kenkre [G. Abramson, V.M. Kenkre, Spatiotemporal patterns in the hantavirus infection, Phys. Rev. E 66 (2002) 011912], by using a simple analytical method called the variational iteration method or VIM. The results obtained by the variational iteration method are compared with the classical Runge–Kutta method (fourth-order) to gauge its effectiveness. Numerical values from these analyses provide us with some useful observation on the behaviour of the infection subjected to certain conditions.