A new class of arylpiperazine derivatives: the library synthesis on SynPhase lanterns and biological evaluation on serotonin 5-HT(1A) and 5-HT(2A) receptors

An efficient solid-supported method for the synthesis of a new class of arylpiperazine derivatives containing amino acid residues has been developed. A 72-membered library was synthesized on SynPhase Lanterns functionalized by a BAL linker. A one-pot cleavage/cyclization step of aspartic and glutamic acid derivatives yielded succinimide- and pyroglutamyl-containing ligands (chemsets 9 and 10). The library representatives under study showed different levels of affinity for 5-HT(1A) and 5-HT(2A) receptors (estimated K(i) = 24-4000 and 1-2130 nM, respectively). Several dual 5-HT(1A)/5-HT(2A) ligands were found, of which two (9(3,3) and 9(3,5)) displayed high 5-HT(2A) affinity comparable to that of the reference drug ritanserin. A set of individual fragment contributions for the prediction of 5-HT(1A) and 5-HT(2A) affinity of all the library members were defined on the basis of the Free-Wilson analysis of 26 compounds. An alkylarylpiperazine fragment had essentially the same impact on the affinity for both receptors, whereas different terminal amide fragments were preferred by 5-HT(1A) (chemset 17, R(2) = adamantyl) and 5-HT(2A) (chemset 9, R(2) = norborn-2-ylmethyl) binding sites.     

Recurrence Relations for the Coefficients in Series Expansions with Respect to Semi-Classical Orthogonal Polynomials

Let {P _k } be a sequence of the semi-classical orthogonal polynomials. Given a function f satisfying a linear second-order differential equation with polynomial coefficients, we describe an algorithm to construct a recurrence relation satisfied by the coefficients a _k [f] in f= _k a _k [f]P _k . A systematic use of basic properties (including some nonstandard ones) of the polynomials {P _k } results in obtaining a recurrence of possibly low order. Recurrences for connection or linearization coefficients related to the first associated generalized Gegenbauer, Bessel-type and Laguerre-type polynomials are given explicitly.     

A new approach to the integrated calibration in flow injection analysis

A new proposal how to perform the analytical procedure according to the integrated calibration method is presented. An original flow injection system has been designed for this purpose. When using only a single standard solution, the measurement information gathered during a single analytical course permits construction of four calibration graphs and calculation of as many as four independent estimations of the analyte concentration in the sample examined. As the calibration method applied integrates the set of standards method and the standard addition method, the analytical estimations may be obtained in both the interpolative and the extrapolative manner and the final result can be effectively verified in terms of accuracy. The system developed was experimentally tested on the example of spectrophotometric determination of chromium. It has been proved to be capable of saving time and reagents as well as providing reliable analytical results. Owing to the instrumental simplicity and analytical efficiency the system is expected to be useful for routine analysis.     

Sampling sets and sufficient sets for A

We give new characterizations of the subsets S of the unit disc of the complex plane such that the topology of the space A^−∞ of holomorphic functions of polynomial growth on coincides with the topology of space of the restrictions of the functions to the set S. These sets are called weakly sufficient sets for A^−∞. Our approach is based on a study of the so-called (p,q)-sampling sets which generalize the A^−p-sampling sets of Seip. A characterization of (p,q)-sampling and weakly sufficient rotation invariant sets is included. It permits us to obtain new examples and to solve an open question of Khôi and Thomas.     

On Herbrand consistency in weak arithmetic

We prove that the G?del incompleteness theorem holds for a weak arithmetic T = IΔ₀ + Ω₂ in the form

Deactivation of the S2 and Two Lowest Triplet States of 4H-1-Benzopyran-4-thione and Its Alkyl Derivatives in Methanol Solution

Spectral and photochemical properties of three aromatic thioketones, 4H-1-benzopyran-4-thione and its two alkyl derivatives, in their second excited singlet and two lowest triplet states have been a subject of stationary and time-resolved studies. Quantum yields of emissions from the above-mentioned states as well as lifetimes of these states have been measured. The results indicate an important role of intermolecular solvent-induced processes in deactivation of the excited states of the thioketones studied. The possible mechanism of these processes involves hydrogen atom abstraction and/or formation of exciplex. For relatively high thione concentrations, the contribution of self-quenching in deactivation of the triplet states becomes significant. The effect of the alkyl chain in a thione molecule on deactivation parameters is discussed.     

Depletion potentials between colloids and patterned surfaces

Effective interactions between the hard-sphere colloids and the patterned substrates created by depositing one or more hemispheres on the structureless walls are studied. The deposition of only one hemispherical cap gives rise to a new global minimum of the depletion potential but the difference from the planar hard wall case is moderate. On the other hand, when the hemispherical caps form a periodic array, multiple overlaps of the excluded volumes lead to formation of deep global minimum of the depletion potential. In some cases this minimum is deeper than −10k_BT and this is more than triple of the potential minimum for the structureless wall. We conclude that templated surfaces affect depletion potentials significantly. This effect will have a major impact even when the residual attractive/repulsive interactions are present.