Combinatorial Chemistry & High Throughput Screening - Volume 10, Issue 5, 2007

One of the high impact events to celebrate during 2007 is the 40th anniversary of the publication of the first supramolecular chemistry paper (Pedersen, C.J. J. Am. Chem. Soc., 1967, 89, 2495-2496) and its coincidence with the 20th anniversary of the Nobel Prize recognizing the pioneers in this field, namely, Charles J. Pedersen (1904-1989), Donald J. Cram (1919-2001) and Jean-Marie Lehn (1939). The vigorous and impressiv Read More

A review is given from the stand-point of applying methods utilizing electrospray ionization - mass spectrometry (ESI-MS) for quantitative binding (affinity and selectivity) determinations in small molecule host-guest (receptorligand, selector-selectand, etc.) systems. Advantages over more commonly utilized and traditional solution phase approaches, both in the context of developing new chiral selector molecules for separa Read More

Chiral separations facilitated using microchip devices are reviewed in this paper. The first research paper on this topic was published in 1999. It was seen that analysis times are greatly reduced compared with more conventional techniques such as liquid chromatography and capillary electrophoresis, and that these devices enable the separation of chiral molecules. Method optimization can be conducted in a rather eas Read More

One of the enantiomers of a racemic drug may be pharmacologically inactive or toxic or ballast and, hence, U.S. FDA and European agencies have issued certain guidelines for marketing of optically active (homochiral) drugs. However, some homochiral drug enantiomers racemize in to human body leading to the generation of other antipodes, which may be toxic or ballast to the human beings. In addition, racemization reduces Read More

Dendrimers are a new class of artificial macromolecules with well-defined hyperbranched structures which enable bio-active molecules such as drugs to be presented in a highly multi-valent fashion. Covalent conjugation of drugs to the surface of dendrimers can be easily achieved either by direct chemical reactions between dendrimers and drug molecules including esterification and amidation or through cleavable linkers, d Read More

The molecular recognition behaviors of some representative bile salts by three 3,6'-bridged β-cyclodextrin dimers with oligo(ethylenediamino) linkers in different lengths, i.e. 3,6'-(ethylenediamino-bridged) β-cyclodextrin dimer (1), 3,6'-(diethylenetriamino-bridged) β-cyclodextrin dimer (2), and 3,6'-(triethylenetetraamino-bridged) β-cyclodextrin dimer (3), were investigated in aqueous phosphate buffer solution (pH 7.20) at 2 Read More

Interaction of the antipsychotic drug risperidone with hydroxypropyl-beta-cyclodextrin (HPBCD) in solution and in the solid state was studied with the aim of overcoming the limitations associated with nasal administration of low solubility drugs. Risperidone solubility studies revealed inclusion complex formation with a 1:1 stoichiometry. Low concentrations (0.1 w/v %) of hydroxypropylmethyl cellulose (HPMC) and carbomer aff Read More

Biomimetic poly(amidoamine)-poly(benzyl L-glutamate) (PAMAM-PBLG) amphiphiles with multi-armed architecture were synthesized by the ring-opening polymerization (ROP) of β-benzyl-L-glutamate N-carboxyanhydride (BLG-NCA) using primary amine-terminated PAMAM dendrimer as the macroinitiator. Both 1H NMR and 13C NMR demonstrated that all the primary amines of PAMAM participated in initiating the ROP of BLG- Read More

The changes in antioxidant compounds of Brassica oleracea L. var. costata DC seeds were monitored during the first twelve days of seedling development. Sprouts were screened at time intervals of two days for phenolic compounds and organic acids. The identified phenolic compounds included esters of sinapic acid with glucose, gentiobiose and kaempferol, as well as sinapoylcholine. The organic acids were oxalic, aconi Read More

The effect of different chromatographic conditions, such as buffer concentration and type of organic modifier, on the retention behavior of nine tricyclic neuroleptics on three different RP-HPLC columns was investigated. Two recently developed columns, calixarene-bonded (CALTREX® AIII) and monolithic (Chromolith® Performance RP-18e) columns, were compared with a conventional RP-C18 HPLC column (LiChrospher®). Read More