Background. Intravenous lipid emulsion (ILE) is recommended as a "rescue" treatment for local anaesthetic (LA) toxicity. A purported mechanism of action suggests that lipophilic LAs are sequestered into an intravascular "lipid-sink," thus reducing free drug concentration. There is limited data available correlating the effects of ILE on LAs. Aims. To compare the in vitro effect of ILE on LA con...

Lipophilicity is a physicochemical property of crucial importance in medicinal chemistry. On the molecular level it encodes information on the network of inter- and intramolecular forces affecting drug transport through lipid structures as well as drug's interactions with the target protein. In result, on the organism level, lipophilicity is an important factor defining pharmacokinetics and pha...

We report QSAR calculations using VolSurf descriptors to model the lipophilicity of 53 Pt(iv) complexes with a diverse range of axial and equatorial ligands. Lipophilicity is measured using an efficient HPLC method. Previous models based on a subset of these data are shown to be inadequate, due to incompatibility of whole molecule descriptors between carboxylato and hydroxido ligands. Instead, ...

The series of nine amides of substituted 8-hydroxyquinolines were prepared. The synthetic procedures of compounds are presented. All the prepared quinoline derivatives were analyzed using RP-HPLC method for the lipophilicity measurement and their lipophilicity were determined. The prepared compounds were tested for the reduction of chlorophyll content in Chlorella vulgaris Beij. Several compoun...

Quantitative structure-property relationship models were developed for the prediction of pesticides and some PAH compounds lipophilicity based on a wide set of computational molecular descriptors and a set of experimental chromatographic data. The chromatographic lipophilicity of pesticides has been evaluated by high-performance liquid chromatography (HPLC) using different chemically bonded (C1...

Acylation of an intermediate tetrahydroxoplatinum(IV) complex, [Pt(OH)4(dach)] (dach = trans-(±)-1,2-diaminocyclohexane), with one or two kinds of carboxylic anhydrides in stepwise manner afforded various carboxylatoplatinum(IV) complexes, [Pt(O2CR)x(OR’)4−x(dach)] (R = (CH2)3CH3 or C(CH3)3, R’ = H or OCCH3, and x = 1-4) with a wide range of lipophilicity. The title complexes were subjected to ...

This work studied the structure-hepatic disposition relationships for cationic drugs of varying lipophilicity using a single-pass, in situ rat liver preparation. The lipophilicity among the cationic drugs studied in this work is in the following order: diltiazem > propranolol > labetalol > prazosin > antipyrine > atenolol. Parameters characterizing the hepatic distribution and elimination kinet...

The relationship between lipophilicity and CYP2D6 affinity of cyclic tertiary (N-alkyl-4-phenyl-1,2,3,6-tetrahydropyridines) and quaternary (N-alkyl-4-phenylpyridinium) amines was examined. The 1,2,3,6-tetrahydropyridine scaffold was chosen due to its common occurrence in the structures of CYP2D6 ligands such as the Parkinsonian neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and...

E-2-Arylmethylen-1- tetralones and E-3-phenylme thylene chromanone-4-ones and their derivatives closely related to flavonoids belong to the plant secondary metabolites most investigated recently.The class of flavonoids is an enormous class of plant secondary metabolites having so different pharmacological effects as inhibition of nitric oxide synthasecancer preventive effect or potential impact...