OBJECTIVES Vector-borne diseases are still a major mortality factor in Africa and South-east Asia and effective mosquito repellents are therefore needed. An efficient and safe in-vitro assay system using artificial blood and skin substitute could facilitate the development of novel repellents, as most assays currently rely on human subjects or vertebrate whole blood. Moreover, examining the ski...

The lipophilicity (R(MW)) of betamethasone and its four related compounds: betamethasone-17,21-dipropionate, betamethasone-17-valerate, betamethasone-21-valerate and also betamethasone disodium phosphate was determined by reversed phase HPTLC and various mobile phase systems (methanol-water, dioxane-water and acetonitrile-water). The chromatographic lipophilicity parameters obtained for all exa...

We propose a reversed phase HPLC (RP-HPLC) with an alkaline-resistant silica-based stationary phase, XBridge Shield RP(18), for the determination of the lipophilicity of drugs with diverse chemical nature ranging from acidic to basic. A set of 40 model compounds with well-defined solvatochromic parameters was selected to allow a broad distribution of structural properties. The chromatographic r...

Lipophilicity of chemicals and drug candidates is normally described in terms of octanol/water partitioning and log P. We investigated an alternate approach to lipophilicity determination using a mimic of an alkyl alcohol with compound partitioning quantified using acoustic sensing. A self-assembled monolayer composed of HSC(10)(CH(2)CH(2)O)(6)C(18) was formed on planar gold electrodes of a pie...

Bioactive compounds generally need to cross membranes arrive at their site of action. The octanol-water partition coefficient (lipophilicity, logPOW) has proven be an excellent proxy for membrane permeability. In modern drug discovery, logPOW and bioactivity are optimized simultaneously, which fluorination is one the relevant strategies. question arises as extent often subtle logP modifications...

The parameters of lipophilicity of spironolactone (a single member of steroids group), which is widely applied as diuretic and antihypertensive agent, were experimentally determined by reversed-phase TLC and HPLC methods as well as calculated using different computer programs and also by a novel mode based on topological indices. Various stationary phases, such as RP-18WFA4254, RP-2F254, RP-18F...

The retention behavior for a series of amine neurotransmitters, their precursors, metabolites and structurally related drugs has been investigated in reversed-phase thin-layer chromatography using RP-18, RP-8, RP-2, CN and Diol stationary phases and mixtures of phosphate buffer and methanol as mobile phase. According to the computed lipophilicity of the neutral form of the investigated compound...

The transmembrane anion transport activity of a series of synthetic molecules inspired by the structure of tambjamine alkaloids can be tuned by varying the lipophilicity of the receptor, with carriers within a certain log P range performing best.