Retention-activity relationship studies of benzodiazepines by micellar liquid chromatography

Kinetic and Conformational Studies of Adenosine Deaminase Upon Interaction with Oxazepam and Lorazepam

“…As confirmed by the partition coefficient data [31], it is evident that both drugs have near similar degrees of hydrophobicity; yet lorazepam is more hydrophobic and can establish a better interaction with the enzyme, which is validated by both the kinetic and structural results. The mixed inhibition system, observed in the case of oxazepam at 27 °C conforms to the fact that oxazepam is more hydrophilic (has a smaller octanol/water partition coefficient) and can establish a minute degree of interaction with the polar residues of the enzyme; the increase in the temperature leads to the increased hydrophobicity; which in turn leads to the observation of noncompetitive inhibition in the case of oxazepam at 37 °C.…”

Biopartitioning micellar chromatography to predict skin permeability

“…In order to compare the predictive ability of the model in terms of cross-validated data, the RMSEC and RMSECV values for the QRAR model were obtained essentially as in Martens and Naes (1989) and Molero-Monfort et al (1999). The RMSEC and RMSECV values, 0.498 and 0.537 respectively, were similar suggesting the reliability of the model as well as adequate predictive ability of the current QRAR model.…”

Profiling Drug Membrane Permeability and Activity Via Biopartitioning Chromatography

“…Medina-Hernandez research group first put forward BMC system and suggested that the surfactant in the micellar solution of BMC should be Brij35, which best models the biological behavior of different kinds of drugs [89][90][91][92][93][94]. It is proposed that the characteristics of the BMC systems are similar to in vivo biological conditions: firstly, the stationary phase modified by hydrophobic adsorption of Brij35 surfactant monomers structurally resembles the ordered array of the membranous hydrocarbon chains, and the hydrophilic character of the adsorbed surfactant monomers resembles the polar membrane regions; secondly, Brij35 micellar mobile phases could also mimic the environment of drug biological partitioning, where phospholipids, cholesterol, fatty acids and triglycerides form micellar complexes with proteins (lipoproteins) in the extracellular and intracellular fluids.…”

“…Medina-Hernandez research group had extended the QRAR model based on BMC to investigate activity and toxicity for various types of drugs, such as antihistamine drugs, benzodiazepines, pesticides, butyrophenones, antipsychotics, antidepressant drugs, aromatic amines, anilines and phenols and so [89][90][91][92][93][94][95][96][97][98][99][100]. Recently, other research groups also adopted this method to carry out pharmacokinetic/pharmacodynamic study for quinolones, cardiovascular system drugs and antihypertensive drugs, etc [101][102][103][104].…”