Lipophilicity Modulations by Fluorination Correlate with Membrane Partitioning

Partitioning and lipophilicity in quantitative structure-activity relationships.

The history of the relationship of biological activity to partition coefficient and related properties is briefly reviewed. The dominance of partition coefficient in quantitation of structure-activity relationships is emphasized, although the importance of other factors is also demonstrated. Various mathematical models of in vivo transport and binding are discussed; most of these involve partit...

Prediction of Lipophilicity and Pharmacokinetics of Chloroacetamides by Chemometric Approach

In this study, the existence of biological potential of selected N-(substituted phenyl)-2-chloroacetamides was examined none empirically, as was the possibility of applying simpleexperimental technique in predicting essential properties which affect the biological activityof the compounds. By applying the Lipinski and Ghose’s rules, it has been revealed that theexamined chloroacetamides fulfill...

Detection of Toxoplasma Parasitemia by PCR: Does it Correlate with IgG and IgM Antibody Titers?

Background: Toxoplasmosis is a zoonotic disease with high seroprevalence worldwide. Several immunological methods have been described for diagnosis of toxoplasmosis. Objective: To determine the parasitemia period in patients infected with toxoplasma using PCR and comparing serological data with molecular results. Methods: 154 serum samples from patients with toxoplasmosis were examined. Presenc...

Targeted fluorination with the fluoride ion by manganese-catalyzed decarboxylation.

We describe the first catalytic decarboxylative fluorination reaction based on the nucleophilic fluoride ion. The reported method allows the facile replacement of various aliphatic carboxylic acid groups with fluorine. Moreover, the potential of this method for PET imaging has been demonstrated by the successful (18) F labeling of a variety of carboxylic acids with radiochemical conversions up ...

Enhanced Ovarian Folliclular Development by Metformin Does Not Correlate with Pregnancy Rate: A Randomized Trial