Biomedical subjects

A Paleti

Publications and source records attributed to A Paleti.

2 recordsLinked to original sources

PubMed1999

Quantitative structure-activity relationship study on some nonpeptidal cholecystokinin antagonists.

A quantitative structure-activity relationship (QSAR) analysis has been performed on a series of 1,4-benzodiazepine derivatives, which were found to act as antagonists of cholecystokinin (CCK), a gastrointestinal peptide hormone. The CCK acts with three different receptor subtypes termed as CCK-A, CCK-B, and gastrin receptor, which can be found in peripheral system, brain, and stomach, respectively. With all the three subtypes, the binding of the compounds is found to significantly depend on the lipophilicity of the compounds and their ability to form the hydrogen bonds with the receptor. However, the binding sites in CCK-A receptor seem to be slightly rigid as compared to those in CCK-B or gastrin receptor. The latter two appear to have similar binding features.

Animals↗

PubMed1998

Quantitative structure-activity relationship studies on some nonbenzodiazepine series of compounds acting at the benzodiazepine receptor.

Quantitative structure-activity relationship (QSAR) studies have been made on a few non-benzodiazepine series of compounds such as 3-substituted imidazo[1,2-b]pyridazines, 2-phenylimidazo[1,2-alpha]pyridines, 2-(alkoxycarbonyl) imidazo[2,1-b]benzothiazoles, and 2-arylquinolines. For the first series of compounds a Fujita-Ban approach has been followed, which revealed the highest activity contribution for 3,4-OCH2O group of 2-phenyl moiety and for a methoxy group at 6-position. For the rest of the series, a Hansch approach has been adopted. The hydrophobic and electronic properties of the various substituents have been found to play major roles in the binding of these compounds with the receptor. Based on these studies, a hypothetical model for the drug-receptor interaction has been proposed.

Animals↗