The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

The activities of aldehyde oxidase and xanthine oxidase were determined in partially purified preparations from livers and kidneys of male and female Dhubb, Uromastyx microlepis, four times daily at equal intervals. The maximum activity of male and female hepatic aldehyde oxidase appeared at 2100 h, whereas the minimum activity was observed at 0300 h, using phthalazine and 3-methylisoquinoline ...

The goal of this study was to provide a reasonable assessment of how probe substrate selection may impact the results of in vitro aldehyde oxidase (AO) inhibition experiments. Here, we used a previously studied set of seven known AO inhibitors to probe the inhibition profile of a pharmacologically relevant substrate N-[(2dimethylamino)ethyl]acridine-4-carboxamide (DACA). DACA oxidation in human...

Common marmosets (Callithrix jacchus), New World monkeys, are a promising primate model for preclinical drug metabolism studies because of the similarities of cytochrome P450 (P450) enzyme function to those of humans. Despite an increasing number of drug candidates catalyzed by non-P450 enzymes, drug metabolizing enzymes other than P450s have been hardly identified or characterized in marmosets...

The bacterial burden on human health is quickly outweighing available therapeutics. Our long-term goal is the development of antimicrobials with the potential for broad-spectrum activity. We previously reported phthalazine-based inhibitors of dihydrofolate reductase (DHFR) with potent activity against Bacillus anthracis, a major component of Project BioShield. The most active molecule, named RA...