Metabolic stability of a hydrazone derivative: N′-[(4-chlorophenyl)methylidene)]-4-[(4-methylphenyl)sulfonyloxy]benzohydrazide

Year 2024, , 97 - 101, 20.12.2024

Hasan Erdinç Sellitepe , Göknil Coşkun , Kaan Birgül , Mert Ülgen , İnci Selin Doğan

https://doi.org/10.51435/turkjac.1514896

Abstract

Metabolic stability, a key parameter in drug development, refers to a drug substance's resistance to metabolism. The failure rate can be significantly reduced by conducting metabolism studies for the drug candidate compound from the early stages. These studies are primarily carried out on in vitro microsomal enzymes, which play a crucial role in the process. Various analytical methods, predominantly liquid chromatography, can be used for analysis. In this context, we conducted metabolic stability studies of a hydrazone-sulfonate derivative compound previously synthesized by our group, the biological activity of which was investigated. Metabolic stability was determined by LC-MS/MS on rat microsomes in vitro. Analyses were performed at 0., 5., 10., 15, 30, and 60. minutes during incubation. The analysis revealed that the stability of the compound was highly cofactor-dependent, maintaining its stability without cofactor and in a buffer medium.

Keywords

metabolism, hplc, metabolic stability, hydrazone

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