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

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.

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Publication Details

Journal
Turkish Journal of Analytical Chemistry
Published
2024-11-19
DOI
https://doi.org/10.51435/turkjac.1514896
Primary Topic
Pharmacogenetics and Drug Metabolism
Type
article
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article

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

Göknil Pelin Coşkun, Kaan Birgül, Mert Ülgen, İnci Selin Doğan et al.
Turkish Journal of Analytical Chemistry
Pharmacogenetics and Drug Metabolism
article

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

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

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.

Turkish Journal of Analytical ChemistryVol. 6(2)
Bahçeşehir University (TR), Karadeniz Technical University (TR), Acıbadem University (TR)
Good health and well-being
Openalex Percentile: Top 73%
Pharmacogenetics and Drug Metabolism
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Metabolic stability of a hydrazone derivative: N′-[(4-chlorophenyl)methylidene)]-4-[(4-methylphenyl)sulfonyloxy]benzohydrazide — Göknil Pelin Coşkun, Kaan Birgül, et al. · Turkish Journal of Analytical Chemistry (2024) | TGRS Research Map | TGRS