Synthesis, structure elucidation and in vitro microsomal metabolism of adamantane hydrazide-hydrazone derivatives
Acta Pharmaceutica Sciencia, cilt.61, sa.1, ss.65-79, 2023 (Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 61 Sayı: 1
- Basım Tarihi: 2023
- Doi Numarası: 10.23893/1307-2080.aps6105
- Dergi Adı: Acta Pharmaceutica Sciencia
- Derginin Tarandığı İndeksler: Scopus, EMBASE
- Sayfa Sayıları: ss.65-79
- Anahtar Kelimeler: Adamantane, hydrazide-hydrazone, hydrolysis, in vitro metabolism
- Acıbadem Mehmet Ali Aydınlar Üniversitesi Adresli: Evet
Özet
The discovery of adamantane has led to the researchers to find different drug molecules which exhibit diverse biological activities. On the other hand, hydrazide-hy-drazones possess strong anticancer, antibacterial, antienflamatory and antiseptic activites. However, we have limited knowledge on the metabolic profiles of ada-mantane hydrazide-hydrazones. The metabolic pathway of adamantane hydrazide-hydrazones emerged to be an important step for pre-clinical drug discovery studies. In this study, the metabolic profile of adamantane hydrazones was the main mo-tivation for our research group. The synthesis of hydrazide-hydrazone derivatives as substrates of this study was performed via condensation of corresponding hy-drazide with aldehyde and ketone and their authentic metabolites were also synthe-sized. Following their structures were elucidated with spectroscopic methods, their in-vitro microsomal metabolic study was performed. The results indicated that the aldehyde derivative is susceptible to metabolic hydrolysis, whereas ketone derivative is stable for metabolic changes. LC-MS results proved the metabolic hydrolysis.