engleski

Stability of amidino substituted benzothiazole derivatives with antitumor activity

This study focused on the forced degradation tests as one of the routine stability testing methods in the pharmaceutical industry to investigate the stability of benzothiazoles. In recent years, these newly synthesized compounds have attracted attention in medicinal chemistry as potential biological agents with antitumor activity. In general, the performance of stress tests according to the guideline ICH [1] is necessary with the aim of determining and characterizing newly formed by- products (organic, inorganic) that may ultimately affect the safety and efficacy of the active ingredients. In order to investigate the intrinsic stability and possibly identify newly formed degradation products, some amidino-substituted benzothiazol compounds were exposed to different environmental conditions. Photolytic, hydrolytic, oxidative and thermal degradation of the main compound were applied. High resolution mass spectrometry technique (UHPLC-QTOF- MS /MS) was used for separation, identification and characterization of the above compounds. Based on the spectral data obtained, preliminary structures of the major degradation products with proposed degradation pathways of the identified products were given. REFERENCES [1] International Conference on Harmonization (ICH), Stability Testing of new drug substances and products, Q1A (R2), IFPMA, Geneva, 2003.

forced degradation, benzothiazoles, mass spectrometry

nije evidentirano