RESUMEN
α-Glycosidase inhibition is one of the main approaches to treat Diabetes mellitus. Polyphenolic moieties are known to be responsible for yielding exhibit potent α-glycosidase inhibitory effects. In addition, compounds containing benzothiazole and Schiff base functionalities were previously reported to show α-glycosidase inhibition. In this paper, the synthesis of seven new phloroglucinol-containing benzothiazole Schiff base derivatives through the reaction of 6-substituted-2-aminobenzothiazole compounds with 2,4,6-trihydroxybenzaldehyde using acetic acid as a catalyst was reported. The synthesized compounds were characterized using spectroscopic methods such as FT-IR, 1H NMR, 13C NMR, and elemental analysis. The synthesized compounds were evaluated for their inhibitory effects on α-glycosidase, compounds 3f and 3g were found to show significant inhibitory properties when compared to the positive control. The IC50 values of 3f and 3g were calculated as 24.05 ± 2.28 and 18.51 ± 1.19 µM, respectively. Kinetic studies revealed that compounds 3f and 3g exhibited uncompetitive mode of inhibition against α-glycosidase. Molecular modeling predicted druglikeness for the title compounds and underpinned the importance of phloroglucinol hydroxyls for interacting with the key residues of α-glycosidase.
Asunto(s)
Benzotiazoles , Inhibidores Enzimáticos , Polifenoles , Benzotiazoles/química , Benzotiazoles/farmacología , Benzotiazoles/síntesis química , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/síntesis química , Polifenoles/química , Polifenoles/farmacología , Polifenoles/síntesis química , Relación Estructura-Actividad , Estructura Molecular , Glicósido Hidrolasas/antagonistas & inhibidores , Glicósido Hidrolasas/metabolismo , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/síntesis química , Simulación del Acoplamiento Molecular , Humanos , Relación Dosis-Respuesta a Droga , alfa-Glucosidasas/metabolismo , CinéticaRESUMEN
INTRODUCTION: Computer Engineering Students (CES) and Medical Students (MS) will actively participate in the management of health information system in the future. AIM: The aim of the study was to evaluate the views of CES and MS about the patient privacy and security of health information systems. METHODS: The participants of this cross-sectional study were the 3rd and 4th year CES of Marmara University, (n=163, F/M:71/92) and the 5th and 6th year MS of Marmara University (n=65, F/M:38/27). The data were collected via questionnaire comprising questions and statements about patient information security and confidentiality. Responses were prepared on the basis of 5 Point Likert Scale. RESULTS: During the assessment of the questionnaires, it was observed that the statement "Health records should be accessible to the other health workers besides the physician" discomforted more CES (93,3%) than MS (78,5%) (p=0.003). A similar proportion was observed about "On-line communication with the physician" more CES (87,1%) prefer to communicate with the physician via electronic media than do the MS (66,2%) (p=0.001). Another significant point to be noted about the questionnaire results was that slightly more CES (40,5%) favor restrictions on the accessibility of "personal correspondance information" than MS (35,4%) (p>0.05). CONCLUSION: In the future, CES, who will be both internal and external stakeholders of the multi-disciplinary structure of healthcare management, thought that problems regarding security and privacy may occur. Therefore, the relation between health information system and the occupational education and training of CES and MS are extremely important through the perspective in healthcare management.