METHOD: Hydrazinyl thiazole substituted coumarins 4-20 were synthesized via two step reaction. First step was the acid catalyzed reaction of 3-formyl/acetyl coumarin derivatives with thiosemicarbazide to form thiosemicarbazone intermediates 1-3, followed by the reaction with different phenacyl bromides to afford products 4-20. All the synthetic analogs 4-20 were characterized by different spectroscopic techniques such as EI-MS, HREI-MS, 1H-NMR and 13C-NMR. Stereochemical assignment of the iminic double bond was carried out by the NOESY experiments. Elemental analysis was found in agreement with the calculated values.
RESULTS: Compounds 4-20 were screened for α-amylase inhibitory activity and showed good activity in the range of IC50 = 1.829 ± 0.102-3.37 ± 0.17 µM as compared to standard acarbose (IC50 = 1.819 ± 0.19 µM). Compounds were also investigated for their DPPH and ABTS radical scavenging activities and displayed good radical scavenging potential. In addition to that molecular modelling study was conducted on all compounds to investigate the interaction details of compounds 4- 20 (ligands) with active site (receptor) of enzyme.
CONCLUSION: The newly identified hybrid class may serve as potential lead candidates for the management of diabetes mellitus.
AIM: This study seeks to evaluate the effective radiation doses associated with common diagnostic and treatment procedures, as well as propose diagnostic reference levels (DRLs), within two nuclear medicine centers in Madinah, Saudi Arabia.
METHODOLOGY: Data from 445 patients were gathered from two nuclear medicine centers in the Madinah region of Saudi Arabia. The data were categorized based on the type of nuclear medicine (NM) procedure, the chemical composition of the administered radiopharmaceutical, as well as patient age and weight. Effective radiation doses for prevalent NM procedures were computed, and suggested DRLs were formulated.
RESULTS: Effective radiation doses were analyzed for 16 adult and 2 pediatric NM procedures (divided into 8 groups). The effective radiation doses for adult diagnostic nuclear medicine procedures range from 0.05 mSv (Nanocoloid) to 29 mSv (67Ga-citrate). For pediatric procedures, the doses range from 0.80 mSv (5-year-old undergoing renal DTPA) to 1.6 mSv (1-year-old undergoing renal DMSA). Furthermore, DRL values were determined for both adult and pediatric NM procedures. The study's findings demonstrated a high degree of concordance between effective radiation doses and DRL values, aligning well with previously published research.
CONCLUSION: While the effective radiation doses outlined in this study were generally within acceptable limits and consistent with prior research findings, optimizing radiation doses remains imperative, particularly for pediatric NM procedures.