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A library of N-benzylpyridinium-based compounds, 7a-j and 8a-j, was designed and synthesised as potential acetylcholinesterase) AChE (inhibitors. An in vitro assay for the synthesised compounds showed that most compounds had significant AChE inhibitory activities at the nanomolar and submicromolar levels. The benzyl (8a) and fluoro (8b) derivatives were the most active, with IC50 values ≤56 nM. Compound 7f, which had a benzyl moiety, showed the highest potency among all the target compounds, with an IC50 value of 7.5 ± 0.19 nM against AChE, which was higher than that of the activities of tacrine (IC50 = 30 ± 0.2 nM) and donepezil (IC50 = 14 ± 0.12 nM). Compounds with vanillin moieties exhibited antioxidant activity. Among the tested compounds, four derivatives (7f, 7 g, 8f, and 8 g) exhibited superior AChE inhibitory activity, with Ki values of 6–16 nM, which were potent in the same range as the approved drug, donepezil. These compounds showed moderate antioxidant activities, as indicated by the results of the ABTS assay. [ABSTRACT FROM AUTHOR]

Although several interventions are utilized for pain management, opioids remain the most effective intervention for moderate to severe pain. Despite opioids being the most potent analgesics used in different pain settings, several factors impede the optimal prescribing of opioids. The study seeks to identify and address the barriers physicians face to prescribing opioids in managing pain. This study was conducted in a tertiary care center in Riyadh, Saudi Arabia. It involved distributing questionnaires to the participants. The questionnaires sought to identify prescribers' knowledge and current practices as well as obstacles that they face when prescribing opioids. A total of 109 questionnaires were completed by participants. More than half [59.6%] of the respondents thought that opioid use was an optimal way to treat moderate to severe pain. About 33% chose "never" when asked if they fear legal sanctions when prescribing opioids. Fear of side effects limited almost 90% of the respondents from prescribing opioids. The study confirmed the perception that opioids are the most potent pharmacological intervention in treating pain. Several barriers were identified and discussed in this study. Further studies from different settings to understand these barriers are highly recommended. [ABSTRACT FROM AUTHOR]

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