Synthesis of Fluoroflavones as Potential Neuroprotective Agents

Flavones are polyphenol natural products that are known to have neuroprotective effects against many diseases caused by the formation of reactive species. Flavonoids are subgroup of flavones and they are believed to function as antioxidants. Specifically, they target free radicals and eliminate its harmful effect on the cell. Fluoroflavones were designed to improve the potency of the antioxidant activity and potentially be used as neuroprotective agents. A monofluorinated and trifluoromethylated flavone were synthesized by using commercially available fluorination reagents, N-fluorobenzenesulfonimide; and Togni’s or Umemoto\u27s respectively. After the synthesis of the desired flavones and their monofluorinated and trifluoromethylated derivatives, biological testing was conducted. First, antioxidant activity was evaluated by using DPPH antioxidant assay and displayed that the fluorinated flavones are more potent compared to their non-fluorinated derivatives. Second, 19 FNMR experiments were conducted to investigate the effect of fluorination on the antioxidant activity of flavones

Synthesis of Fluoroflavonoids As Potential Antioxidant Against Alzheimer’s Disease.

Overview: Maali Alshammari joined the lab of Professor David A. Colby in spring of 2017; she\u27s currently a third-year Ph.D. student in medicinal chemistry in the graduate program in the Department of BioMolecular Sciences at the University of Mississippi. Maali\u27s project involves the syntheses of fluoroflavones to improve the potency of the antioxidant activity of the original non-fluorinated flavones. The fluoroflavones will potentially be used as neuroprotective agents to prevent the toxic effect of ROS and used to prevent neurogenerative diseases like Alzheimer\u27s. Intellectual Merit: We are in need of medications that prevent Alzheimer\u27s disease or even reverse its damage; all of the approved medications are aimed to manage its symptoms delaying the progression of them; most importantly, none of the approved ones target the toxic reactive oxygen species (ROS). I\u27m designing fluoroflavones to improve the potency of the antioxidant activity and potentially use them as neuroprotective agents. A monofluorinated flavone will be synthesized by using commercially available starting materials and fluorination reagents. After the synthesis of the desired flavones and their monofluorinated derivatives, biological testing will be conducted to see if the fluorinated flavones are more potent than their non-fluorinated derivatives. External Opportunity: I\u27m applying to the 2020 Alzheimer\u27s drug discovery foundation (ADDF) young investigator travel scholarship and award; it also includes graduate students who\u27re conducting research related to Alzheimer\u27s. This funding opportunity will cover the registration fee to attend the 14th drug discovery for neurodegeneration workshop, I will be presenting a poster with my research findings and I will also have the chance to win the outstanding poster presentation award that will be awarded to three individuals from the 25 young investigator travel scholarship winners. Each scholarship provides a name recognition in the program and on the conference website. Attending this workshop will give me insights on the current research projects targeting Alzheimer\u27s and the chance to network with pharmaceutical companies, this meeting which will be held in Philadelphia, PA from April 26th to 28th, 2020, I\u27m planning to submit the abstract (the proposal) in the last week of January, before the deadline on January 31, 2020

Synthetic Studies on Valuable Fluorinated Building Blocks

Fluorine chemistry plays a diverse role in the pharmaceutical, agricultural, and material industries. In fact, around 25% of pharmaceuticals and 40% of agrochemicals contain at least one fluorine atom. The incorporation of fluorine into pharmaceuticals or natural products can increase bioavailability by enhancing lipophilicity, metabolic stability, and overall pharmacokinetics properties. Our laboratory has designed a method to generate difluoroenolates from pentafluoro-gem-diols. This reactivity can be used to produce molecules displaying a difluoromethyl group. The reaction occurs through the release of trifluoroacetate. We improved the design and synthesis of fluorinated derivatives of flavones and measured their antioxidants activities. This work expanded the understanding of structure-activity relationships of the flavone class of natural products for use in neurodegenerative disorders. The search for selective and more efficient fluorination methods is of interest to academia and industry as the demand for fluorinated building blocks increases. We utilized the difluoroenolates from the trifluoroacetate releases in synthesizing difluorinated α-haloketones and alcohols. This work enables the preparation of valuable difluorinated molecules, which can serve as building blocks in drug discovery. We also investigated the reactivity of under-explored fluorinated functional groups, like the pentafluorosulfanyl group. The pentafluorosulfanyl (SF5) group is one of the most recent additions to the fluorinated functional groups. We characterized the stability of the pentafluorosulfanyl group by examining different aromatic pentafluorosulfanyl compounds. We believe these studies will introduce novel reactivity that can be utilized to develop fluorinated molecules

Navigating post COVID-19 education: an investigative study on students’ attitude and perception of their new normal learning environment

Background The incidence and aftermath of the COVID-19 pandemic brought about a drastic change in health professional education around the world. Traditional classrooms made way for online classrooms in order to ensure that learning continued in a safe and secure environment. However, how well health professional students perceived and accepted these changes have not been fully gauged yet. Therefore, this study aims to evaluate the perception of health professional students about their new educational climate. Methods A modified and validated Dundee Ready Education Environment Measure (DREEM) questionnaire was used to collect data regarding student perception of their educational environment. Results The mean DREEM scores for three time periods were in the accepted positive range of 101 to 150 indicating that most of the students perceived the changes positively. The results indicated that most students preferred blended learning over online learning or face-to-face learning alone. Areas where students were unsatisfied with their learning environment that need improvement were identified by poor item-wise scores. Conclusion Strategic remedial measures for these concerns need to be developed to improve the quality of education received by the students. However, the results of our study indicated that most of the students were able to adapt positively to the new education environment due to the change in the circumstances during COVID