From recipe to research: introducing undergraduate students to the nature of science using a hybrid practical course centred on drug discovery for neglected diseases

Edink, Ewald; Linden, Oscar P.J. van; Zheng, Yang; Blaazer, Antoni R.; Siderius, Marco; Muijlwijk‐Koezen, Jacqueline E. van

doi:10.1016/j.drudis.2021.02.012

Cited by 8 publications

(10 citation statements)

References 33 publications

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“…The following bachelor students are greatly acknowledged for their technical assistance: Soogand Ansaryma-habady, Thijs Bakker, Joshua Bekman, Lazar Buckic, Fleur van Bussel, Rafael Feijs, Wiebe Fontein, Tim Giele, Mees van Haasen, Mariska Hendricks, Jimmy Huynh, Alette Kooiker, Marc Minnema, Ylana Rijsbergen, Miranda Ruiter, Mattijn Steenmeijer, Maaike Storck, Hidde Strabbing, Karen Swart, Ovidiu Todoran, Simone Verkaik, Kyromina Wahba, Marco van Wijk, and Roy Zuidema. This opportunity enabled them to get acquainted with the nature of science [ 69 , 70 ], the importance of which we have discussed previously [ 71 ], in two essential areas of science: health and sustainability. In addition, the need for training future scientists to have a “green” research mindset is evident [ 72 , 73 ].…”

Section: Acknowledgmentsmentioning

confidence: 99%

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (CyreneTM)

et al. 2023

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Biomass-derived molecules can provide a basis for sustainable drug discovery. However, their full exploration is hampered by the dominance of millions of old-fashioned screening compounds in classical high-throughput screening (HTS) libraries frequently utilized. We propose a fragment-based drug discovery (FBDD) approach as an efficient method to navigate biomass-derived drug space. Here, we perform a proof-of-concept study with dihydrolevoglucosenone (CyreneTM), a pyrolysis product of cellulose. Diverse synthetic routes afforded a 100-membered fragment library with a diversity in functional groups appended. The library overall performs well in terms of novelty, physicochemical properties, aqueous solubility, stability, and three-dimensionality. Our study suggests that Cyrene-based fragments are a valuable green addition to the drug discovery toolbox. Our findings can help in paving the way for new hit drug candidates that are based on renewable resources.

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Section: Acknowledgmentsmentioning

confidence: 99%

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (CyreneTM)

et al. 2023

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“…The course serves to bridge the gap between secondary education and university chemistry in terms of content level, and accommodates 50 to 90 students per year. The teacher has more than 10 years of teaching experience at the undergraduate and graduate level and has a track record of implementing educational innovations. − At the time (2014), the course consisted of lectures and tutorials with a ratio of 2:1. It already had activities to engage students in active learning during lectures and tutorials, such as electronic multiple choice (MC) questions both in an introductory quiz administered during the first lecture and as formative questions throughout all lectures …”

Section: Phase I: the Development Of The Redesign Guidelinesmentioning

confidence: 99%

Practical Guidelines to Redesign Introductory Chemistry Courses Using a Flexible and Adaptive Blended Format

et al. 2021

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Incorporation of increased flexibility and adaptivity in courses can support freshmen with taking responsibility for their learning process. This is especially beneficial in the case of chemistry courses given their typically abstract nature and associated need for engaging in practice and higher order thinking. Blended learning can be used to achieve course flexibility and adaptivity, and increased student engagement. Adopting blended learning requires teachers to reconsider and redesign their course setup. The willingness for this will largely be dictated by perceived practicality, however. To this end, our aim is to develop practical redesign guidelines for flexible blended learning. Such guidelines need to be instrumental, congruent, and of ‘low cost’ for a teacher. The resulting four guidelines were fine-tuned in two phases over 5 years using two introductory chemistry courses and incorporated various blended learning elements, such as slide-cast lectures, live lectures, formative in-cast multiple choice questions, tutorials, formative electronic tutorial questions, and student voting on the course schedule. The outcome of our multiyear endeavor was positive and sustainable by all metrics used, including online engagement by students, learning outcomes, and student evaluations. The teachers in phase II largely embraced the guidelines emerging from phase I, and in their course experienced them predominantly as practical while limitations were also identified. We hope that our guidelines and experiences can provide fellow teachers with a blueprint for practical incorporation of flexibility and adaptivity using blended learning in their chemistry courses.

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“…At the time of this writing, there is a large literature of CUREs, with the majority in the biological sciences , and biochemistry and a growing but smaller number of CUREs in chemistry, − specifically in the field of organic chemistry. − The application of synthetic organic chemistry in the context of a medicinal-chemistry-inspired project involving library synthesis and a biological assay lends itself well to the CURE model. − The number of CUREs in organic and medicinal chemistry is growing, and all have their own specific merits. However, there are some limitations that are addressed by the CURE presented herein.…”

Section: Introductionmentioning

confidence: 99%

“…For example, some CUREs require a full semester, which, while providing ample time for iteration and failure, can limit implementation in institutions that lack flexibility in their laboratory course curricula. Additionally, while some CUREs allow students to synthesize a small-molecule library for biological testing, in many cases the students are not able to carry out the biological assay themselves. ,− While this model allows students who do not have access to a biology laboratory to carry out medicinal-chemistry-inspired research, it does limit students’ participation in truly collaborative research. Furthermore, some CUREs use reagents that pose significant safety hazards (i.e., sodium cyanide, potassium cyanide, OsO 4 , pyrophoric reagents such as LAH, NaH in DMF, and/or TFA , ) or require the target compounds to be rigorously pure for biological assays .…”

Section: Introductionmentioning

confidence: 99%

“…Additionally, while some CUREs allow students to synthesize a small-molecule library for biological testing, in many cases the students are not able to carry out the biological assay themselves. ,− While this model allows students who do not have access to a biology laboratory to carry out medicinal-chemistry-inspired research, it does limit students’ participation in truly collaborative research. Furthermore, some CUREs use reagents that pose significant safety hazards (i.e., sodium cyanide, potassium cyanide, OsO 4 , pyrophoric reagents such as LAH, NaH in DMF, and/or TFA , ) or require the target compounds to be rigorously pure for biological assays . Finally, while some CUREs provide students with the opportunity to troubleshoot routes to synthesize known bioactive molecules, in many cases the biological activities of these compounds are already known, , preventing students from having the opportunity to analyze how simple changes in molecular structure can have an impact in a given biological system.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Biological Assay of Small-Molecule Quorum Sensing Inhibitors: A Three-Week Course-Based Undergraduate Research Experience

et al. 2021

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From recipe to research: introducing undergraduate students to the nature of science using a hybrid practical course centred on drug discovery for neglected diseases

Cited by 8 publications

References 33 publications

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (CyreneTM)

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (CyreneTM)

Practical Guidelines to Redesign Introductory Chemistry Courses Using a Flexible and Adaptive Blended Format

Synthesis and Biological Assay of Small-Molecule Quorum Sensing Inhibitors: A Three-Week Course-Based Undergraduate Research Experience

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