Biginelli Reaction and [Beta]-Secretase Inhibition: A Multicomponent Reaction as a Friendly Educational Approach to Bioactive Compounds

Autor/inn/en	Funicello, Maria; Cerminara, Iole; Chiummiento, Lucia; Lupattelli, Paolo; Felluga, Fulvia; Berti, Federico
Titel	Biginelli Reaction and [Beta]-Secretase Inhibition: A Multicomponent Reaction as a Friendly Educational Approach to Bioactive Compounds
Quelle	In: Journal of Chemical Education, 98 (2021) 5, S.1756-1761 (6 Seiten)Infoseite zur Zeitschrift PDF als Volltext Verfügbarkeit
Zusatzinformation	ORCID (Funicello, Maria) ORCID (Lupattelli, Paolo) ORCID (Felluga, Fulvia) ORCID (Berti, Federico)
Sprache	englisch
Dokumenttyp	gedruckt; online; Zeitschriftenaufsatz
ISSN	0021-9584
DOI	10.1021/acs.jchemed.0c01298
Schlagwörter	Organic Chemistry; Experiments; Advanced Courses; Introductory Courses; Course Objectives; Course Evaluation; Biochemistry + Suchen Sie Ihr Suchwort? Organische Chemie; Erprobung; Fortgeschrittenenunterricht; Einführungskurs; Biochemie
Abstract	Multicomponent reactions (MCRs) represent very interesting tools to reach eco-friendly and sustainable transformations in organic chemistry. In particular, the Biginelli reaction furnishes a very easy approach to the synthesis of a library of biological active compounds in an academic course. Here we describe the realization of several experiments involving the synthesis of potential inhibitors of [beta]-secretase by the Biginelli reaction. All of the obtained compounds were tested with a FRET fluorimetric assay. The experiments were proposed to students either at entry level or during advanced laboratory courses of organic and bioorganic chemistry. The learning objectives at the advanced level were to introduce the students to the practice of combinatorial synthesis and to the evaluation of biological activity of combinatorial libraries by enzyme inhibition assays. The meeting of the learning objectives was probed first by analyzing their daily performance in the laboratory and their increasing proactive attitude, and the contents of their final presentations. The resulting marks obtained by the students were compared with the average evaluation of their career. Second, the students were asked to evaluate the course and their own experience, and the outcome of their evaluation was compared with that of the teachers. (As Provided).
Anmerkungen	Division of Chemical Education, Inc. and ACS Publications Division of the American Chemical Society. 1155 Sixteenth Street NW, Washington, DC 20036. Tel: 800-227-5558; Tel: 202-872-4600; e-mail: eic@jce.acs.org; Web site: http://pubs.acs.org/jchemeduc
Erfasst von	ERIC (Education Resources Information Center), Washington, DC
Update	2024/1/01