abordagem didÁtica para o desenvolvimento de molÉculas bioativas: regra dos cinco de lipinski e preparaÇÃo de heterociclo 1,3,4-oxadiazol em forno de micro-ondas domÉstico
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ID: 187628
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Abstract
In Brazil, the development of new chemical entities (NEQ) is still limited to small advances in the academic and public research sectors, the authors understand that this is a sector of the pharmaceutical industry that needs encouragement. Accepting that education transforms society, educate students in the development of bioactive molecules, it’s a way to stimulate the national pharmaceutical industry to invest in the sector. Thus, this work brings a didactic sequence, applicable in undergraduate courses, which exemplifies some stages of development of the NEQ through its rational planning. The synthesis of a 1,3,4-oxadiazole heterocycle was planned and its potentiality assessed through the Lipinski’s Rule of Five (RO5), using the ChemSpider® database. Once in accordance with RO5, the heterocycle was prepared using a simple and accessible methodology, using microwaves for domestic use as heating source. The 2-phenyl-5-(pyridin-4-yl)-1,3,4-oxadiazole was synthesized by oxidative cyclization of acylhydrazone and an overall yield of 90%. So was possible to demonstrate in a practical way some steps for the development of a substance with potential biological activity and thus to attract greater interest of undergraduate students by this follow-up of the Medicinal Chemistry.
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| Authors | ;Victória Laysna dos Anjos Santos;Arlan de Assis Gonsalves;Cleônia Roberta Melo Araújo |
| Journal | greece and rome |
| Year | Year not found |
| DOI |
10.21577/0100-4042.20170135
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