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
AUTOR(ES)
Santos, Victória Laysna dos Anjos, Gonsalves, Arlan de Assis, Araújo, Cleônia Roberta Melo
FONTE
Quím. Nova
DATA DE PUBLICAÇÃO
2018-01
RESUMO
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.
Documentos Relacionados
- Monoqueima de porcelanas esmaltadas em forno de micro-ondas
- Preparação e caracterização de absorvedores de micro-ondas à base de polipirrol/epóxi.
- Determinação espectrofotométrica de hexametilenotetramina (HMT) em medicamentos, utilizando ácido cromotrópico e forno de micro-ondas
- Utilização de irradiação micro-ondas na polimerização em emulsão
- Sinterização ultra-rápida de pós submicrométricos de CoFe2O4 por micro-ondas