Synthesis of a new drug candidate trough molecular hybridization and application as a learning strategy / Síntese de um novo candidato à fármaco através de hibridação molecular e aplicação como estratégia de aprendizagem

Leyliane Teixeira Dias dos Santos, Mariana Lopes Teixeira, Jaqueline Carneiro


Introduction: Molecular hybridization is a synthesis strategy in which new molecules are obtained by linking two drugs or pharmacophoric groups. Skin conditions treatment, such as acne, generally  requires the association of drugs, for instance, sulfacetamide and salicylic acid. The present study aimed to synthesize and characterize a new drug candidate by molecular hybridization using sulfacetamide and salicylic acid. We also intended to further explore and evaluate this synthesis as a practical educational strategy for undergraduate students. Methods: The synthesis was carried out through an azo coupling reaction between the aromatic amine from sulfacetamide and the ring from salicylic acid. The compound obtained was characterized by melting point and infrared spectroscopy (IR). A short course was developed and applied to evaluate the impact of this synthesis and its discussion in class. The evaluation was performed using an initial and a final questionnaire. Results: The compound was obtained as an orange solid (41%), with a melting point of 108 ºC, and showing as main IR bands: 3247-3041 cm-1, 1662 cm-1, 1608 cm-1, 1439 cm-1. The data from the questionnaires showed that the students improve their knowledge of drug development strategies (73%). Discussion: The experimental evidences suggest the formation of a new chemical entity, possibly the proposed hybrid. Besides, the questionnaire results suggest that new teaching methodologies mixing theoretical-practical moments, allowed students to better understand a specific issue. Conclusion: The proposal synthesis showed to be viable and an interesting possibility to approach several issues with pharmacy undergraduate students in a multidisciplinary way.


organic synthesis, diazotization, short course, pharmacy education.


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