Medicinal Chemistry is a multidisciplinary discipline and the discovery of new bioactive molecules is one of its objectives. Molecular Hybridization (MH) is a strategy of rational design of new prototypes, where the lead compound is produced through an adequate fusion of pharmacophoric sub-unities. Undergraduate laboratory experiments for Medicinal Chemistry education with a focus on MH are scarce. Therefore, the present paper describes a practice class for some undergraduate courses (Pharmacy, Chemistry and/or Chemical Engineering) involving drug development and MH that can be performed at low cost. In this work, alternative materials such as paracetamol and sulfadiazine tablets were used to engage student's attention and to contextualize important concepts of MH. The experiment describes the synthesis of a new compound involving the azo coupling between an aromatic amine (sulfadiazine) and a phenol (paracetamol) to show undergraduate students a practical example of MH. In this case, SciFinder
®
- a search website of the American Chemical Society - was also demonstrated and utilized as a search tool in the proposed experimental class.
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RESUMO Objetivo: verificar a ocorrência e o tipo mais frequente de alteração auditiva em crianças expostas a toxoplasmose durante a gestação. Métodos: estudo retrospectivo longitudinal realizado em instituição pública de saúde de São Paulo. Análise de prontuários de crianças nascidas entre 2010 e 2015 distribuídos em dois grupos: grupo estudo, composto por 48 crianças de mães com diagnóstico de toxoplasmose durante a gestação; e grupo controle, composto por 43 crianças sem infecção congênita que foram acompanhadas por apresentar baixo peso ao nascimento. As crianças foram avaliadas de duas a quatro vezes durante os dois primeiros anos de vida, por meio de testes que avaliam a função auditiva periférica e central. Resultados: 47 crianças fizeram apenas duas avaliações e apenas 11 completaram todas as avaliações até 24 meses. No grupo controle 58,1% apresentaram audição normal, 37,2% perda condutiva, 4,7% perda coclear e ausência de alteração retrococlear, enquanto o grupo estudo apresentou 56,3% de audição normal, 20,8% de perda condutiva, 2,1% de perda coclear e 20,8% de alteração retrococlear. Conclusão: crianças expostas à toxoplasmose durante a gestação não diferiram das não expostas em relação à ocorrência de perda auditiva coclear e condutiva. Entretanto, apresentaram maior ocorrência de alteração retrococlear.
Recebido em 26/9/12; aceito em 26/3/13; publicado na web em 14/5/13 CONTEXTUALIZING ACID-BASE REACTIONS ACCORDING TO BRÖNSTED-LOWRY PROTONIC THEORY USING PROPRANOLOL AND NIMESULIDE TABLETS. This paper reports the use of alternative materials for teaching experimental chemistry. In this context, nimesulide and propranolol tablets were used to teach chemical concepts about acid-base reactions according to Brönsted-Lowry protonic Theory. Important topics of Organic, Analytical and Pharmaceutical Chemistry were discussed, such as purification by acid-base extraction, solubility of organic compounds in aqueous solutions, buffers, the dissociation constant (pK a ), potentiometric titration and ionization of drugs in biological fluids. The purification of propranolol and nimesulide from tablets produced yields of 75% and 90%, respectively. The experimental values of pK a for both drugs were in agreement with those from the literature.
There are still no valid, clinically feasible instruments to assess backward masking (BM), an auditory temporal processing (ATP) phenomenon. The aim of this study was to develop, standardize and present evidence of validity for a behavioral test for BM assessment. Young adults were submitted to a BM test (BMT), where they were asked to identify a 1000 Hz pure tone followed by a narrowband noise with interstimulus intervals of 0 to 400 ms and signal-to-noise ratio (SNR) between −20 and −30 dB. The correct response rate and target sound detection threshold were calculated, and the results compared with those of young adults with abnormal ATP tests and older adults. Diagnostic accuracy analyses were carried out. Young adults with normal ATP obtained an average correct response rate of 89 and 87% for SNR −20 and −30 dB, respectively, with average thresholds between 10 and 15 ms and no difference between the left and right ears. Results were more consistent at SNR −20 dB, and the best diagnostic accuracy was obtained for SNR −20 dB, with good specificity, but low sensitivity. Normative values were obtained for the BMT, which proved to be clinically feasible, with preliminary evidence of validity.
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