Publicação
Synthesis of new positive allosteric modulators of the AMPA receptors belonging to the benzothiadiazine chemical class
| Resumo: | Nowadays, neurological diseases have become a growing challenge for health systems in developed and developing regions. Over the past half century, pharmaceutical research has helped transform mental illnesses from misunderstood causes of shame and fear into highly treatable conditions. Although several efforts have been made to develop the research in this area, new strategies are still needed to overwhelm these diseases trend. Among the numerous strategic possibilities, AMPApams arises as a new and interesting approach. In fact, in the last years, the Laboratory of Medicinal Chemistry at the ULg developed an extensive research on AMPApams belonging to the benzothiadiazine class. Recently, a crystallographic study of a GluA2 dimer subunit suggested that the synthesis of dimers of benzothiadiazines could lead to a new class of superligands. Therefore, we herein present a synthetic strategy for the synthesis of four different dimers. The synthesis of these superligands comprises several challenging steps which difficult the conclusion of their synthesis. However, we managed to synthesize one dimer, ameliorated the yields of numerous steps and the full synthesis of the other dimers will certainly be performed more easily thanks to the work disclosed herein. |
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| Autores principais: | Farias, Gonçalo Diogo Vaz Filipe |
| Assunto: | Glutamate AMPA AMPApam Benzothiadiazines Dimers Mestrado Integrado - 2014 |
| Ano: | 2014 |
| País: | Portugal |
| Tipo de documento: | dissertação de mestrado |
| Tipo de acesso: | acesso restrito |
| Instituição associada: | Universidade de Lisboa |
| Idioma: | inglês |
| Origem: | Repositório da Universidade de Lisboa |
| Resumo: | Nowadays, neurological diseases have become a growing challenge for health systems in developed and developing regions. Over the past half century, pharmaceutical research has helped transform mental illnesses from misunderstood causes of shame and fear into highly treatable conditions. Although several efforts have been made to develop the research in this area, new strategies are still needed to overwhelm these diseases trend. Among the numerous strategic possibilities, AMPApams arises as a new and interesting approach. In fact, in the last years, the Laboratory of Medicinal Chemistry at the ULg developed an extensive research on AMPApams belonging to the benzothiadiazine class. Recently, a crystallographic study of a GluA2 dimer subunit suggested that the synthesis of dimers of benzothiadiazines could lead to a new class of superligands. Therefore, we herein present a synthetic strategy for the synthesis of four different dimers. The synthesis of these superligands comprises several challenging steps which difficult the conclusion of their synthesis. However, we managed to synthesize one dimer, ameliorated the yields of numerous steps and the full synthesis of the other dimers will certainly be performed more easily thanks to the work disclosed herein. |
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