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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

Síntese de derivados adamantóides diaminados e amino álcoois, potenciais agentes farmacológicos

Barbosa, Gisele 11 July 2014 (has links)
Submitted by Renata Lopes (renatasil82@gmail.com) on 2016-01-29T12:13:52Z No. of bitstreams: 1 giselebarbosa.pdf: 13872105 bytes, checksum: 80b53c78204148b2895105c24b335d8c (MD5) / Rejected by Adriana Oliveira (adriana.oliveira@ufjf.edu.br), reason: Adicionar instituição on 2016-02-01T15:45:14Z (GMT) / Submitted by Renata Lopes (renatasil82@gmail.com) on 2016-02-01T16:10:54Z No. of bitstreams: 1 giselebarbosa.pdf: 13872105 bytes, checksum: 80b53c78204148b2895105c24b335d8c (MD5) / Approved for entry into archive by Adriana Oliveira (adriana.oliveira@ufjf.edu.br) on 2016-02-01T20:10:28Z (GMT) No. of bitstreams: 1 giselebarbosa.pdf: 13872105 bytes, checksum: 80b53c78204148b2895105c24b335d8c (MD5) / Made available in DSpace on 2016-02-01T20:10:28Z (GMT). No. of bitstreams: 1 giselebarbosa.pdf: 13872105 bytes, checksum: 80b53c78204148b2895105c24b335d8c (MD5) Previous issue date: 2014-07-11 / CAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior / Compostos adamantóides têm sido alvo de interesse desde a virada do século 20, devido a sua analogia com a estrutura do diamante. A estrutura única do adamantano é refletida em suas propriedades físicas e químicas altamente diferenciadas, que podem ter muitas aplicações, incluindo a concepção de medicamentos e carreação de fármacos. Estes estão presentes numa grande variedade de compostos bioativos, mostrando atividade contra alguns agentes infecciosos e em muitos distúrbios fisiológicos. Juntamente com as aminas e, principalmente, as poliaminas que são substâncias que ocorrem amplamente em materiais biológicos podendo estar envolvidas em muitos aspectos como crescimento, divisão e diferenciação celular, os compostos adamantóides são considerados um alvo potencial para a quimioterapia de várias doenças, principalmente as infecciosas. Nesse contexto, esse trabalho tem como proposta a preparação de novos derivados adamantóides diaminados e amino álcoois, que sejam potenciais agentes farmacológicos. Para obtenção dos compostos almejados, o 1- adamantano metanol teve o grupo hidroxila transformado em um melhor grupo abandonador e em seguida substituído por diferentes aminas e amino álcoois. E, para a síntese dos derivados da 2-adamantanona foi realizada a aminação redutiva da mesma com as diaminas e amino álcoois utilizados. Obteve-se 19 compostos, sendo 12 inéditos, os quais foram caracterizados por espectroscopia na região do Infravermelho e Ressonância magnética nuclear de 1H e 13C. Foram realizados diferentes ensaios biológicos e o composto 7 apresentou maior destaque nos testes realizados. / Adamantoids compounds have been the subject of interest since the turn of the 20th century due to its analogy with the diamond structure. The unique structure of adamantane is reflected in their highly differing physical and chemical properties, which can have many applications, including drug design and drug delivery, and is present in a variety of bioactive compounds showing activity against several infectious agents, and in many physiological disorders. Along with amines and especially polyamines which are substances that widely occur in biological material may be involved in many aspects such as growth, cell division and differentiation been considered a potential target for chemotherapy for several, especially infectious diseases. In this context, this paper aims at the preparation of new diamines and amino alcohols adamantoids derivatives, which are potential pharmacological agents. To obtain the desired compounds, 1-adamantane methanol has the hydroxyl group converted into a better leaving group, and then replaced by different amines and amino alcohols. For the synthesis of the 2- adamantanone derivatives it was employed reductive amination with diamines and amino alcohols followed by the reduction with NaBH3CN. It was prepared in this work 19 compounds, including 12 previously unpublished, which were characterized by infrared spectroscopy and 1H and 13C nuclear magnetic resonance. Preliminary biological evaluations were performed and compound 7 showed the best activity on the realized biological assays.

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