Browsing by Author "Moreira, Rui"
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- Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-onesPublication . Vale, Nuno; Collins, Margaret S.; Gut, Jiri; Ferraz, Ricardo; Rosenthal, Philip J.; Cushion, Melanie T.; Moreira, Rui; Gomes, PaulaA series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 lg/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the lM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead com pound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.
- Anti-pneumoscystis carinni activitiy of primaquine imidazolidin-4-onesPublication . Vale, Nuno; Ferraz, Ricardo; Azevedo, Joana; Araújo, Maria João; Moreira, Rui; Collins, Margaret S.; Cushion, Melanie T.; Gomes, PaulaPneumocystis pneumonia (PCP) is one of the most frequent causes of mortality among HIV-infected patients. Primaquine (PQ) is an antimalarial 8-aminoquinoline effective against PCP when given in combination with clindamycin. This has drawn the attention of Medicinal Chemists towards the anti-PCP activity of 8-aminoquinolines, not only confined to those exhibiting antimalarial activity [1]. It is thought that anti-PCP 8-aminoquinolines exert their anti-PCP activity by acting on the electronic transport and redox system of the P. carinii pathogen [1]. Recently, our research group has been developing imidazolidin-4-one derivatives of PQ (Scheme 1), targeting novel compounds with improved therapeutic action, namely, higher resistance to metabolic inactivation, lower toxicity and equal or higher antimalarial activity than that of the parent drug [2,3]. These imidazolidin-4-ones were seen to block the transmission of rodent malaria, caused by Plasmodium berghei on BalbC mice, to the mosquito vector Anopheles stephensi [3]. The anti-PCP activity of our PQ derivatives is now under study and preliminary in vitro assays [4] show that some of the compounds exhibit slight to moderate activity after a 72 h incubation period against P. carinii. In one case, the IC50 was comparable to that of parent PQ. Both these studies and forthcoming results from ongoing biological assays will be presented and discussed.
- Plano de Igualdade da ESE.IPPPublication . Serrão, Carla; Martins, Teresa; Cardoso, Márcia; Moreira, Rui; Botelho, SaraCom vista à concretização da igualdade de oportunidades entre mulheres e homens, são definidos Planos para a Igualdade nas organizações, considerando-se que estes se revelam como importantes instrumentos no sentido da execução de mudanças efetivas que conduzam a essa meta. OsPlanos de Igualdade nas organizações surgem, neste sentido, como contributo significativo para potenciar uma estratégia de mainstreaming de género, ou seja, de “transversalização da Igualdade de Género a todos os domínios de política e de funcionamento das instituições” (Ferreira, 2011, p.2). Devem constituir-se, por isso, como instrumentos capazes “de introduzir a coerência e a sistematicidade necessárias à reforma de qualquer coletivo organizado” (p. 3).
- Representações de colaboradores e colaboradoras da ESE.IPP sobre o processo de conciliação da vida profissional, familiar e pessoal e o papel da Organização neste âmbitoPublication . Serrão, Carla; Martins, Teresa; Cardoso, Márcia; Botelho, Sara; Moreira, RuiO presente estudo incide sobre as representações que os colaboradores e as colaboradoras da Escola Superior de Educação (ESE) do Instituo Politécnico do Porto (IPP) têm sobre o processo de conciliação entre vida profissional e familiar e vida pessoal, tendo como objetivo compreender: 1)os significados e opiniões dos/as participantes sobre a temática da conciliação entre vida profissional, familiar e pessoal; 2)as estratégias que desencadeiam e as dificuldades que sentem os/as participantes ao nível da conciliação entre vida profissional, familiar e pessoal; 3)o papel da ESE.IPP na facilitação de processos de conciliação entre vida profissional, familiar e pessoal dos seus colaboradores e das suas colaboradoras; 4)as opiniões dos/as participantes sobre a preocupação da ESSE.IPP no que diz respeito ao apoio nos processos de conciliação entre vida profissional, familiar e pessoal do seu pessoal docente e não docente. Trata-se de um estudo de caráter qualitativo, descritivo e exploratório, com base no qual se pretende criar um referencial de boas práticas organizacionais com vista à promoção da conciliação da atividade profissional com a vida familiar e pessoal.
- Sexismo ambivalente, atitudes perante os papéis de género e estratégias de antecipação da conciliação entre vida familiar e vida profissionalPublication . Serrão, Carla; Martins, Teresa; Cardoso, Márcia; Botelho, Sara; Moreira, Rui; Cadima, JoanaCom o intuito de avaliar as atitudes face à igualdade entre homens e mulheres, a ideologia de género e as estratégias de antecipação da conciliação entre vida familiar e vida profissional, foi aplicada uma bateria de testes a 408 sujeitos de ensino superior
- Steroselective synthesis of imidazolidin-4-ones from α-amino amides of the antimalarial primaquine and substituted benzaldehydesPublication . Ferraz, Ricardo; Gomes, José R. B.; Passo, Joana; Oliveira, Eliandre; Moreira, Rui; Gomes, PaulaImidazolidin-4-ones are commonly employed as skeletal modifications in bioactive oligopeptides, either as proline surrogates or for protection of the N-terminal amino acid against aminopeptidase-catalysed hydrolysis . We have been working on the synthesis of imidazolidin-4-ones of the antimalarial primaquine , through acylation of primaquine with an α-amino acid and subsequent reaction of the resulting α-aminoamide with a ketone or aldehyde. Thus, when using racemic primaquine, an optically pure chiral α-amino acid and an aldehyde as starting materials, four imidazolidin-4-one diastereomers are to be expected (Scheme 1). However, we have recently observed that imidazolidin-4-one synthesis was stereoselective when 2-carboxybenzaldehyde (2CBA)* was used, as only two diastereomers were produced2. Computational studies have shown that the imine formed prior to ring closure had, for structures derived from 2CBA, a quasi-cyclic rigid structure2. This rigid conformation is stabilized by an intramolecular hydrogen bond involving the C=O oxygen atom of the 2-carboxyl substituent in 2CBA and the N-H group of the α-amino amide moiety2. These findings led us to postulate that the 2-carbonyl substituent in the benzaldehyde moiety was the key for the stereoselective synthesis of the imidazolidin-4-ones2.
- Unanticipated stereoselectivity in the reaction of primaquine α-aminoamides with substituted benzaldehydes: A computational and experimental study†Publication . Ferraz, Ricardo; Gomes, José R. B.; Oliveira, Eliandre de; Moreira, Rui; Gomes, PaulaImidazolidin-4-ones are commonly employed as skeletal modifications in bioactive oligopeptides, either as proline surrogates or for protection of the N-terminal amino acid against aminopeptidase- and endopeptidase-catalyzed hydrolysis. Imidazolidin-4-one synthesis usually involves the reaction of an α-aminoamide moiety with a ketone or an aldehyde to yield an imine, followed by intramolecular cyclization. We have unexpectedly found that imidazolidin-4-one formation is stereoselective when benzaldehydes containing o-carboxyl or o-methoxycarbonyl substituents are reacted with α-aminoamide derivatives of the antimalarial drug primaquine. A systematic computational and experimental study on the stereoselectivity of imidazolidin-4-one formation from primaquine α-aminoamides and various substituted benzaldehydes has been carried out, and they have allowed us to conclude that intramolecular hydrogen-bonds involving the CO oxygen of the o-substituent play a crucial role.