Anti-pneumoscystis carinni activitiy of primaquine imidazolidin-4-ones

Pneumocystis 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.

Development and biological evaluation of API-ILs based on anti-bacterial and anti-fungal drugs

In recent years Ionic Liquids (ILs) are being applied in life sciences. ILs are being produce with active pharmaceutical drugs (API) as they can reduce polymorphism and drug solubility problems [1] Also ILs are being applied as a drug delivery device in innovative therapies What is appealing in ILs is the ILs building up platform, the counter-ion can be carefully chosen in order to avoid undesirable side effects or to give innovative therapies in which two active ions are paired. This work shows ILs based on ampicillin (an anti-bacterial agent) and ILs based on Amphotericin B. Also we show studies that indicate that ILs based on Ampicillin could reverse resistance in some bacteria. The ILs produced in this work were synthetized by the neutralization method described in Ferraz et. al. [2] Ampicillin anion was combined with the following organic cations 1-ethyl-3-methylimidazolium, [EMIM]; 1-hydroxy-ethyl-3-methylimidazolium, [C2OHMIM]; choline, [cholin]; tetraethylammonium, [TEA]; cetylpyridinium, [C16pyr] and trihexyltetradecylphosphonium, [P6,6,6,14]. Amphotericin B was combined with [C16pyr], [cholin] and 1-metohyethyl-3-methylimidazolium, [C3OMIM]. The ILs-APIs based on ampicillin[2] were tested against sensitive Gram-negative bacteria Escherichia coli ATCC 25922 and Klebsiella pneumonia (clinical isolated), as well as on Gram positive Staphylococcus Aureus ATCC 25923, Staphylococcus epidermidis and Enterococcus faecalis. The arising resistance developed by bacteria to antibiotics is a serious public health threat and needs new and urgent measures. We study the bacterial activity of these compounds against a panel of resistant bacteria (clinical isolated strains): E. coli CTX M9, E. coli TEM CTX M9, E. coli TEM1, E. coli CTX M2, E. coli AmpC Mox2. In this work we demonstrate that is possible to produce ILs from anti-bacterial and anti-fungal compounds. We show here that the new ILs can reverse the bacteria resistance. With the careful choice of the organic cation, it is possible to create important biological and physic-chemical properties. This work also shows that the ion-pair is fundamental in ampicillin mechanism of action.

O impacto do ruído na qualidade de vida dos enfermeiros de cuidados intensivos

Mestrado em Segurança e Higiene do Trabalho.

A influência da reeducação vestibular nas medidas objetivas e subjetivas em pacientes com défice vestibular periférico unilateral

Mestrado em Fisioterapia.

Adequação da acústica e controlo do ruído em unidades de ressonância magnética: projeto de investigação

Mestrado em Segurança e Higiene do Trabalho.

Caracterização da exposição e eventuais efeitos para a saúde da exposição profissional ao estireno nos ortoprotésicos

Mestrado em Segurança e Higiene do Trabalho.

Influência das condições de trabalho na exposição aos fumos de soldadura e efeitos na saúde

Mestrado em Segurança e Higiene do Trabalho.

Avaliação da margem do PTV em tumores ginecológicos com irradiação dos gânglios lomboaórticos, que realizaram IMRT

Mestrado em Radioterapia.

Écrire à l' université: jeux et enjeux didactiques

Nous présentons, dans cette communication, les resultats d'une étude menée dans le cours d'expression orale et écrite dispensé en premier année à l'Escola Superior de Educação de Lisbonne.

Nintendo Wii: uso terapêutico no controlo postural em indivíduos que sofreram um acidente vascular cerebral

Mestrado em Fisioterapia.

História da fisioterapia em Portugal: da origem a 1966

Mestrado em Fisioterapia.

Contributo para a utilização segura de câmaras de segurança biológica na manipulação de medicamentos citotóxicos

Mestrado em Segurança e Higiene do Trabalho.

Análise da influência da aplicação de kinesio tape na ativação muscular durante um passe de futsal

Mestrado em Fisioterapia.

Efeitos de um programa baseado em tarefas orientadas na competência de marcha em indivíduos com acidente vascular cerebral

Mestrado em Fisioterapia.