Antifungal activity of Imidazolidin-4-ones of the antimalarial primaquine

The 5-Isopropyl-3-[4-(6-methoxy-quinolin-8-ylamino)-pentyl]-2,2-dimethyl-imidazolidin-4-one (ValPQacet) was sinthesized through acylation of the anti-malarial primaquine with α-valine and subsequent reaction of the resulting -aminoamide with propanone (Sheme 1).Imidazolidin-4-ones of the anti malarial primaquine are being sinthesized to develop new variants in order to improve more effective treatments against malaria . Recently it has been observed that primaquine derivates could have effect in a new kind of yeast . To study the fungicidal activity against Candida albicans, Candida tropicalis, Issatchenkia orientalis, Sacharomyces cerevisae, the ValPQacet was put in the form of the hydrochloride salt. The minimal inhibitory concentration (MIC) could be determined for all yeast in the concentration range assayed. Also was determined MIC’s of primaquine hydrochloride salt for all yeast, and this shows that the parent drug is less active than our compound. Further studies are being performed to determine viability and cellular injury with this drugs.

Steroselective synthesis of imidazolidin-4-ones from α-amino amides of the antimalarial primaquine and substituted benzaldehydes

Imidazolidin-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.

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.

Cabo e radio frequência em sistemas deteção de incêndio

Novos produtos são sempre aliados a novas tecnologias, mas nem sempre aplicadas no imediato. No que se refere à radio frequência (RF), são inúmeros os obstáculos aplicados à deteção de incêndio sejam eles, o custo, o interface ou somente a falta de informação por parte da engenharia de projeto. Durante os últimos anos a comunicação sem fios esteve também aliada a equipamentos para aplicação dita “doméstica”, com pouca fiabilidade, baixa autonomia, difícil comunicação entre equipamentos e essencialmente não regulada, isto é, sem normalização. Por parte do comité europeu de normalização, no que se refere à introdução desta tecnologia pela norma que regula os equipamentos de deteção de incêndio, EN54, estão reunidas as condições para que os equipamentos certificados pelos diferentes e reconhecidos laboratórios, entre outros, a LPCB, BSI ou VdS possam ser utilizados conferindo assim à engenharia de segurança e ao utilizador a confiança necessária para a sua instalação. Sistemas de deteção de incêndio por cabo usam tecnologias e protocolos de tal forma evoluídos que são “integráveis” com os sistemas que completam a gestão técnica e de emergência de uma infraestrutura,

Radio link quality estimation in wireless sensor networks: a survey

Radio link quality estimation in Wireless Sensor Networks (WSNs) has a fundamental impact on the network performance and also affects the design of higher-layer protocols. Therefore, for about a decade, it has been attracting a vast array of research works. Reported works on link quality estimation are typically based on different assumptions, consider different scenarios, and provide radically different (and sometimes contradictory) results. This article provides a comprehensive survey on related literature, covering the characteristics of low-power links, the fundamental concepts of link quality estimation in WSNs, a taxonomy of existing link quality estimators, and their performance analysis. To the best of our knowledge, this is the first survey tackling in detail link quality estimation in WSNs. We believe our efforts will serve as a reference to orient researchers and system designers in this area.

System Level Simulation and Radio Resource Management for Distributed Antenna Systems with Cognitive Radio and Multi-Cell Cooperation

4th International Conference on Future Generation Communication Technologies (FGCT 2015), Luton, United Kingdom.

Teaching mathematics using Massive Open Online Courses

Distance learning - where students take courses (attend classes, get activities and other sort of learning materials) while being physically separated from their instructors, for larger part of the course duration - is far from being a “new event”. Since the middle of the nineteenth century, this has been done through Radio, Mail and TV, taking advantage of the full educational potential that these media resources had to offer at the time. However, in recent times we have, at our complete disposal, the “magic wonder” of communication and globalization - the Internet. Taking advantage of a whole new set of educational opportunities, with a more or less unselfish “look” to economic interests, focusing its concern on a larger and collective “welfare”, contributing to the development of a more “equitable” world, with regard to educational opportunities, the Massive Open Online Courses (MOOCs) were born and have become an important feature of the higher education in recent years. Many people have been talking about MOOCs as a potential educational revolution, which has arrived from North America, still growing and spreading, referring to its benefits and/or disadvantages. The Polytechnic Institute of Porto, also known as IPP, is a Higher Education Portuguese institution providing undergraduate and graduate studies, which has a solid history of online education and innovation through the use of technology, and it has been particularly interested and focused on MOOC developments, based on an open educational policy in order to try to implement some differentiated learning strategies to its actual students and as a way to attract future ones. Therefore, in July 2014, IPP launched the first Math MOOC on its own platform. This paper describes the requirements, the resulting design and implementation of a mathematics MOOC, which was essentially addressed to three target populations: - pre-college students or individuals wishing to update their Math skills or that need to prepare for the National Exam of Mathematics; - Higher Education students who have not attended in High School, this subject, and who feel the need to acquire basic knowledge about some of the topics covered; - High School Teachers who may use these resources with their students allowing them to develop teaching methodologies like "Flipped Classroom” (available at http://www.opened.ipp.pt/). The MOOC was developed in partnership with several professors from several schools from IPP, gathering different math competences and backgrounds to create and put to work different activities such video lectures and quizzes. We will also try to briefly discuss the advertising strategy being developed to promote this MOOC, since it is not offered through a main MOOC portal, such as Coursera or Udacity.