Hybrids of Imatinib with Quinoline: Synthesis, Antimyeloproliferative Activity Evaluation, and Molecular Docking.

Imatinib (IMT) is the first-in-class BCR-ABL commercial tyrosine kinase inhibitor (TKI). However, the resistance and toxicity associated with the use of IMT highlight the importance of the search for new TKIs. In this context, heterocyclic systems, such as quinoline, which is present as a pharmacophore in the structure of the TKI inhibitor bosutinib (BST), have been widely applied. Thus, this work aimed to obtain new hybrids of imatinib containing quinoline moieties and evaluate them against K562 cells. The compounds were synthesized with a high purity degree. Among the produced molecules, the inhibitor 4-methyl-N3-(4-(pyridin-3-yl)pyrimidin-2-yl)-N1-(quinolin-4-yl)benzene-1,3-diamine (2g) showed a suitable reduction in cell viability, with a CC50 value of 0.9 µM (IMT, CC50 = 0.08 µM). Molecular docking results suggest that the interaction between the most active inhibitor 2g and the BCR-ABL1 enzyme occurs at the bosutinib binding site through a competitive inhibition mechanism. Despite being less potent and selective than IMT, 2g is a suitable prototype for use in the search for new drugs against chronic myeloid leukemia (CML), especially in patients with acquired resistance to IMT.

Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors.

Acquired immunodeficiency syndrome (AIDS) is caused by human immunodeficiency virus (HIV) and remains a global health problem four decades after the report of its first case. Despite success in viral load suppression and the increase in patient survival due to combined antiretroviral therapy (cART), the development of new drugs has become imperative due to strains that have become resistant to antiretrovirals. In this context, there has been a continuous search for new anti-HIV agents based on several chemical scaffolds, including nitrogenated heterocyclic pyrrole rings, which have been included in several compounds with antiretroviral activity. Thus, this review aims to describe pyrrole-based compounds with anti-HIV activity as a new potential treatment against AIDS, covering the period between 2015 and 2020. Our research allowed us to conclude that pyrrole derivatives are still worth exploring, as they may provide highly active compounds targeting different steps of the HIV-1 replication cycle and act with an innovative mechanism.

Phenylamino-pyrimidine (PAP) Privileged Structure: Synthesis and Medicinal Applications.

The phenylamino-pyrimidine (PAP) nucleus has been demonstrated to be useful for the development of new drugs and is present in a wide variety of antiretroviral agents and tyrosine kinase inhibitors (TKIs). This review aims to evaluate the application of PAP derivatives in drugs and other bioactive compounds. It was concluded that PAP derivatives are still worth exploring, as they may provide highly competitive ATP TKI's with nano/picomolar activity.

Conhecimentos e crenças de universitários do curso de engenharia sobre as infecções sexualmente transmissíveis / Knowledge and beliefs of university students of the engineering course on sexually transmitted infections / Conocimientos y creencias de los estudiantes universitarios del curso de ingeniería sobre infecciones de transmisión sexual

Objetivo: analisar o conhecimento e crenças sobre as infecções sexualmente transmissíveis entre universitários do curso de engenharia. Método: pesquisa descritiva, transversal, quantitativa, realizada em universidade privada no Rio de Janeiro. Selecionou-se uma amostra de 170 estudantes do curso de engenharia. Os achados foram organizados e analisados com emprego da estatística descritiva. Resultados: houve predomínio do sexo masculino (86,47%); idades de 18-23 anos (78,83%); solteiros (60%); sem filhos (97,06%); moram com os pais (76,47%). Não utilizam preservativo de forma contínua (62,25%), mas acreditam ser pouco possível adquirir infecções (42,35%). Apresentam conhecimento insuficiente sobre as infecções (77,65%); reconhecendo as mais divulgadas pela mídia. Conclusão: a maioria dos estudantes reconhece a importância do preservativo, mas não usa regularmente. Os jovens apresentam conhecimentos insuficientes e crenças que colocam em risco a sua saúde sexual

Objective: to analyze the knowledge and beliefs about sexually transmitted infections among university students in the engineering course. Method: descriptive, transversal, quantitative research carried out at a private university in Rio de Janeiro. A sample of 170 students from the engineering course was selected. The findings were organized and analyzed using descriptive statistics. Results: there was a predominance of males (86,47%); ages 18 to 23 years (78,83%); singles (60%); without children (97,06%); live with their parents (76,47%). They not use condoms continuously (62,25%); but they believe it is not possible to acquire infections (42,35%). They have insufficient knowledge about infections (77,65%), recognizing the most widely disseminated by the media. Conclusion: most students recognize the importance of condoms, but do not use them regularly. Young people have insufficient knowledge and beliefs that put their sexual health at risk

Objetivo: analizar el conocimiento y las creencias sobre las infecciones de transmisión sexual entre estudiantes universitarios en el curso de ingeniería. Método: investigación descriptiva, transversal y cuantitativa realizada en una universidad privada de Río de Janeiro. Se seleccionó una muestra de 170 estudiantes del curso de ingeniería. Los hallazgos se organizaron y analizaron mediante estadística descriptiva. Resultados: predominó el sexo masculino (86.47%); edades 18 a 23 años (78.83%); solteros (60%); sin hijos (97,06%); viven con sus padres (76.47%). No usan condones continuamente (62.25%), pero creen que no es posible adquirir infecciones (42.35%). Tienen un conocimiento insuficiente sobre las infecciones (77,65%); reconociendo lo más publicitado por los medios de comunicación. Conclusión: la mayoría de los estudiantes reconoce la importancia de los condones, pero no los usa regularmente. Los jóvenes tienen conocimientos y creencias insuficientes que ponen en riesgo su salud sexual

Acompanhamento terapêutico: caminhos clínicos, políticos e sociais para a consolidação da reforma psiquiátrica brasileira / Therapeutic accompaniment: clinical, political and social paths for the brazilian psychiatric reform

O Acompanhamento Terapêutico (AT) é um dispositivo que tem caráter transetorial em seu fazer porque pode atravessar ou compor com os espaços interdisciplinares e intersetoriais, como o Centro de Atenção Psicossocial, uma infinidade de projetos construídos coletivamente para ampliar os sentidos da vida de um sujeito. A partir dessa premissa, esta pesquisa define como objeto de estudo o AT como dispositivo de intervenção na vida de uma usuária de um serviço público de saúde mental e as interferências operadas por este dispositivo na sua vida em relação com o corpo social. Trata-se de uma pesquisa qualitativa que utiliza o Estudo de Caso como procedimento metodológico para apreensão e compreensão dos dados empíricos. Para isso, o estudo se propõe a enfrentar as questões: o AT produz transformação real na vida dos sujeitos? Que tipo de transformações opera no interno do campo transferencial, no serviço e na rede de cuidados? Sustenta-se por si só ou depende da rede ampliada pelos serviços territoriais? A origem do AT se dá em instituições privadas e só timidamente é transposta para os serviços da rede pública de atenção à saúde. Essa transposição não se dá de forma instituída e sua oficialização como dispositivo em saúde mental sofre percalços, como constatado com o desaparecimento do termo acompanhamento terapêutico e do financiamento do procedimento na legislação vigente e que constava na Portaria SNAS n.° 189 de 19 de novembro de 1991. Essa anulação do ATdas políticas públicas é defendida, nesta pesquisa, como uma contradição em relação às diretrizes do Sistema Único de Saúde (SUS) e da própria Reforma Psiquiátrica, que orientam ações territoriais, intersetoriais, articulação de rede de serviços e articulação de recursos do território para a atenção em saúde mental. O resultado é a inacessibilidade do dispositivo AT aos que dele se beneficiariam, como foi comprovado ) no caso em análise. O cenário do estudo destaca-se por acionar este dispositivo e construir em conjunto com as acompanhantes terapêuticas envolvidas uma trajetória de enriquecimento e acesso a novas territorialidades para a K. Entretanto, o estudo questiona porquê os trabalhadores dos serviços de saúde mental não assumem para si a função potencializadora do AT e sua conseqüente legitimação na esfera pública e coletiva, o palco de ações e conexões de redes, propiciadoras de produção de vida. Este estudo sustenta que o AT é, no campo da saúde mental, um dispositivo que vem se sofisticando no decorrer de seu processo histórico com o questionamento de sua função estritamente clínica e se propõe a enfrentar os desafios para a retomada do diálogo e conexão do seu fazer com as políticas públicas.

Therapeutic Accompaniment (TA) is a device of a cross sector nature because it can interact with interdisciplinary and intersected areas, like the Social and Psychic Help Center (Centro de Atenção Psicossocial), \'crossing or being a component of an infinity of collectively built projects that can broaden the meaning of life of a subject. Starting from that premise, this research defines TA as the study object that acts as a device of intervention in the life of a woman who uses mental health public services and the interferences resulted from this device in her life related to her social interactions. It is a qualitative research that uses the Case Study as a methodological procedure for collection and comprehension of empirical data. Therefore, this study proposes to face the following questions: Does TA produces real changes in the lives of its subjects? What types of changes are produced in the internal transferential field, services offered and the care network? Is it self-sustainable or does it depend on an amplified network by territorial services? TA origins takes place in private institutions and only very timidly is used by public health services. The use in public services doesn\'t take place in an established form and its officialization in health care is not easy. It was found that the term therapeutic accompaniment and its financing procedures disappeared from the current legislation. It used to be part of the SNAS Bill number 189 ofNovember 19th of 1991 (Portaria SNAS n°189 de 19 de novembro de 1991). This TA annulment of public policies is viewed on this research as not only a contradiction of the Brazilian Heath Care Program (Sistema Único de Saúde SUS) but also of the Psychiatric Reform, that suggests territorial actions, cross sectoring, articulation of networking services and articulation of territorial resources for mental health management. The result is the inaccessibility of the TA device to the ones that could benefit from it as it was proved on the case study analyzed. The study scenario differentiates itself because it triggers this device and builds, with the therapeutic companion, an enriching path and offers accessibility to new territories to the K. However, this paper questions why workers of public mental health system do not take the transforming responsibility of TA and its consequent legitimization in public and collective sphere, the stage of actions and connections of network, which are auspicious for a more broaden meaning of life. This paper sustains that TA is, in the field of public mental health, a device that is becoming more sophisticated through its historical process with the questioning of its strictly clinical mission and its willingness to face the challenges to restart dialogue and to establish a connection with public policies.