Design of hybrid molecules as antimycobacterial compounds: Synthesis of isoniazid-naphthoquinone derivatives and their activity against susceptible and resistant strains of Mycobacterium tuberculosis.

Isoniazid-naphthoquinone hybrids were synthesized and evaluated against a susceptible (H37Rv) strain and two isoniazid-resistant strains (INHR1 and INHR2) of Mycobacterium tuberculosis. The antimycobacterial activity of the derivatives was determined based on the resazurin microtiter assay and their cytotoxicity in adhered mouse monocyte macrophage J774.A1 cells (ATCC TIB-67). Of the twenty-two compounds evaluated against the three strains of M. tuberculosis, twenty-one presented some activity against the H37Rv and INHR1 (katG S315T) or INHR2 (inhA C(-5)T) strains. Compounds 1a, 2a, and 8a were effective against the INHR1 strain, and compounds 1a, 1b, 2a, 3a, 5a, 5b and 8a were effective against the INHR2 strain, with MICs in the range of 3.12-6.25 µg/mL. Compounds 1b and 5b were the most active against H37Rv, with MIC of 0.78 µg/mL. Based on the selectivity index, 1b and 5b can be considered safe as a drug candidate compounds. These results demonstrate that quinoidal compounds can be used as promising scaffolds for the development of new anti-TB drugs and hybrids with activity against M. tuberculosis-susceptible and INH-resistant strains.

Catalytic asymmetric reactions and synthesis of quinones.

Asymmetric reactions and the synthesis of various quinones, carried out in the presence of chiral organocatalysts and metal-ligand complexes, are reviewed here. The role of quinones as Michael donors/acceptors, Diels-Alder dienophiles and 1,3-dipolarophiles has been extensively investigated to access complex structural frameworks. Additionally, reports in the literature on the stereoselective synthesis of simple and complex quinoidal compounds with potential biological activities have also been summarized in this review.

Dor nas unidades de internação de um hospital universitário / Pain management at inpatient wards of a university hospital / Dolor en las unidades de ingreso de un hospital universitario

JUSTIFICATIVA E OBJETIVOS: Estudo exploratório-descritivo, transversal, com objetivo de determinar a prevalência, caracterização, localização, mensuração e discussão de medidas farmacológicas analgésicas em dor aguda em cinco unidades de internação de um hospital universitário. MÉTODO: Participaram 856 sujeitos, dos quais 272 com dor no momento. As informações relacionadas à dor foram obtidas através de entrevista estruturada junto ao leito. Usou-se a escala numérica de dor e diagrama corporal. RESULTADOS: A analgesia foi verificada no prontuário. A prevalência geral de dor foi de 31,8%, sendo intensa em 44,2% e a média de 6,6 na escala numérica de dor. O motivo principal foi traumatismo, o local mais frequente, o abdômen. O analgésico mais usado foi a dipirona em 76,1%, com/sem associação. Opioide forte foi prescrito em 4,4%. Para 27,5% não houve melhoria. CONCLUSÃO: Conclui-se que a dor é de alta prevalência, pouco avaliada, subtratada, com uso incorreto de analgésicos.

BACKGROUND AND OBJECTIVES: This is an exploratory, descriptive and transversal study aiming to determine the prevalence, characterization, location, and measurement and discuss pharmacological analgesic measures for acute pain management in five inpatient wards of a university hospital. METHOD: We enrolled 856 subjects in the study, of whom 272 were in pain at the time. Information related to pain was obtained using a bedside structured interview. Numeric pain scale and body diagram were used. RESULTS: Analgesia was assessed through medical records. The overall prevalence of pain was 31.8%, with severe pain in 44.2% and mean of 6.6 on numeric pain scale. The main reason was trauma and the most common site the abdomen. The most widely used analgesic was dipyrone (76.1%) with/without combination. Strong opioid was prescribed to 4.4%. For 27.5% there was no improvement. CONCLUSION: We conclude that pain is highly prevalent, poorly evaluated, undertreated, with inappropriate use of analgesics.

JUSTIFICATIVA Y OBJETIVOS: Estudio exploratorio, descriptivo y transversal, con el objetivo de determinar la prevalencia, la caracterización, la ubicación, la mensuración y la discusión de las medidas farmacológicas analgésicas en dolor agudo, en cinco unidades de ingreso de un hospital universitario. MÉTODO: Participaron 856 sujetos, de los cuales 272 tenían dolor en ese momento. Las informaciones relacionadas con el dolor se obtuvieron por medio de una entrevista estructurada con el paciente y junto a la cama de hospital. Se usó la escala numérica de dolor y el diagrama corporal. RESULTADOS: La analgesia fue verificada en la historia clínica del paciente. La prevalencia general de dolor fue de un 31,8% siendo intensa en un 44,2% y con un promedio de 6,6 en la escala numérica de dolor. El motivo principal fue el traumatismo y la región más frecuente fue el abdomen. El analgésico más usado fue la dipirona en un 76,1%, con/sin asociación. Se prescribió opioide fuerte en un 4,4%. Para el 27,5% no se registró mejoría. CONCLUSIONES: Llegamos a la conclusión de que el dolor es de alta prevalencia, poco evaluado, mal tratado, y con el uso incorrecto de analgésicos.

Pain management at inpatient wards of a university hospital.

BACKGROUND AND OBJECTIVES: This is an exploratory, descriptive and transversal study aiming to determine the prevalence, characterization, location, and measurement and discuss pharmacological analgesic measures for acute pain management in five inpatient wards of a university hospital. METHOD: We enrolled 856 subjects in the study, of whom 272 were in pain at the time. Information related to pain was obtained using a bedside structured interview. Numeric pain scale and body diagram were used. RESULTS: Analgesia was assessed through medical records. The overall prevalence of pain was 31.8%, with severe pain in 44.2% and mean of 6.6 on numeric pain scale. The main reason was trauma and the most common site the abdomen. The most widely used analgesic was dipyrone (76.1%) with/without combination. Strong opioid was prescribed to 4.4%. For 27.5% there was no improvement. CONCLUSION: We conclude that pain is highly prevalent, poorly evaluated, undertreated, with inappropriate use of analgesics.