Quinolines: microwave-assisted synthesis and their antifungal, anticancer and radical scavenger properties

An efficient method for the synthesis of quinolines using microwave irradiation was developed providing 28 quinolines with good yields. The reaction procedures are environmentally friendly, convenient, mild and of easy work-up. Quinolines were evaluated for their antifungal, anticancer and antioxidant properties and exhibited high activities in all tests performed.Centro de Investigación y Desarrollo en Ciencias Aplicada

Prevalence of non-communicable diseases in Brazilian children: follow-up at school age of two Brazilian birth cohorts of the 1990's

<p>Abstract</p> <p>Background</p> <p>Few cohort studies have been conducted in low and middle-income countries to investigate non-communicable diseases among school-aged children. This article aims to describe the methodology of two birth cohorts, started in 1994 in Ribeirão Preto (RP), a more developed city, and in 1997/98 in São Luís (SL), a less developed town.</p> <p>Methods</p> <p>Prevalences of some non-communicable diseases during the first follow-up of these cohorts were estimated and compared. Data on singleton live births were obtained at birth (2858 in RP and 2443 in SL). The follow-up at school age was conducted in RP in 2004/05, when the children were 9-11 years old and in SL in 2005/06, when the children were 7-9 years old. Follow-up rates were 68.7% in RP (790 included) and 72.7% in SL (673 participants). The groups of low (<2500 g) and high (≥ 4250 g) birthweight were oversampled and estimates were corrected by weighting.</p> <p>Results</p> <p>In the more developed city there was a higher percentage of non-nutritive sucking habits (69.1% vs 47.9%), lifetime bottle use (89.6% vs 68.3%), higher prevalence of primary headache in the last 15 days (27.9% vs 13.0%), higher positive skin tests for allergens (44.3% vs 25.3%) and higher prevalence of overweight (18.2% vs 3.6%), obesity (9.5% vs 1.8%) and hypertension (10.9% vs 4.6%). In the less developed city there was a larger percentage of children with below average cognitive function (28.9% vs 12.2%), mental health problems (47.4% vs 38.4%), depression (21.6% vs 6.0%) and underweight (5.8% vs 3.6%). There was no difference in the prevalence of bruxism, recurrent abdominal pain, asthma and bronchial hyperresponsiveness between cities.</p> <p>Conclusions</p> <p>Some non-communicable diseases were highly prevalent, especially in the more developed city. Some high rates suggest that the burden of non-communicable diseases will be high in the future, especially mental health problems.</p

The complete genome sequence of Chromobacterium violaceum reveals remarkable and exploitable bacterial adaptability

Chromobacterium violaceum is one of millions of species of free-living microorganisms that populate the soil and water in the extant areas of tropical biodiversity around the world. Its complete genome sequence reveals (i) extensive alternative pathways for energy generation, (ii) ≈500 ORFs for transport-related proteins, (iii) complex and extensive systems for stress adaptation and motility, and (iv) wide-spread utilization of quorum sensing for control of inducible systems, all of which underpin the versatility and adaptability of the organism. The genome also contains extensive but incomplete arrays of ORFs coding for proteins associated with mammalian pathogenicity, possibly involved in the occasional but often fatal cases of human C. violaceum infection. There is, in addition, a series of previously unknown but important enzymes and secondary metabolites including paraquat-inducible proteins, drug and heavy-metal-resistance proteins, multiple chitinases, and proteins for the detoxification of xenobiotics that may have biotechnological applications

Calix[n]arenes as organocatalysts in reactions of Povarov

Neste trabalho empregou-se o ácido p-sulfônico calix[4]areno (CX4SO 3 H) como organocatalisador em reações de Povarov para a obtenção de compostos N- heterocíclicos. A reação de Povarov é uma reação tricompenentes entre uma arilamina, um aldeído e um alqueno ou alquino, catalisada por ácidos de Lewis ou de Brønsted. A reação de Povarov pode fornecer 1,2,3,4-tetraidroquinolinas, quinolinas e julolidinas dependendo das condições de reações empregadas. Neste trabalho foram sintetizadas dezoito julolidinas a partir de diferentes anilinas, estireno e formaldeído. As condições otimizadas para a síntese de julolidina foram: água como solvente, temperatura ambiente,o tempo de reação de 2 horas e a concentração de catalisador de 2 mol%. Os rendimentos variaram de 26% a 89%. As julolidinas foram obtidas como uma mistura de diasterioisômeros com excessos diasterioméricos que variaram de 31-74%, sendo o isômero majoritário cis. Uma nova investigação sobre o mecanismo da reação de Povarov foi estudado pela técnica de espectrometria de massas (ESI-MS), que permitiu detectar intermediários catiônicos para reação, comprovando que o mecanismo da reação de Povarov nessas condições é um processo em etapas. Além disso, foram obtidas oito 1,2,3,4-tetraidroquinolinas também foram obtidas seguindo a mesma metodologia em rendimentos de 9% a 60%. Outra classe de N-heterocíclicos obtida neste trabalho foi as quinolinas, para tanto o formaldeído foi substituído pelo benzaldeído na reação de Povarov. Novamente as condições de reação foram otimizadas, acetonitrila como solvente, temperatura de 80 °C, 12 horas de reação e concentração do catalisador de 1 mol%. Foram sintetizadas dezesseis quinolinas com rendimentos de 38% a 71%. O processo de oxidação da 1,2,3,4- tetraidroquinolina, intermediário da síntese de quinolinas, foi investigado pela técnica de ressonância magnética nuclear (RMN) visando determinar os possíveis aceptores de hidretos.In this work we employed the p-sulphonic acid calix[4]arene (CX4SO 3 H) as organocatalyst in Povarov reactions for obtaining N-heterocyclic compounds. The Povarov reaction is tricompenentes reaction between an aryl amine, an aldehyde and an alkene or alkyne catalyzed by Lewis or Brønsted acids. The Povarov reaction can provide 1,2,3,4-tetrahydroquinoline, quinolines and julolidines depending on the reaction conditions employed.In this study eighteen julolidines were synthesized from various anilines, styrene and formaldehyde. The optimized conditions for synthesis julolidine were: water as solvent, room temperature, reaction time of 2 hours and the catalyst concentration of 2 mol%. Yields ranged from 26% to 89%. The julolidines were obtained as a mixture of diastereomers with diastereomeric excesses ranging from 31-74%, the major cis isomer. New research on the mechanism of the Povarov reaction was studied by technique of mass spectrometry (ESI-MS), which allowed to detect cationic reaction intermediates, confirming that the mechanism for reaction of Povarov these conditions is a process in steps. In addition, eight were obtained 1,2,3,4- tetrahydroquinoline obtained following the same methodology, the yields were of 9% and 60%. Another class of N-heterocyclic obtained in this work was quinolines, for this, the formaldehyde was replaced by the benzaldehyde in Povarov reaction . Again, the reaction conditions were optimized acetonitrile was used as solvent, at 80 ° C, 12 hours of reaction, catalyst concentration of 1 mol%. Sixteen quinolines were synthesized with yields of 38% to 71%.The oxidation of 1,2,3,4-tetrahydroquinoline, intermediate in the synthesis of quinoline was investigated by the technique of nuclear magnetic resonance (NMR) for determine potential acceptors hydrides.Coordenação de Aperfeiçoamento de Pessoal de Nível Superio

Organocatalysis in the three-component Povarov reaction and investigation by mass spectrometry

A diastereoselective three-component cascade reaction, catalyzed by p-sulfonic acid calix[4]arene, provides a unique method to access diverse julolidine derivatives in high yields. Additionally, the reaction was also monitored by mass spectrometry and the mechanistic pathway uncovered

Quinolines: Microwave-assisted synthesis and their antifungal, anticancer and radical scavenger properties

An efficient method for the synthesis of quinolines using microwave irradiation was developed providing 28 quinolines with good yields. The reaction procedures are environmentally friendly, convenient, mild and of easy work-up. Quinolines were evaluated for their antifungal, anticancer and antioxidant properties and exhibited high activities in all tests performed.Fil: Liberto, Natália Aparecida. Universidade Federal de Viçosa. Departamento de Química. Grupo de Química Supramolecular e Biomimética (GQSB); BrasilFil: Baptista Simões, Juliana. Universidade Federal de Viçosa. Departamento de Química. Grupo de Química Supramolecular e Biomimética (GQSB); BrasilFil: Paiva Silva, Sarah de. Universidade Federal de Viçosa. Departamento de Química. Grupo de Química Supramolecular e Biomimética (GQSB); BrasilFil: Silva, Cristiane Jovelina da. Universidade Federal do Minas Gerais; BrasilFil: Modolo, Luzia Valentina. Universidade Federal do Minas Gerais; BrasilFil: Fátima, Ângelo de. Universidade Federal do Minas Gerais; BrasilFil: Silva, Luciana Maria. Fundação Ezequiel Dias. Laboratório de Biologia Celular; BrasilFil: Derita, Marcos Gabriel. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe; ArgentinaFil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; ArgentinaFil: Portilla Zúñiga, Omar Miguel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Investigación y Desarrollo en Ciencias Aplicadas "Dr. Jorge J. Ronco". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Investigación y Desarrollo en Ciencias Aplicadas; ArgentinaFil: Romanelli, Gustavo Pablo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Investigación y Desarrollo en Ciencias Aplicadas "Dr. Jorge J. Ronco". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Investigación y Desarrollo en Ciencias Aplicadas; ArgentinaFil: Fernandes, Sergio Antonio. Fundação Ezequiel Dias. Laboratório de Biologia Celular; Brasi

Evaluation of a quality improvement intervention to reduce anastomotic leak following right colectomy (EAGLE): pragmatic, batched stepped-wedge, cluster-randomized trial in 64 countries

Background Anastomotic leak affects 8 per cent of patients after right colectomy with a 10-fold increased risk of postoperative death. The EAGLE study aimed to develop and test whether an international, standardized quality improvement intervention could reduce anastomotic leaks. Methods The internationally intended protocol, iteratively co-developed by a multistage Delphi process, comprised an online educational module introducing risk stratification, an intraoperative checklist, and harmonized surgical techniques. Clusters (hospital teams) were randomized to one of three arms with varied sequences of intervention/data collection by a derived stepped-wedge batch design (at least 18 hospital teams per batch). Patients were blinded to the study allocation. Low- and middle-income country enrolment was encouraged. The primary outcome (assessed by intention to treat) was anastomotic leak rate, and subgroup analyses by module completion (at least 80 per cent of surgeons, high engagement; less than 50 per cent, low engagement) were preplanned. Results A total 355 hospital teams registered, with 332 from 64 countries (39.2 per cent low and middle income) included in the final analysis. The online modules were completed by half of the surgeons (2143 of 4411). The primary analysis included 3039 of the 3268 patients recruited (206 patients had no anastomosis and 23 were lost to follow-up), with anastomotic leaks arising before and after the intervention in 10.1 and 9.6 per cent respectively (adjusted OR 0.87, 95 per cent c.i. 0.59 to 1.30; P = 0.498). The proportion of surgeons completing the educational modules was an influence: the leak rate decreased from 12.2 per cent (61 of 500) before intervention to 5.1 per cent (24 of 473) after intervention in high-engagement centres (adjusted OR 0.36, 0.20 to 0.64; P &lt; 0.001), but this was not observed in low-engagement hospitals (8.3 per cent (59 of 714) and 13.8 per cent (61 of 443) respectively; adjusted OR 2.09, 1.31 to 3.31). Conclusion Completion of globally available digital training by engaged teams can alter anastomotic leak rates. Registration number: NCT04270721 (http://www.clinicaltrials.gov)