Biodiesel demand is increasing all over the world and the inhibition of microbial growth during the storage of this biofuel is extremely important. There are few studies involving the evaluation of biocides specifically for biodiesel. In the present work, we synthesized and evaluated a set of biocide candidates from chemical transformations in triacylglycerides. Samples of pure biodiesel with the products were evaluated against microorganisms which have been isolated from biodiesel/diesel blends (fungi A. niger, A. fumigatus, C. albicans and S. cerevisiae; and bacteria B. subtilis and Acinetobacter sp.). None of the products inhibited the growth of bacteria. Four nitrated derivatives presented fungicidal activity. The nitrated derivatives were also evaluated as cetane number improvers for B7 biodiesel/diesel blend. The nitrates of soybean methoxylated ethylene glycol esters increased the cetane number by more than three points. Despite showing modest biocide activity, the results can guide the planning of new products from triacylglycerides.

In the last decade, the research works on microbial as a potential source of lipid for biodiesel production have been growing. In this work, the potential of a sludge from high-rate lagoons in urban sewage treatment, composed mainly by Chlorella sp., as oil source for biodiesel production, was studied. The potential of Chlorella sp. growth in photobioreactor under controlled conditions was also investigated. Low lipid content (up to 3%) was observed in both cases. The composition of both oils showed high amount of fatty acids and fatty acid based compounds, however there are also other non-fatty acid based lipids. Density and viscosity of biodiesel from biosolid oil were determined and the results showed that these physico-chemical properties do not match the specification required for biodiesel. The results showed that sewage sludge from Samambaia treatment station (DF, Brazil) and Chlorella sp. cultivated under the conditions described in this work are not potential sources of fatty material for biodiesel production.

Chagas' disease is a parasitic disease with unsatisfactory treatment, mainly in chronic stage. This study aimed to evaluate the trypanocidal activity and action mechanisms of α/β-amyrin and its semi-synthetic derivatives, together with four isolated natural triterpenes, tested against trypomastigote and amastigote forms. The structure-activity relationship was suggested and cytotoxicity was measured. In general, greater polar compounds may have improved the selectivity to the protozoan. Action mechanisms were only performed for the amastigotes of Trypanosoma cruzi by evaluating the ultrastructural alterations, membrane permeability, mitochondrial membrane potential and cell volume, since the majority of compounds displayed promising antiamastigote activities. Triterpenes promoted changes on mitochondrial membrane potential and ultrastructural features that suggest autophagy processes. Both combinations between α/β-amyrin and 3-O-acetyl-11-oxo-α/β-amyrin and 3-O-acetyl-α/β-amyrin with benznidazole displayed synergistic effects against amastigotes and antagonistic effects on LLCMK2 cells. The antiamastigote activities, chemical derivatization, drug combinations and action mechanisms revealed to be crucial approaches toward this chronic disease.

In this study, whole cells of marine-derived fungi were used to reduce isatin (1H-indole-2,3-dione) to dioxindole (3-hydroxyindolin-2-one) for 7 days at 32 °C. The screening showed that several strains could reduce isatin and produce the enantioenriched dioxindole. The best conversions were obtained by Cladosporium sp. CBMAI 1237 and Westerdykella sp. CBMAI 1679, however, the best enantiomeric excess was obtained only by Aspergillus sydowii CBMAI 935 (66% ee). In conclusion, marine-derived fungi show potential for asymmetric and chemoselective reduction of isatin (1H-indole-2,3-dione).

Through dereplication strategies using gas chromatography-mass spectrometry (GC-MS) and ultra fast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS), the ethanol extract from Psycotria nemorosa leaves (Rubiaceae) showed to be composed of: cinnamic acid, dihydroactinidiolide, 4-hydroxy-β-ionone, phytol, isophytol, 4,8,12,16-tetramethylheptadecan-4-olide, lupeol, a mixture of α/β-amyrin, the keto and acetylated derivatives, besides stigmast-4-en-3-one, campesterol, stigmasterol and γ-sitosterol by GC-MS. Likewise, by UFLC-MS/MS, the main compounds identified were: butin, resveratrol, rutin, kaempferol 7-O-β-D-glucopyranoside, deacetylasperuloside, epiloganin, hordenine, strictosidine, N-methyl-1,2,3,4-tetrahydro-β-carboline and N-formyl-tryptamine. The antinociceptive activity of the crude extract ant its fractions was reported.

This short report describes the preparation of twelve isatin derivatives, 5'-(4-alkyl/aryl-1H-1,2,3-triazoles), using 5-azido-spiro[1,3-dioxolane-2,3'-indol]-2'(1'H)-one in the presence of various alkynes under acidic conditions and ultrasound irradiation. Compared with conventional methods, yields increased to 78-98%, and reaction times decreased to 5 min. Besides time and energy saving, there was no need for purification of the product by column chromatography on silica gel, generating less waste and spent solvent.

Psychotria genus (Rubiaceae) is featured into the angiosperm, being the most speciose genus comprising approximately 1600 species. The available references demonstrate that Psychotria has several uses on traditional medicine including spiritual and cultural purposes, and presents great potential on pharmacological properties, especially the one related to neurodegenerative diseases. Despite its wide biological properties, this genus has shown complex phylogenetic analysis due to lack of chemotaxonomic information. In recent years, the interest in these plants has increased considerably and many active compounds have been isolated. Phytochemical investigations described in the literature confirmed the indole alkaloids as the major compounds and besides that, another particular chemical constituent are cyclic peptides, known as cyclotides. This present review will cover the relevant literature from 1962 until 2015, and outlines the current data on taxonomy, chemotaxonomy, traditional uses, pharmacological properties, chemical composition and ecological approach from Psychotria genus.

RESUMO O Geissospermum vellosii (Pau pereira) é uma árvore brasileira, cujas cascas do caule são ricas em alcalóides indólicos que apresentam intensa atividade anticolinesterásica. Este estudo avaliou os efeitos de uma fração da casca (fração PPAC) e do extrato etanólico (EE) do Pau pereira em modelos clássicos de inflamação e dor em murinos. O EE e a fração PPAC, ambos na dose de 30 mg/kg, reduziram significativamente a constrição abdominal induzida por ácido acético em camundongos em 34,8% e 47,5% respectivamente. No teste da formalina, o EE (30 mg/kg) e a fração PPAC (30 e 60 mg/kg) inibiram somente a segunda fase em 82,8%; 84,9% e 100%, respectivamente. Comparado com a indometacina, doses similares do EE ou da fração PPAC foram cerca de duas vezes mais eficazes em causar antinocicepção. A fração PPAC não foi eficaz no teste da placa quente, enquanto reduziu a resposta inflamatória na segunda (50,6%) e na terceira (57,8%) horas do edema de pata de rato induzido por carragenina. A atividade anti-hiperalgésica foi observada depois de 30 min com um pico em 2 h (60,1%). Esses resultados mostrararam que os compostos presentes na fração PPAC têm atividade anti-inflamatória e antinociceptiva por um mecanismo aparentemente não relacionado ao sistema opióide. A despeito das respostas similares às observadas para a indometacina, os efeitos da fração PPAC são atribuídos principalmente às ações da acetilcolina.

ABSTRACT Geissospermum vellosii (Pao pereira) is a Brazilian tree whose stem barks are rich in indole alkaloids that present intense anticholinesterase activity. The present study evaluated the effects of a stem bark fraction (PPAC fraction) and ethanolic extract (EE) of Pao pereira in classic murine models of inflammation and pain. The EE and PPAC fraction, both at a dose of 30 mg/kg, significantly reduced mice abdominal constriction induced by acetic acid by 34.8% and 47.5%, respectively. In the formalin test, EE (30 mg/kg) and PPAC fraction (30 and 60 mg/kg) inhibited only the second phase, by 82.8%, 84.9% and 100%, respectively. Compared with indomethacin, similar doses of EE or PPAC fraction were approximately twice as effective in causing antinociception. PPAC fraction was not effective in the hot plate test but reduced the inflammatory response at the second (50.6%) and third (57.8%) hours of rat paw edema induced by carrageenan. Antihyperalgesic activity was observed within 30 min with a peak at 2 h (60.1%). These results demonstrate that compounds in PPAC fraction have anti-inflammatory and antinociceptive activity by a mechanism apparently unrelated to the opioid system. Regardless of similar responses to indomethacin, the effects of PPAC fraction are mainly attributed to acetylcholine actions.

Nuclear magnetic resonance is a technique that is widely used for elucidating and characterizing organic substances. Organofluorine substances have applications in many areas from drugs to liquid crystals, but their NMR spectra are often challenging due to fluoride coupling with other nuclei. For this reason, NMR spectra of this class of substances are not commonly covered in undergraduate and graduate chemistry courses and related fields. Thus, the aim of this work was the presentation and discussion of 1H, 13C, and 19F NMR spectra of eleven organofluorine substances which, in the case of 1H and 13C nuclei, showed classic patterns of first-order coupling and the effects of the fluorine nucleus in different chemical and magnetic environments. In addition, the observation of long distance coupling constants was possible through the use of apodization functions in the processing of the spectra. It is expected that the examples presented herein can be utilized and discussed in undergraduate and graduate NMR spectroscopy disciplines and thus improve the teaching and future research of organofluorine compounds.

Este artigo descreve a preparação de uma série de 16 ácidos antranílicos, em rendimentos que variaram de 51 a 97%, através do tratamento de isatinas com NaOH e H2O2. Independentemente da natureza do substituinte no anel aromático, as reações se completaram em 15 min. a temperatura ambiente, ao passo que as isatinas contendo substituinte no átomo de nitrogênio requereram um tempo maior para completar a reação (45 min.), sob as mesmas condições.

This paper describes the preparation of a series of 16 anthranilic acids in yields ranging from 51 to 97%, by treating the isatins with NaOH and H2O2. Independently of the nature of the substituent on the aromatic ring, the reactions were complete in 15 min at room temperature, whereas those of isatins containing a substituent on the nitrogen atom required longer reaction time for completion (45 min) under the same reaction conditions.

As isatinas e os 1H-1,2,3-triazóis são duas classes de compostos com grande destaque na síntese orgânica e na química medicinal uma vez que são núcleos heterociclos com elevada reatividade, que permitem a obtenção de diversos compostos com importantes propriedades biológicas. Neste artigo, a síntese de novos 5`-(4-alquil/aril-1H-1,2,3-triazóis)-isatina via reação de cicloadição 1,3-dipolar catalisada por ácido acético é descrita.

Isatin and 1H-1,2,3-triazoles are two classes of compounds with great prominence in organic synthesis and medicinal chemistry as they are heterocycle nuclei with a high reactivity allowing to obtain several compounds with important biological properties. Herein, the synthesis of novel 5'-(4-alquil/aril-1H-1,2,3-triazole)-isatin via reaction of 1,3-dipolar cycloaddition catalyzed by acetic acid is reported.

The paper traces a panorama of the development of new drugs and hopes to contribute for Brazil to become a player in the discovery of new drugs. Brazil is the sixth world market retail consumer of medicines prone to expansion, has a pharmaceutical industry focused on the production of generics and a very large number of undergraduate courses in Pharmacy. The national industry has grown over the last decade after the Generics Act 9787/99. Despite these positive aspects, a number of bottlenecks prevent Brazilian pharmaceutical industry to invest in the development of new drugs. There are, however, a number of initiatives to reduce the dependence on imported generic drugs. It is a very good start for the development of new pharmaceutical drugs.