Discovery of Furan-2,4(3H,5H)-dione

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Ethyl 1-aryl-4,5-dioxo-2-phenyl-4,5-dihydro-1H-pyrrole-3-carboxylates reacted with tetronic acid in boiling anhydrous toluene in the presence of acetic acid to give ethyl 1-aryl-4,4-bis(4-hydroxy-2-oxo-2,5-dihydrofuran-3-yl)-5-oxo-2-phenyl-4,5-dihydro-1H-pyrrole-3-carboxylates.

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A comprehensive review on the chemistry of Spongia sp. is here presented, together with the biological activity of the isolated compounds. The compounds are grouped in sesquiterpene quinones, diterpenes, C21 and other linear furanoterpenes, sesterterpenes, sterols (including secosterols), macrolides and miscellaneous compounds. Among other reports we include studies on the intraspecific diversity of a Mediterranean species, compounds isolated from associated sponge and nudibranch and compounds isolated from S. zimocca and the red seaweed Laurentia microcladia. Under biological activity a table of the reported biological activities of the various compounds and the biological screening of extracts are described. The present review covers the literature from 1971 to 2015.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Ethyl 1-aryl-4,5-dioxo-2-phenyl-4,5-dihydro-1H-pyrrole-3-carboxylates reacted with tetronic acid in boiling anhydrous toluene in the presence of acetic acid to give ethyl 1-aryl-4,4-bis(4-hydroxy-2-oxo-2,5-dihydrofuran-3-yl)-5-oxo-2-phenyl-4,5-dihydro-1H-pyrrole-3-carboxylates.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.

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Whitefly (Bemisia tabaci Gennadius) is a devastating pest of vegetables, cotton, and many other agricultural and horticultural crops worldwide. Since control of B. tabaci on vegetable crops solely depends on the use of chemical insecticides in India; monitoring the insecticide resistance of B. tabaci populations would be very much essential for achieving successful control and for managing the resistance development. Hence, the aim of the present study was to examine the resistance in different field strains of B. tabaci to traditional organophosphates and new chemical insecticides in India. The resistance ratios were recorded in the range of 30.67?131.48 fold for acephate, 29.17?83.67 fold for triazophos, 0.38?2.51 fold for indoxacarb, 4.55?34.52 fold for dinotefuran, 6.26?27.56 fold for tolfenpyrad, 7.87?31.89 fold for spiromesifen, 1.61?30.08 fold for pyriproxyfen, and 3.09?45.92 fold for flonicamid in comparison to that of the susceptible strain in the laboratory. Resistance levels of B. tabaci populations against the tested insecticides were significantly variable among localities. The present data will be helpful for the selection of proper insecticides on vegetable crops in the field for successful management of B. tabaci in near future.

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Tetrahydrofuran – Wikipedia,
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Synthesis of diverse spiro-heterocyclic compounds via the ring-closing (RCM) metathesis approach is described. Specifically, synthesis of various derivatives of barbituric acid, Meldrum’s acid, tetronic acid and thiotetronic acid are described by RCM approach.

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Current dietary assessment methods including FFQ, 24-h recalls and weighed food diaries are associated with many measurement errors. In an attempt to overcome some of these errors, dietary biomarkers have emerged as a complementary approach to these traditional methods. Metabolomics has developed as a key technology for the identification of new dietary biomarkers and to date, metabolomic-based approaches have led to the identification of a number of putative biomarkers. The three approaches generally employed when using metabolomics in dietary biomarker discovery are: (i) acute interventions where participants consume specific amounts of a test food, (ii) cohort studies where metabolic profiles are compared between consumers and non-consumers of a specific food and (iii) the analysis of dietary patterns and metabolic profiles to identify nutritypes and biomarkers. The present review critiques the current literature in terms of the approaches used for dietary biomarker discovery and gives a detailed overview of the currently proposed biomarkers, highlighting steps needed for their full validation. Furthermore, the present review also evaluates areas such as current databases and software tools, which are needed to advance the interpretation of results and therefore enhance the utility of dietary biomarkers in nutrition research.

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Tetrahydrofuran – Wikipedia,
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Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. Mutations in copper/zinc superoxide dismutase 1 (SOD1) have been implicated in the pathophysiology of this disease. Using a high-throughput screening assay expressing mutant G93A SOD1, two bioactive chemical hit compounds (1 and 2), identified as arylsulfanyl pyrazolones, were identified. The structural optimization of this scaffold led to the generation of a more potent analogue (19) with an EC50 of 170 nM. To determine the suitability of this class of compounds for further optimization, 1 was subjected to a battery of pharmacokinetic assays; most of the properties of 1 were good for a screening hit, except it had a relatively rapid clearance and short microsomal half-life stability. Compound 2 was found to be blood-brain barrier penetrating with a brain/plasma ratio = 0.19. The optimization of this class of compounds could produce novel therapeutic candidates for ALS patients.

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The first enantioselective synthesis of 4-aza-podophyllotoxin derivatives by partial transfer hydrogenation of lactone-fused quinolines was achieved using a chiral Bronsted acid catalyst. This reaction was extended to a large scope of substrates with good yields and enantioselectivities.

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The quinoline core possesses a vast number of biological activities such as anticancer, antimalarial, antimicrobial, antifungal, antitubercular and antileishmanial. The conventional classical synthetic methods require the use of expensive and harsh conditions such as high temperature. Currently the scientific communities are searching new methodology to eliminate the use of chemicals, solvents and catalysts, which are hazardous to human health as well as to environment. This review provides a concise overview of new dimensions of green chemistry approaches in designing quinoline scaffold that would encourage the researchers towards green chemistry as well as future application of these greener, non-toxic, environment friendly methods in designing quinoline scaffold.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem