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Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands

A set of novel heterocyclic ligands (7a-9a, 7b-9b, and 9c) structurally related to oxotremorine 2 was designed, synthesized, and tested at muscarinic receptor subtypes. In the binding experiments at cloned hm1-5, the presence of the 2-methylimidazole/2-methyl-3-alkylimidazolium moiety in place of the pyrrolidine ring revealed, in derivatives 8a, 8b, and 9c, a moderate selectivity for some receptor subtypes. The functional in vitro assays yielded results that correlated closely to binding data. In general, on passing from agonists bearing the pyrrolidine moiety to their analogues carrying the 2-methylimidazole function, the overall pharmacological efficacy profile is shifted from agonism toward partial agonism. The insertion of the 2-methyl-3-alkylimidazolium moiety advances the effect such that the compounds are pure antagonists. Quite similarly, chiral 3-oxo-Delta 2-isoxazoline (¡À)-10 behaved as a weak antagonist unable to discriminate the different muscarinic receptor subtypes.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1233NO – PubChem

 

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Acrylic compound as well as preparation method, pharmaceutical composition and application thereof (by machine translation)

The invention provides an acrylic compound as well as a preparation method, a pharmaceutical composition and application thereof, and concretely provides a compound represented by the following formula I: wherein each group is defined as described in the specification. The compound disclosed by the invention can be used as CREB/CRTC2 an angiogenesis inhibitor and is used for preparing a pharmaceutical composition for treating diabetes and other diseases. (by machine translation)

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Oxazolidine – Wikipedia,
Oxazolidine | C3H156NO – PubChem

 

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Direct entry to peptidyl ketones via SmI2-mediated C-C bond formation with readily accessible N-peptidyl oxazolidinones

(Chemical Equation Presented) In this work, a new method for the preparation of peptidyl ketones is presented employing a SmI2/H 2O-mediated coupling of N-peptidyl oxazolidinones with electron-deficient alkenes. The requisite peptide imides were easily prepared by solution-phase peptide synthesis starting from an N-acyl oxazolidinone derivative of an amino acid. Importantly, they could be used directly in the C-C bond-forming step without the need for further functionalization. Coupling of these peptide derivatives with a second peptide possessing an N-terminal acryloyl group leads to ketomethylene isosteres of glycine-containing peptides. This method represents an alternative means for ligating two small peptides through a C-C bond-forming step.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H821NO – PubChem

 

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, 1192-07-0, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1192-07-0, Name is Isoxazolidin-3-one, molecular formula is C3H5NO2. In a Article, authors is Reis£¬once mentioned of 1192-07-0

Use of herbicides in sugarcane in the Sao Paulo state

Sugarcane is one of the main agricultural cultivations of Brazil, and one of the crops in which herbicides are most applied. In the 2017/2018 season, the estimated sugarcane production was 694.54 million tons, with an estimated increase of 0.9% in yield for this season. In order to evaluate the use of herbicides in this crop in the Sao Paulo State during a five-year period, a survey was carried out with sugarcane farmers. The use of herbicides applied alone and in a formulated mixture, according to their mechanism of action, were evaluated from 2010 to 2014. Photosystem II inhibitor herbicides were the most used in this period and the total amount of herbicides of almost all mechanism of action increased from 2010 to 2014, except for photosystem I inhibitors herbicides. The use of formulated mixtures also increased during this period. The area treated with carotenoid biosynthesis and photosystem II inhibitor herbicides was the largest for the control of monocotyledonous species (Poaceae, Cyperaceae and Commelinaceae). In relation to the dicotyledonous species, the area treated with PROTOX inhibitor herbicides was the largest in all evaluated years.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H1242NO – PubChem

 

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497-25-6, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 497-25-6, Name is Oxazolidin-2-one, molecular formula is C3H5NO2. In a Article, authors is Pereira, Elisabeth Rodrigues£¬once mentioned of 497-25-6

Syntheses and antimicrobial activities of five-membered ring heterocycles coupled to indole moieties

Indole-substituted oxazolidinones, oxazolones, pyrrolidinone, imidazolidinone and imidazolones were synthesized. Their inhibitory potencies towards protein kinase C and protein kinase A were determined and their in vitro activities against Streptomyces chartreusis, Streptomyces griseus, Bacillus cereus, Candida albicans and Escherichia coli were examined. The inhibition of Streptomyces sporulation observed for some of them could not be linked to in vitro protein kinase C inhibition. All proved inactive against C. albicans but three of them exhibited a marked activity towards E. coli. This effect extends to other Gram-negative bacteria.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H892NO – PubChem

 

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Multicomponent Strategy for the Synthesis of Prostaglandin E2 Methyl Ester under Anion Relay Chelation Control

(Chemical Equation Presented). Starting with four components, the enantioselective synthesis of prostaglandin E2 methyl ester has been achieved through a highly stereoselective heteroatom-directed conjugate addition reaction and cyclopentanone ring cyclization as the key steps. This asymmetric strategy includes (i) an asymmetric Reformatsky reaction; (ii) conjugate addition of a chiral vinyllithium reagent; (iii) cyclization to form a sulfonylated cyclopentanone in one-pot; followed by (iv) allylation of the side chain. Four carbon-carbon bond-forming processes and three stereogenic centers were established, with the steps from (ii) to (iii) being achieved in a one-pot process.

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Oxazolidine | C3H626NO – PubChem

 

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Analysis of volatile flavour compounds and acrylamide in roasted Malaysian tropical almond (Terminalia catappa) nuts using supercritical fluid extraction

Considering the importance of tropical almond nuts as a snack item, a study was conducted to identify the flavour volatiles and acrylamide generated during the roasting of the nuts. The supercritical fluid extracted flavour components revealed 74 aroma active compounds made up of 27 hydrocarbons, 12 aldehydes, 11 ketones, 7 acids, 4 esters, 3 alcohols, 5 furan derivatives a pyrazine, and 2 unknown compounds. While low levels of acrylamide (8-86 mug/kg) were obtained in the roasted nuts, significant (P< 0.05) increases occurred in concentration with increased roasting temperature and time. Carboxylic acids were the most abundant volatiles in the roasted almond nuts and less significant (P>. 0.05) concentration of acrylamide was generated with mild roasting and shorter roasting period.

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Oxazolidine | C3H719NO – PubChem

 

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497-25-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 497-25-6, molcular formula is C3H5NO2, introducing its new discovery.

Meta-phenylenediamines, process for preparation thereof, intermediate compounds and use of these meta-phenylenediamines as couplers for the oxidation dyeing of keratinous fibres and especially human hair

New meta-phenylenediamines, process for preparation thereof, intermediate compounds and use of these metaphenylenediamines as couplers for the oxidation dyeing of keratinous fibres and especially human hair. The invention relates to the compounds of the formula: STR1 in which R1 and R2 denote, independently of one another, a hydrogen atom, a C1 -C4 alkyl radical or a C2 -C3 mono- or polyhydroxyalkyl radical, Z and Z’ denote, independently of one another, a C1 -C4 alkyl or C2 -C4 hydroxyalkyl radical, with the proviso that, when R1 and R2 simultaneously denote a hydrogen atom, Z and Z’ do not simultaneously denote a methyl radical, and to their addition salts with an acid, to a process for preparation thereof and also to their use, by way of couplers, in an aqueous vehicle, in combination with at least one oxidation dye percursor of the para type, for the dyeing of human hair. The invention also relates to the intermediate compounds of the formula: STR2 in which R’ denotes a hydrogen atom, a C1 -C4 alkyl radical, a C2 or C3 mono- or polyhydroxyalkyl radical, or an acetyl or beta-chloethoxycarbonyl radical, and z and z’ denote, independently of one another, a C1 -C4 alkyl radical.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H137NO – PubChem

 

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Direct assembly of 2-oxazolidinones by chemical fixation of carbon dioxide

The reaction of beta- and gamma-haloamines with carbon dioxide to give pharmaceutically relevant 2-oxazolidinones and 1,3-dioxazin-2-ones, was found to proceed efficiently in the presence of a base and in the absence of catalyst. After optimization of reaction conditions, the system was successfully expanded to a variety of haloamines, even at multigram scale. The reaction was further studied in silico by DFT calculations. The reaction of beta- and gamma-haloamines with carbon dioxide to give pharmaceutically relevant cyclic urethanes was found to proceed efficiently in the presence of a base and in the absence of catalyst (see figure). After optimization of reaction conditions, the system was expanded to a variety of haloamines, even at a multigram scale. The reaction was further studied in silico by DFT calculations.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H861NO – PubChem

 

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497-25-6, Name is Oxazolidin-2-one, belongs to oxazolidine compound, is a common compound. 497-25-6In an article, authors is Akkarachalanont, Phattara, once mentioned the new application about 497-25-6.

New reactive extraction based reclaiming technique for amines used in carbon dioxide capture process from industrial flue gases

A new reclaiming technique based on reactive extraction for removal of heat stable salts (HSS) from monoethanolamine (MEA) used in carbon dioxide (CO2) capture process has been developed. The extraction process was based on the use of tri-n-octylamine (TOA), Aliquat 336, OH- modified Aliquat 336, a two-step extraction (modified Aliquat followed by TOA), and mixed extractant (modified Aliquat and TOA) in 1-octanol diluent. The best parameters were 69% OH- modified Aliquat, two-step extraction, and mixed extractant (modified Aliquat and TOA) and under optimum extraction conditions were able to improve the extraction efficiency of the original Aliquat and TOA to over 90%. The two-step extraction and mixed extractant were also capable of managing Cl- contamination in MEA solution. Extraction was found to be independent of temperature whereas efficiency reduced with increase of CO2 loading. Therefore, it is recommended to apply this extraction technique to the lean MEA stream after the rich/lean heat exchanger either with or without cooling. Regeneration of used extractant (OH Aliquat) was implemented and optimized with the use of 4 kmol/m3 NaOH. In addition to HSS removal, the new extraction technique was also able to remove major nonionic degradation products also by up to 90%.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H280NO – PubChem