Tag: M.W:100-200

Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings, and research on the structure and performance of functional materials. 702-79-4, Name is 1,3-Dimethyladamantane, SMILES is CC12CC3CC(C1)CC(C)(C3)C2, belongs to quinuclidines compound. In a document, author is Ugawa, T, introduce the new discover, Quality Control of 1,3-Dimethyladamantane.

Effect of YM-53601, a novel squalene synthase inhibitor, on the clearance rate of plasma LDL and VLDL in hamsters

1 To better understand how it decreases plasma cholesterol and triglyceride, we evaluated the effect of YM-53601 ((E-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbozole monohydrochloride) on the clearance rate of low density lipoprotein (LDL) and very low density lipoprotein (VLDL) in hamsters. 2 Treatment with YM-53601 at 50 mg kg(-1) for 5 days in hamsters fed a normal diet enhanced the disappearance of 1,1′-Dioctadecyl-3,3,3′,3′-tetramethylindocarbocyanine perchlorate (DiI)-VLDL and DiI-LDL. This effect on DiI-LDL was lost in the early phase after DiI-methyl(met)-LDL, chemically modified to block LDL receptor binding, was injected in hamsters, but was retained in the late phase. Pre-treatment with prolamine sulphate, which inhibits the activity of LPL, also failed to enhance DiI-VLDL clearance rate by YM-53601. 3 Even on single oral administration at 30 mg kg(-1), YM-53601 enhanced the disappearance of the high concentration of plasma triglyceride after injection of intrafat, an emulsion of fat. Plasma triglyceride was significantly decreased as soon as 1 h after single administration of YM-53601 in hamsters fed a normal diet. 4 These results indicate that the decrease in plasma total cholesterol and triglyceride after the treatment with YM-53601 is due to its enhancement of the clearance rate of LDL and VLDL, respectively. Moreover, YM-53601 may be effective in decreasing plasma triglyceride levels early in the course of treatment of hypertriglyceridaemia in humans.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.If you¡¯re interested in learning more about 702-79-4. The above is the message from the blog manager. Quality Control of 1,3-Dimethyladamantane.

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Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 645-49-8, Name is (Z)-1,2-Diphenylethene, SMILES is C1(/C=CC2=CC=CC=C2)=CC=CC=C1, in an article , author is NORDVALL, G, once mentioned of 645-49-8, Product Details of 645-49-8.

3-LITHIOQUINUCLIDIN-2-ENE – A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF MUSCARINIC AGONISTS AND ANTAGONISTS

A method for the generation of 3-lithioquinuclidin-2-ene (3) as a nucleophilic intermediate for the synthesis of 3-substituted quinuclidin-2-enes is presented.

Because enzymes can increase reaction rates by enormous factors, typically producing only a single product in quantitative yield, they are the focus of active research.In my other articles, you can also check out more blogs about 645-49-8. Product Details of 645-49-8.

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Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 6153-56-6, Name is Oxalic acid dihydrate, SMILES is O=C(O)C(O)=O.[H]O[H].[H]O[H], in an article , author is Ugawa, T, once mentioned of 6153-56-6, Application In Synthesis of Oxalic acid dihydrate.

YM-53601, a novel squalene synthase inhibitor, suppresses lipogenic biosynthesis and lipid secretion in rodents

1 To better understand how it decreases plasma cholesterol and triglyceride levels, we evaluated the effect of (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole monohydrochloride (YM-53601) on lipogenic biosynthesis in the liver and lipid secretion from the liver in rats and hamsters. 2 Single administration of YM-53601 in cholestyramine-treated rats inhibited triglyceride and free fatty acid (FFA) biosynthesis at a similar dose range to that at which it inhibited cholesterol biosynthesis. YM-53601 inhibited both triglyceride and FFA biosynthesis in hamsters treated with cholestyramine. 3 YM-53601 by single oral administration decreased the enhanced plasma triglyceride levels in hamsters induced by an injection of protamine sulfate, which inhibits lipoprotein lipase (LPL) and consequently increases plasma very low-density lipoprotein (VLDL) triglyceride levels. YM-53601 also decreased the enhanced plasma triglyceride and cholesterol levels in hamsters treated with Triton WR1339, which also inhibits the degradation of VLDL. Plasma cholesterol was significantly decreased as soon as I h after single administration of YM-53601 in hamsters fed a normal diet. 4 This is the first report that a squalene synthase inhibitor suppresses lipogenic biosynthesis in the liver and cholesterol and triglyceride secretion from the liver in vivo. We therefore suggest that the mechanism by which YM-53601 decreases plasma triglyceride might include these effects. The finding that YM-53601 rapidly decreased plasma cholesterol suggests that this compound may be effective in decreasing plasma cholesterol levels early in the course of treatment of hypercholesterotemia in humans.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.Interested yet? Keep reading other articles of 6153-56-6, you can contact me at any time and look forward to more communication. Application In Synthesis of Oxalic acid dihydrate.

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Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 1490-25-1, Name is Methyl 4-chloro-4-oxobutanoate, SMILES is O=C(OC)CCC(Cl)=O, in an article , author is Macor, JE, once mentioned of 1490-25-1, Application In Synthesis of Methyl 4-chloro-4-oxobutanoate.

A chiral synthesis of (-)-spiro[1-azabicyclo[2.2.2] octane-3,5 ‘-oxazolidin-2 ‘-one]: A conformationally restricted analogue of acetylcholine that is a potent and selective alpha 7 nicotinic receptor agonist

A direct, short chiral synthesis of the selective 0 nicotinic receptor agonist (-)-spiro[l-azabicyclo[2.2.2]octane-3,5′-oxazolidin-2’-one] (AR-R17779) is presented. The key step utilized attack of the dianion of the (R)-HYTRA ester [(R)-(+)-2-hydroxy-1,2,2-triphenylethyl acetate] on quinuclidin-3-one, followed by a selective precipitation of the diasteriomeric tertiary alcohol that led to (S)-(-)-AR-R17779 in two additional steps.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. 1490-25-1, you can contact me at any time and look forward to more communication. Application In Synthesis of Methyl 4-chloro-4-oxobutanoate.

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner.In an article, author is Naito, R, once mentioned the application of 765-70-8, Name is 3-Methylcyclopentane-1,2-dione, molecular formula is C6H8O2, molecular weight is 112.13, MDL number is MFCD00001417, category is quinuclidines. Now introduce a scientific discovery about this category, Recommanded Product: 3-Methylcyclopentane-1,2-dione.

Selective muscarinic antagonists. II. Synthesis and antimuscarinic properties of biphenylylcarbamate derivatives

A novel series of biphenylylcarbamate derivatives were synthesized and evaluated for binding to M-1, M-2 and M-3 receptors and for antimuscarinic activities. Receptor binding assays indicated that biphenyl-2-ylcarbamate derivatives had high affinities for M-1 and M-3 receptors and good selectivities for M-3 receptor over M-2 receptor, indicating that the biphenyl-2-yl group is a novel hydrophobic replacement for the benzhydryl group in the muscarinic antagonist field. In this series, quinuclidin-1-yl biphenyl-2-ylcarbamate monohydrochloride (81, YM-46303) exhibited the highest affinities for M-1 and M-3 receptors, and selectivity for M-3 over M-2 receptor. Compared to oxybutynin, YM-46303 showed approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats. Moreover, selective antagonistic activity was also observed in vitro. Further evaluation of antimuscarinic effects on bradycardia and presser in pithed rats, and on tremor in mice, showed that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M-3 antagonist with potent activities and fewer side effects.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.Interested yet? Keep reading other articles of 765-70-8, you can contact me at any time and look forward to more communication. Recommanded Product: 3-Methylcyclopentane-1,2-dione.

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Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings, and research on the structure and performance of functional materials. 1679-51-2, Name is Cyclohex-3-en-1-ylmethanol, SMILES is OCC1CCC=CC1, belongs to quinuclidines compound. In a document, author is Johansson, G, introduce the new discover, Application In Synthesis of Cyclohex-3-en-1-ylmethanol.

Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: Synthesis and structure-activity relationships

A series of 25 derivatives of the muscarinic antagonist 3-(2-furanyl)quinuclidin-2-ene (4) was synthesized and evaluated for muscarinic and antimuscarinic properties. Substitution at all three positions of the furan ring has been investigated. The affinities of the new compounds were determined by competition experiments in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate as the radioligand, and the antimuscarinic potency was determined in a functional assay on isolated guinea pig urinary bladder using carbachol as the agonist. Several of the novel derivatives displayed high muscarinic affinities. Whereas the affinity of lead compound 4 for cortical muscarinic receptors is moderate (K-i 300 nM), it is much higher for the 6-methyl (49; K-i = 12 nM), 5-ethyl (52; K-i = 7.4 nM), 5-bromo (33; K-i = 6.4 nM), and 3-phenyl (49; K-i = 2.8 nM) substituted derivatives. The substituent-induced increases in affinity do not appear to be additive as a 5-bromo-3-phenyl (54), and a 5-methyl-3-phenyl (55) substitution pattern only slightly increases affinity (K-i = 1.55 and 2.39 nM, respectively). The conformational preferences of the 3-phenyl (49) and 5-phenyl (51) derivatives were studied by X-ray crystallography and molecular mechanics calculations. Because of the observed high affinity of 49, a series of 16 meta-and para-substituted analogues of 49 was synthesized and tested. derivative (68) exhibited more than 10-fold improvement in affinity as compared to 49. The structure-activity relationships of the new series are well described with QSAR and CoMFA models.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. 1679-51-2, you can contact me at any time and look forward to more communication. Application In Synthesis of Cyclohex-3-en-1-ylmethanol.

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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. 101-39-3, Name is ¦Á-Methyl-trans-cinnamaldehyde, molecular formula is C10H10O, belongs to quinuclidines compound, is a common compound. In a patnet, author is Johansson, G, once mentioned the new application about 101-39-3, Recommanded Product: 101-39-3.

Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: Synthesis and structure-activity relationships

A series of 25 derivatives of the muscarinic antagonist 3-(2-furanyl)quinuclidin-2-ene (4) was synthesized and evaluated for muscarinic and antimuscarinic properties. Substitution at all three positions of the furan ring has been investigated. The affinities of the new compounds were determined by competition experiments in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate as the radioligand, and the antimuscarinic potency was determined in a functional assay on isolated guinea pig urinary bladder using carbachol as the agonist. Several of the novel derivatives displayed high muscarinic affinities. Whereas the affinity of lead compound 4 for cortical muscarinic receptors is moderate (K-i 300 nM), it is much higher for the 6-methyl (49; K-i = 12 nM), 5-ethyl (52; K-i = 7.4 nM), 5-bromo (33; K-i = 6.4 nM), and 3-phenyl (49; K-i = 2.8 nM) substituted derivatives. The substituent-induced increases in affinity do not appear to be additive as a 5-bromo-3-phenyl (54), and a 5-methyl-3-phenyl (55) substitution pattern only slightly increases affinity (K-i = 1.55 and 2.39 nM, respectively). The conformational preferences of the 3-phenyl (49) and 5-phenyl (51) derivatives were studied by X-ray crystallography and molecular mechanics calculations. Because of the observed high affinity of 49, a series of 16 meta-and para-substituted analogues of 49 was synthesized and tested. derivative (68) exhibited more than 10-fold improvement in affinity as compared to 49. The structure-activity relationships of the new series are well described with QSAR and CoMFA models.

Because enzymes can increase reaction rates by enormous factors, typically producing only a single product in quantitative yield, they are the focus of active research.In my other articles, you can also check out more blogs about 101-39-3. Recommanded Product: 101-39-3.

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Quinuclidine – Wikipedia,
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Reference of 111-12-6, Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter. 111-12-6, Name is Methyl oct-2-ynoate, SMILES is CCCCCC#CC(OC)=O, belongs to quinuclidines compound. In a article, author is Nagashima, Shinya, introduce new discover of the category.

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide. (C) 2014 Elsevier Ltd. All rights reserved.

Reference of 111-12-6, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 111-12-6.

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Electric Literature of 2495-37-6, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 2495-37-6, Name is Benzyl methacrylate, SMILES is CC(C(OCC1=CC=CC=C1)=O)=C, belongs to quinuclidines compound. In a article, author is Macor, JE, introduce new discover of the category.

A chiral synthesis of (-)-spiro[1-azabicyclo[2.2.2] octane-3,5 ‘-oxazolidin-2 ‘-one]: A conformationally restricted analogue of acetylcholine that is a potent and selective alpha 7 nicotinic receptor agonist

A direct, short chiral synthesis of the selective 0 nicotinic receptor agonist (-)-spiro[l-azabicyclo[2.2.2]octane-3,5′-oxazolidin-2’-one] (AR-R17779) is presented. The key step utilized attack of the dianion of the (R)-HYTRA ester [(R)-(+)-2-hydroxy-1,2,2-triphenylethyl acetate] on quinuclidin-3-one, followed by a selective precipitation of the diasteriomeric tertiary alcohol that led to (S)-(-)-AR-R17779 in two additional steps.

Electric Literature of 2495-37-6, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 2495-37-6 is helpful to your research.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 2386-57-4, Name is Sodium methanesulfonate, SMILES is CS(=O)([O-])=O.[Na+], in an article , author is Nomoto, F, once mentioned of 2386-57-4, Category: quinuclidines.

A practical chemoenzymatic process to access (R)-quinuclidin-3-ol on scale

(+/-)-3-Butyryloxyquinuclidinium butyrate 6 (2 M, 571 g/L), prepared from (+/-)-quinuclidin-3-ol 1 and butyric anhydride, undergoes enantioselective hydrolysis by an Aspergillus melleus protease {1.0% (w/v)} in water in the presence of Ca(OH)(2) to keep the reaction at pH 7 and trap butyric acid that is introduced as part of (+/-)-6 and generated by the enzymatic hydrolysis. After a 24 h period, extraction with n-heptane provides (R)-quinuclidin-3-yl butyrate 5a, which, on methanolysis with Na2CO3, is converted into (R)-1, a common pharmacophore of neuromodulators acting on muscarinic receptors, in 96% ee and 42% overall yield from (+/-)-1. The unwanted antipode (S)-1, which is extracted into n-butanol and purified via its hydrochloride salt in 89% ee and 40% overall yield from (+/-)-1, can be racemized by the catalysis of Raney Co at 140degreesC under an atmosphere of H, (5 kg/cm(2)) to regenerate (+/-)-1 in 97% yield. (C) 2003 Elsevier Science Ltd. All rights reserved.

Interested yet? Read on for other articles about 2386-57-4, you can contact me at any time and look forward to more communication. Category: quinuclidines.

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