Category: quinuclidines

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Name: Cyclohex-3-en-1-ylmethanol, 1679-51-2, Name is Cyclohex-3-en-1-ylmethanol, SMILES is OCC1CCC=CC1, belongs to quinuclidines compound. In a document, author is NORDVALL, G, introduce the new discover.

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.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 1679-51-2. Name: Cyclohex-3-en-1-ylmethanol.

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Application of 101-39-3, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 101-39-3, Name is ¦Á-Methyl-trans-cinnamaldehyde, SMILES is O=C/C(C)=C/C1=CC=CC=C1, belongs to quinuclidines compound. In a article, author is McDonald, Ivar M., introduce new discover of the category.

Discovery of a novel series of quinolone alpha 7 nicotinic acetylcholine receptor agonists

High throughput screening led to the identification of a novel series of quinolone alpha 7 nicotinic acetylcholine receptor (nAChR) agonists. Optimization of an HTS hit (1) led to 4-phenyl-1-(quinuclidin-3-ylmethyl)quinolin-2(1H)-one, which was found to be potent and selective. Poor brain penetrance in this series was attributed to transporter-mediated efflux, which was in turn due to high pK(a). A novel 4-fluoroquinuclidine significantly lowered the pK(a) of the quinuclidine moiety, reducing efflux as measured by a Caco-2 assay. (C) 2013 Elsevier Ltd. All rights reserved.

Application of 101-39-3, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 101-39-3 is helpful to your research.

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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 583-60-8, Name is 2-Methylcyclohexanone, molecular formula is C7H12O, belongs to quinuclidines compound, is a common compound. In a patnet, author is Primozic, Ines, once mentioned the new application about 583-60-8, Application In Synthesis of 2-Methylcyclohexanone.

Influence of the Acyl Moiety on the Hydrolysis of Quinuclidinium Esters Catalyzed by Butyrylcholinesterase

Eight chiral esters of quinuclidin-3-ol and butyric, acetic, pivalic and benzoic acid were synthesized as well as their racemic and chiral, quaternary N-benzyl derivatives. All racemic and chiral quaternary compounds were studied as substrates and/or inhibitors of horse serum butyrylcholinesterase (BChE). The best substrate for the enzyme was (R)-N-benzyl butyrate. The rates of hydrolysis decreased in order (R)-butyrate >> (R)-acetate (7-fold slower) > (R)-pivalate (8-fold slower) > (R)-benzoate (9-fold slower reaction), while (S)-N-benzyl esters were much poorer substrates (320 (butyrate) – 4360-fold slower (pivalate) than the appropriate (R)-enantiomer). For all (S)-N-benzyl esters excluding (S)-N-benzyl acetate inhibition constants were determined (K-a = 3.3-60 mu mol dm(-3)). The hydrolysis of racemic mixtures of N-benzyl esters proceeded 1.4 (for acetate) – 5.1 (for benzoate) times slower than that of pure (R)-enantiomers of the corresponding concentrations due to the inhibition with (S)-enantiomers. Change of the acyl moiety of the substrate effected both activity and stereoselectivity of the BChE.(doi: 10.5562/cca1829)

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 583-60-8. The above is the message from the blog manager. Application In Synthesis of 2-Methylcyclohexanone.

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Reference of 272778-12-8, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 272778-12-8, Name is (S)-3-((2R,5S)-5-(4-Fluorophenyl)-2-((S)-((4-fluorophenyl)amino)(4-((trimethylsilyl)oxy)phenyl)methyl)-5-((trimethylsilyl)oxy)pentanoyl)-4-phenyloxazolidin-2-one, SMILES is O=C1OC[C@H](C2=CC=CC=C2)N1C([C@@H]([C@H](NC3=CC=C(F)C=C3)C4=CC=C(O[Si](C)(C)C)C=C4)CC[C@@H](C5=CC=C(F)C=C5)O[Si](C)(C)C)=O, belongs to quinuclidines compound. In a article, author is Naito, R, introduce new discover of the category.

Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists

In the course of continuing efforts to develop potent and bladder-selective muscarinic M-3 receptor antagonists, quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives and related compounds were designed as conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate (8). Binding assays with rat muscarinic receptor subtypes revealed that the quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives showed high affinities for the M3 receptor, and selectivity for the M3 receptor over the M-2 receptor. Of these derivatives, (+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monohydrochloride (9b) exhibited almost the same inhibitory activity against bladder contraction to that of oxybutynin (1), and more than 10-fold selectivity for bladder contraction versus salivary secretion, demonstrating that 9b may be useful for the treatment of symptoms associated with overactive bladder without having side effects such as dry mouth.

Reference of 272778-12-8, 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. you can also check out more blogs about 272778-12-8.

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Chemistry, like all the natural sciences, SDS of cas: 924-50-5, begins with the direct observation of nature¡ª in this case, of matter.924-50-5, Name is Methyl-3,3-dimethylacrylate, SMILES is O=C(OC)C=C(C)C, belongs to quinuclidines compound. In a document, author is Ugawa, T, introduce the new discover.

YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species

1 The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and fibrates, respectively. 2 YM-53601 equally inhibited squalene synthase activities in hepatic microsomes prepared from several animal species and also suppressed cholesterol biosynthesis in rats (ED50, 32 mg kg(-1)). 3 In guinea-pigs, YM-53601 and pravastatin reduced plasma nonHDL-C (= total cholesterol – high density lipoprotein cholesterol) by 47% (P<0.001) and 33% (P<0.001), respectively (100 mg kg(-1), daily for 14 days). In rhesus monkeys, YM-53601 decreased plasma nonHDL-C by 37% (50 mg kg(-1) twice daily for 21 days, P<0.01), whereas the HMG-CoA reductase inhibitor, pravastatin, failed to do (25 mg kg(-1), twice daily for 28 days). 4 YM-53601 caused plasma triglyceride reduction in hamsters fed a normal diet (81% decrease at 50 mg kg-l, daily for 5 days, P<0.001). In hamsters fed a high-fat diet, the ability of YM-53601 to lower triglyceride (by 73%, P<0.001) was superior to that of fenofibrate (by 53%, P<0.001), the most potent fibrate (dosage of each drug: 100 mg kg(-1), daily for 7 days). 5 This is the first report that a squalene synthase inhibitor is superior to an HMG-CoA reductase inhibitor in lowering plasma nonHDL-C level in rhesus monkeys and is superior to a fibrate in significantly lowering plasma triglyceride level. YM-53601 may therefore prove useful in treating hypercholesterolemia and hypertriglyceridemia 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. you can also check out more blogs about 924-50-5. SDS of cas: 924-50-5.

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In an article, author is Macor, JE, once mentioned the application of 140-67-0, Name is 1-Allyl-4-methoxybenzene, molecular formula is C10H12O, molecular weight is 148.2017, MDL number is MFCD00008653, category is quinuclidines. Now introduce a scientific discovery about this category, Recommanded Product: 1-Allyl-4-methoxybenzene.

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.

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Quinuclidine – Wikipedia,
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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 4070-80-8, Name is Sodium 2-octadecylfumarate, molecular formula is C22H39NaO4, belongs to quinuclidines compound, is a common compound. In a patnet, author is Nordvall, G, once mentioned the new application about 4070-80-8, Application In Synthesis of Sodium 2-octadecylfumarate.

3-(2-benzofuranyl)quinuclidin-2-ene derivatives: Novel muscarinic antagonists

A series of 26 derivatives of the novel muscarinic antagonist 3-(2-benzofuranyl) quinuclidin-2-ene (1) has been synthesized and evaluated for muscarinic and antimuscarinic properties. The affinity of the compounds was 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. The 5-fluorobenzofuranyl derivative was slightly more potent than 1. The 7-bromo-substituted 8 displayed a 14-fold tissue selectivity ratio for muscarinic receptors in the cortex versus the parotid gland. Comparative molecular field analysis and quantitative structure-activity relationship models were developed for this series of substituted benzofuranyl derivatives.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 4070-80-8. The above is the message from the blog manager. Application In Synthesis of Sodium 2-octadecylfumarate.

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Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 31566-31-1, Name is Glyceryl monostearate. In a document, author is CLARK, RD, introducing its new discovery. Application In Synthesis of Glyceryl monostearate.

N-(QUINUCLIDIN-3-YL)-2-(1-METHYL-1H-INDOL-3-YL)-2-OXOACETAMIDE – A HIGH-AFFINITY 5-HT3 RECEPTOR PARTIAL AGONIST

The enantiomers of the indolyl-2-oxoacetamide 5 were found to have 5-HT3 receptor partial agonist activity with(R)-5 having higher potency than (S)-5.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 31566-31-1 help many people in the next few years. Application In Synthesis of Glyceryl monostearate.

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Chemistry is an experimental science, Application In Synthesis of 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 25952-53-8, Name is 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, molecular formula is C8H18ClN3, belongs to quinuclidines compound. In a document, author is Naito, R.

Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists

In the course of continuing efforts to develop potent and bladder-selective muscarinic M-3 receptor antagonists, quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives and related compounds were designed as conformationally restricted analogues of quinuclidin-3-yl benzhydrylcarbamate (8). Binding assays with rat muscarinic receptor subtypes revealed that the quinuclidin-3-yl 1-aryl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives showed high affinities for the M3 receptor, and selectivity for the M3 receptor over the M-2 receptor. Of these derivatives, (+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monohydrochloride (9b) exhibited almost the same inhibitory activity against bladder contraction to that of oxybutynin (1), and more than 10-fold selectivity for bladder contraction versus salivary secretion, demonstrating that 9b may be useful for the treatment of symptoms associated with overactive bladder without having side effects such as dry mouth.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 25952-53-8, in my other articles. Application In Synthesis of 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride.

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Quinuclidine – Wikipedia,
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Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 99-67-2, Name is 2-Allylpent-4-enoic acid, molecular formula is C8H12O2, belongs to quinuclidines compound. In a document, author is Sonar, Vijayakumar N., introduce the new discover, Name: 2-Allylpent-4-enoic acid.

Novel substituted (Z)-2-(N-benzylindol-3-ylmethylene)-quinuclidin-3-one and (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)-quinuclidin-3-ol derivatives as potent thermal sensitizing agents

Use of ionizing radiation is essential for the management of many human cancers, and therapeutic hyperthermia has been identified as a potent radio sensitizer. Radiation therapy combined with adjuvant hyperthermia represents a potential too] to provide outstanding local-regional control for refractory disease. (Z)-(+/-)-2-(N-Benzylindol-3-ylmethylene)quinuclidin-3-oI (2) and (Z)-(+/-)-2-(N-benzenesulfonylindol-3-ylmethylene)quinuclidin-3-ol (4) were initially identified as potent thermal sensitizers that could lower the threshold needed for thermal sensitivity to radiation treatment. To define the structural requirements of the molecule that are essential for thermal sensitization, we have synthesized and evaluated a series of (Z)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-one (9), and (Z)-()-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-oI (10) analogs that incorporate a variety of substituents in both the indole and N-benzyl moieties. These systematic structure-activity relationship (SAR) studies were designed to further the development and optimization of potential clinically useful thermal sensitizing agents. The most potent analog was compound 10 (R-1 = H, R 2 = 4-Cl), which potently inhibited (93% inhibition at 50 mu M) the growth of HT-29 cells after a 41 degrees C/2 h exposure. (c) 2007 Elsevier Ltd. All rights reserved.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 99-67-2. Name: 2-Allylpent-4-enoic acid.

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