Day: March 16, 2021

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 502-49-8, Name is Cyclooctanone, SMILES is O=C1CCCCCCC1, in an article , author is Shchekotikhin, AE, once mentioned of 502-49-8, Recommanded Product: 502-49-8.

3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione for circumvention of anticancer drug resistance

A series of 3-aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3 -f]indole-5,10-dione was synthesized by Mannich reaction or by the transamination of 3-dimethylaminomethyl 4,11-dihydroxy- or 4,11-dimethoxynaphtho[2,3-f]indole-5,10-dione. The potency of novel derivatives was tested on a National Cancer Institute panel of 60 human tumor cell lines as well as in cells with genetically defined determinants of cytotoxic drug resistance, P-glycoprotein (Pgp) expression, and p53 inactivation. Mannich derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione with an additional amino function in their side chain, demonstrated equal cytotoxicity against the parental K562 leukemia cells and their Pgp-positive subline, whereas the latter showed similar to 7-fold resistance to adriamycin, a Pgp transported drug. 3-(1-Piperazinyl)methyl and 3-(quinuclidin-3-yl)aminomethyl derivatives of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione killed HCT116 colon carcinoma cells (carrying wild type p53) and their p53-null variant within the similar range of concentrations. We conclude that Mannich modification of 4,11-dihydroxynaphtho[2,3-f]indole-5,10-dione, especially when cyclic diamine (e.g., piperazine, quinuclidine) is used, confers an important feature to the resulting compounds, namely, the potency for tumor cells otherwise resistant to a variety of anticancer drugs. (c) 2004 Elsevier Ltd. All rights reserved.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 502-49-8, you can contact me at any time and look forward to more communication. Recommanded Product: 502-49-8.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

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, 110-44-1, Name is Sorbic acid, SMILES is C/C=C/C=C/C(O)=O, belongs to quinuclidines compound. In a document, author is Naito, R, introduce the new discover, Product Details of 110-44-1.

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 proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 110-44-1 is helpful to your research. Product Details of 110-44-1.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

In an article, author is d’Agostino, Simone, once mentioned the application of 3564-73-6, HPLC of Formula: 238.28, Name is 10,11-Dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, molecular formula is C15H14N2O, molecular weight is 238.28, MDL number is MFCD00005072, category is quinuclidines. Now introduce a scientific discovery about this category.

Intriguing Case of Pseudo-Isomorphism between Chiral and Racemic Crystals of rac- and (S)/(R)2-(1,8-Naphthalimido)-2-quinuclidin-3-yl, and Their Reactivity Toward I-2 and 1Br

Condensation reactions between 1,8-naphthalic anhydride and racemic 3-aminoquinuclidine or chiral (S) or (R)-(-)-3-aminoquinuclidine allowed preparation of three novel racemic and enantiopure aza-donor ligands, namely NMiABCO (1), (S)NMiABCO (2a), and (R)NMiABCO (2b). Racemic NMiABCO (1) crystallizes in the monoclinic space group P2(1)/c, Z’ = 1, while enantiopure (S)NMiABCO (2a) and (R)NMiABCO (2b) crystallize in the chiral monoclinic space group P2(1), Z’ = 2, and show significant pseudocentrosymmetry, being pseudo-isomorphous with racemic NMiABCO (1). Reactivity of both racemic and enantiopure NMiABCO toward iodine and interhalogen IBr was also investigated as a way to remove the pseudoisomorphism, yielding the three new molecular adducts [NMiABCO center dot I-2] (3), [(S)NMiABCO center dot I-2]center dot xCHCl(3) (4), [(S)NMiABCO center dot IBr]center dot xCHCl(3) (5) and the molecular salt [HNMIABCO][1Br(2)] (6). Synthesis of complexes 3 and 4 was also carried out in the solid state via kneading and vapor digestion techniques. All compounds were fully characterized via single crystal and powder X-ray diffraction and Raman spectroscopy.

If you are interested in 3564-73-6, you can contact me at any time and look forward to more communication. HPLC of Formula: 238.28.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Synthetic Route of 272778-12-8, 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. 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 Nomoto, F, introduce new discover of the category.

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.

Synthetic Route of 272778-12-8, 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 272778-12-8 is helpful to your research.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Recommanded Product: trans-Retinal, 116-31-4, Name is trans-Retinal, SMILES is O=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C, in an article , author is NILSSON, BM, once mentioned of 116-31-4.

3-HETEROARYL-SUBSTITUTED QUINUCLIDIN-3-OL AND QUINUCLIDIN-2-ENE DERIVATIVES AS MUSCARINIC ANTAGONISTS – SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

A number of 3-heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives have been prepared and evaluated for muscarinic and antimuscarinic properties. The affinities of the new compounds (13, 14, 16-32, and 36-52a,b) were tested in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[H-3]-3-quinuclidinyl benzilate [(-)-[H-3]QNB] as the radioligand and in a functional assay using isolated guinea pig urinary bladder. The present compounds behaved as competitive muscarinic antagonists in the urinary bladder. The highest receptor binding affinity, K-i (cortex) = 9.6 nM, was observed for 3-(2-benzofuranyl)quinuclidin-2-ene (31). The corresponding 3-benzofuranyl (36) and 3-benzothienyl (37) homologues had about 3.5-fold lower affinity for cortical muscarinic receptors. All quinuclidin-3-ol derivatives (14 and 16-25) had lower binding affinities for the different muscarinic receptor subtypes than the corresponding quinuclidin-2-ene analogues when examined in the various tissue homogenates. In general, the new compounds showed low subtype selectivity. The structure-affinity relationships are discussed in terms of differences in proton basicity of the azabicyclic nitrogen and differences in geometric, conformational, and/or electronic properties of the compounds. The cortical antimuscarinic potency is also related to the complementarity of the compounds to the putative binding site of the muscarinic mi receptor.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 116-31-4, you can contact me at any time and look forward to more communication. Recommanded Product: trans-Retinal.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 4457-71-0, Name is 3-Methylpentane-1,5-diol, molecular formula is C6H14O2, belongs to quinuclidines compound, is a common compound. In a patnet, author is Trost, BM, once mentioned the new application about 4457-71-0, COA of Formula: 118.17.

Intramolecular palladium-catalyzed allylic alkylation: Enantio- and diastereoselective synthesis of [2.2.2] bicycles

[GRAPHICS] Pd-catalyzed asymmetric allylic alkylation provides both enantio- and diastereoselectivity in formation of bicyclo [2.2.2] octan-2,3-diones and quinuclidin-2-ones, the latter potential precursors to quinine alkaloids.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 4457-71-0. The above is the message from the blog manager. COA of Formula: 118.17.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

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 Huang, Mei, once mentioned the application of 22767-49-3, Name is Sodium pentane-1-sulfonate, molecular formula is C5H11NaO3S, molecular weight is 174.19, MDL number is MFCD00007541, category is quinuclidines. Now introduce a scientific discovery about this category, Name: Sodium pentane-1-sulfonate.

The novel alpha 7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens

Background Alpha7 and alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR) agonists have been shown to improve cognition in various animal models of cognitive impairment and are of interest as treatments for schizophrenia, Alzheimer’s disease, and other cognitive disorders. Increased release of dopamine (DA), acetylcholine (ACh), glutamate (Glu), and gamma-aminobutyric acid (GABA) in cerebral cortex, hippocampus, and nucleus accumbens (NAC) has been suggested to contribute to their beneficial effects on cognition. Results Using in vivo microdialysis, we found that EVP-6124 [(R)-7-chloro-N-quinuclidin-3-yl) benzo[b] thiophene-2-carboxamide], a high-affinity alpha 7 nAChR partial agonist, at 0.1 mg/kg, s.c., increased DA efflux in the medial prefrontal cortex (mPFC) and NAC. EVP-6124, 0.1 and 0.3 mg/kg, also increased efflux of ACh in the mPFC but not in the NAC. Similarly, EVP-6124, 0.1 mg/kg, but not 0.03 and 0.3 mg/kg, significantly increased mPFC Glu efflux. Thus, EVP-6124 produced an inverted U-shaped curve for DA and Glu release, as previously reported for other alpha 7 nAChR agonists. The three doses of EVP-6124 did not produce a significant effect on GABA efflux in either region. Pretreatment with the selective alpha 7 nAChR antagonist, methyllycaconitine (MLA, 1.0 mg/kg), significantly blocked cortical DA and Glu efflux induced by EVP-6124 (0.1 mg/kg), suggesting that the effects of EVP-6124 on these neurotransmitters were due to alpha 7 nAChR agonism. MLA only partially blocked the effects of EVP-6124 on ACh efflux in the mPFC. Conclusion These results suggest increased cortical DA, ACh, and Glu release, which may contribute to the ability of the alpha 7 nAChR agonist, EVP-6124, to treat cognitive impairment and possibly other dimensions of psychopathology.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 22767-49-3, Name: Sodium pentane-1-sulfonate.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Synthetic Route of 97-65-4, 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. 97-65-4, Name is Propylenedicarboxylic acid, SMILES is O=C(O)C(CC(O)=O)=C, belongs to quinuclidines compound. In a article, author is Brossat, Maude, introduce new discover of the category.

Simple one-pot process for the bioresolution of tertiary amino ester protic ionic liquids using subtilisin

An efficient hydrolase-catalyzed bioresolution of tertiary amino ester protic ionic liquids has been demonstrated. Protic ionic liquids have been prepared in one step from the corresponding tertiary amino alcohols by treatment with butyric anhydride. After bioresolution, unreacted esters can be easily separated from the corresponding alcohols by extraction with hexane Bioresolution of quinuclidin-3-yl butyrate has been performed with excellent selectivity. (C) 2009 Elsevier Ltd. All rights reserved.

Synthetic Route of 97-65-4, 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 97-65-4.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

143-18-0, Name is Potassium oleate, molecular formula is C18H33KO2, Quality Control of Potassium oleate, belongs to quinuclidines compound, is a common compound. In a patnet, author is Del Bello, Fabio, once mentioned the new application about 143-18-0.

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments

To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3-5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M-1-M-5). Stereochemistry and the nature of the linker between the quinuclidine moiety and the 1,4-dioxane nucleus play an important role on the affinities of the compounds. The presence of an ether bridge confers higher affinities for all mAChR subtypes to the ligand. Interestingly, the ether enantiomer (R,S)-5 shows the highest affinity at all mAChR subtypes with K-p(i) values similar to that of solifenacin at M-3 and higher at the other subtypes. Unlike solifenacin, it shows a preference for M-1 mAChR subtype with respect to the other subtypes. This compound, lacking a permanent positive charge on the nitrogen atom, can be a useful tool for the pharmacological study of mAChRs in the central nervous system. (C) 2017 Elsevier Masson SAS. All rights reserved.

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 143-18-0 help many people in the next few years. Quality Control of Potassium oleate.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

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 Ford, Benjamin M., once mentioned the application of 584-02-1, Name is 3-Pentanol, molecular formula is C5H12O, molecular weight is 88.1482, MDL number is MFCD00004574, category is quinuclidines. Now introduce a scientific discovery about this category, COA of Formula: 88.1482.

Reduced Tolerance and Asymmetrical Crosstolerance to Effects of the Indole Quinuclidinone Analog PNR-4-20, a G Protein-Biased Cannabinoid 1 Receptor Agonist in Mice: Comparisons with Delta(9)-Tetrahydrocannabinol and JWH-018

Most cannabinoid 1 receptor (CB1R) agonists will signal through both G protein-dependent and -independent pathways in an unbiased manner. Recruitment of beta-arrestin 2 desensitizes and internalizes receptors, producing tolerance that limits therapeutic utility of cannabinoids for chronic conditions. We developed the indole quinuclidinone (IQD) analog (Z)-2-((1-(4-fluorobenzyl)1H-indol-3-yl)nnethylene)quinuclidin-3-one (PNR-4-20) as a novel G protein-biased agonist at CB(1)Rs, and the present studies determine if repeated administration of PNR-4-20 produces lesser tolerance to in vivo effects compared with unbiased CB1R agonists, Delta(9)-tetrahydrocannabinol (Delta(9)-THC) and 1-pentyl-3-(1-naphthoyl)indole (JWH-018). Adult male National Institutes of Health Swiss mice were administered comparable doses of PNR-4-20 (100 mg/kg), Delta(9)-THC (30 mg/kg), or JWH-018 (3 mg/kg) once per day for five consecutive days to determine tolerance development to hypothermic, antinociceptive, and cataleptic effects. Persistence of tolerance was then determined after a drug abstinence period. We found that unbiased CB1R agonists Delta(9)-THC and JWH-018 produced similar tolerance to these effects, but lesser tolerance was observed with PNR-4-20 for hypothermic and cataleptic effects. Tolerance to the effects of PNR-4-20 completely recovered after drug abstinence, while residual tolerance was always observed with unbiased CB1R agonists. Repeated treatment with PNR-4-20 and Delta(9)-THC produced asymmetric cross-tolerance to hypothermic effects. Importantly, binding studies suggest PNR-4-20 produced significantly less down-regulation of CB(1)Rs relative to Delta(9)-THC in hypothalamus and thalamus of chronically treated mice. These studies suggest that the G protein-biased CB1R agonist PNR-4-20 produces significantly less tolerance than unbiased cannabinoid agonists, and that the IQD analogs should be investigated further as a novel molecular scaffold for development of new therapeutics.

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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider