Day: March 29, 2021

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. HPLC of Formula: C5H10O, 630-19-3, Name is Pivalaldehyde, SMILES is CC(C)(C)C=O, in an article , author is Nagashima, Shinya, once mentioned of 630-19-3.

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.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 630-19-3, you can contact me at any time and look forward to more communication. HPLC of Formula: C5H10O.

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

In an article, author is Ugawa, T, once mentioned the application of 765-70-8, Formula: C6H8O2, 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.

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.

If you are interested in 765-70-8, you can contact me at any time and look forward to more communication. Formula: C6H8O2.

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

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 4771-80-6, Name is Cyclohex-3-enecarboxylic acid, molecular formula is , belongs to quinuclidines compound. In a document, author is Venkateswaran, Amudhan, COA of Formula: C7H10O2.

Antiangiogenic properties of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol/one analogs and their derivatives

In the past half century research efforts have defined a critical role for angiogenesis in tumor growth and metastasis. We previously reported that inhibition of a novel target, ENOX1, by a (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ol, suppressed tumor angiogenesis. The present study was undertaken in order to establish structure-activity relationships for quinuclidine analogs. The angiogenesis inhibiting activity of a series of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ols (1a-1k), (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ones (2a-2h), (Z)-(+/-)-2-(1H/N-methyl-indol-3-ylmethylene) quinuclidin-3-ols (3a-3b), and substituted (Z)-(+/-)-2-(N-benzenesulfonylindol-3-yl-methylene) quinuclidin-3-ols and their derivatives (4a-4d) that incorporate a variety of substituents in both the indole and N-benzyl moieties was evaluated using Human Umbilical Vein Endothelial Cells (HUVECs) subjected to in vitro cell migration scratch assays, tubule formation in Matrigel, cell viability and proliferation assays. In total, 25 different analogs were evaluated. Based on in vitro cell migration scratch assays, eight analogs were identified as potent angiogenesis inhibitors at 10 mu M, a concentration that was determined to be nontoxic by colony formation assay. In addition, this approach identified a potent antiangiogenic ENOX1 inhibitor, analog 4b. (C) 2010 Elsevier Ltd. All rights reserved.

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 4771-80-6, in my other articles. COA of Formula: C7H10O2.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 253168-94-4, Name is 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine, SMILES is O=S(CC(N)C1=CC=C(OC)C(OCC)=C1)(C)=O, belongs to quinuclidines compound. In a document, author is Ugawa, T, introduce the new discover, SDS of cas: 253168-94-4.

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. 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 253168-94-4 is helpful to your research. SDS of cas: 253168-94-4.

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. 3564-73-6, Name is 10,11-Dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, SMILES is O=C(N1C2=CC=CC=C2CCC3=CC=CC=C31)N, in an article , author is Klimova, EI, once mentioned of 3564-73-6, HPLC of Formula: C15H14N2O.

Stereospecific formation of polycyclic ferrocenyldihydropyrazoles based on Z- and E-isomeric ferrocenyl- substituted alpha,beta-unsaturated ketones of the heterocyclic series

The reactions of E- and Z-isomeric 2-(ferrocenylmethylidene)quinuclidin-3-one, 1-methyl-3-(ferrocenylmethylidene)piperidin-4-one, and 2-(ferrocenylmethylidene)tropinone with hydrazine proceed stereospecifically to form the same diastereomeric polycyclic ferrocenyldihydropyrazoles regardless of the geometrical configuration of the starting alpha,beta -unsaturated ketones. The structure of the trans-diastereomer of 4-acetyl-3-ferrocenyl-1,4,5-triazatricyclo[5.2.2.0(2,6)]undec-5-ene was established by X-ray diffraction analysis.

Interested yet? Read on for other articles about 3564-73-6, you can contact me at any time and look forward to more communication. HPLC of Formula: C15H14N2O.

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

Application of 5392-40-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 5392-40-5, Name is 3,7-Dimethylocta-2,6-dienal, SMILES is C/C(C)=CCC/C(C)=C/C=O, belongs to quinuclidines compound. In a article, author is Primozic, Ines, introduce new discover of the category.

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)

Application of 5392-40-5, 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 5392-40-5 is helpful to your research.

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

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 31906-04-4, Name is 4-(4-Hydroxy-4-methylpentyl)cyclohex-3-enecarbaldehyde. In a document, author is Ishihara, T, introducing its new discovery. Safety of 4-(4-Hydroxy-4-methylpentyl)cyclohex-3-enecarbaldehyde.

Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: Enzyme inhibition and effects on plasma lipid levels

Squalene synthase (E.C. 2.5.1.21) is a microsomal enzyme which catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene, and is involved in the first committed step in cholesterol biosynthesis. It is an attractive target for hypocholesterolemic and hypotriglyceridemic strategies. We synthesized a series of 3-ethylidenequinuclidine derivatives, and evaluated their ability to inhibit squalene synthase in vitro and to lower non-HDL cholesterol levels in hamsters. 3-Ethylidene-quinuclidine derivatives incorporating an unsubstituted 9H-carbazole moiety reduced plasma non-HDL cholesterol levels and did not affect plasma transaminase levels, indicating a lack of hepatotoxicity. Among the novel Compounds, (Z)-2-[2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 8 (YM-53579) and (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 28 (YM-53601) were potent inhibitors of squalene synthase derived from human hepatoma cells, with IC50 Values Of 160 and 79 nM. respectively. They also reduced plasma non-HDL cholesterol levels in hamsters by approximately 50 and 70%, respectively. at all oral dose of 50 mg/kg/day for 5 days. (C) 2003 Elsevier Ltd. 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 31906-04-4 help many people in the next few years. Safety of 4-(4-Hydroxy-4-methylpentyl)cyclohex-3-enecarbaldehyde.

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

Related Products of 123-96-6, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 123-96-6, Name is Octan-2-ol, SMILES is CC(O)CCCCCC, belongs to quinuclidines compound. In a article, author is BESIDSKY, Y, introduce new discover of the category.

SYNTHESIS AND REACTIVITY OF 6-CARBAMOYL-5-PHENYL-2,3,5,6-TETRAHYDRO-1H-1,4-ETHANOBENZO[F]QUINOLINE – X-RAY MOLECULAR-STRUCTURE OF (4AR-ASTERISK,5S-ASTERISK,6R-ASTERISK,10BR-ASTERISK)-5-PHENYL-2,3,4A,5,6,10B-HEXAHYDRO-1H-1,4-ETHANOBENZO[F]QUINOLIN-6-YL ACETATE

Cyclocondensation of 2-(2-cyano-1,2-diphenylethyl)quinuclidin-3-one 1 in the presence of sulfuric acid gave an intramolecular phenylation instead of lactam formation. The cyclic product was hydrogenated to give 6-carbamoyl-5-phenyl-2,3,4a,5,6,10b-hexahydro-1H-1,4-ethanobenzo- [f]quinoline. On treatment with LiAIH(4) the carbamoyl group was stereospecifically replaced by a hydroxy group. The alcohol was acetylated and the structure was confirmed by X-ray crystallography. The hydroxylation reaction is believed to proceed via a carbonitrile intermediate. In the presence of air the nitrile can be converted to a ketone which is then reduced to the alcohol with an overall retention of configuration.

Related Products of 123-96-6, 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.I hope my blog about 123-96-6 is helpful to your research.

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

In an article, author is Shchekotikhin, AE, once mentioned the application of 3159-07-7, Safety of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine, Name is 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine, molecular formula is C13H9NOS, molecular weight is 227.2817, MDL number is MFCD00901197, category is quinuclidines. Now introduce a scientific discovery about this category.

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.

If you are interested in 3159-07-7, you can contact me at any time and look forward to more communication. Safety of 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine.

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

Application of 112-92-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 112-92-5, Name is 1-Hydroxyoctadecane, SMILES is CCCCCCCCCCCCCCCCCCO, belongs to quinuclidines compound. In a article, author is Sonar, Vijayakumar N., introduce new discover of the category.

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.

Application of 112-92-5, 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 112-92-5.

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