Heterocyclic Building Blocks-Quinuclidine

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. Formula: C7H16Cl2N2, C7H16Cl2N2. A document type is Article, introducing its new discovery., Formula: C7H16Cl2N2

Synthesis, crystal structures, second harmonic generation response and temperature phase transitions of two noncentrosymmetric Cu(II)-hybrid halides compounds: [(R)-C7H16N2][CuX4] (X = Cl or Br)

(R)-(+)-3-aminoquinuclidine was used in the synthesis of [(R)-C7H16N2][CuCl4] (1) and [(R)-C7H16N2][CuBr4] (2), which both contain similar [CuX4]2- anions (X = Cl or Br). The structures of the two compounds were determined using single-crystal X-ray diffraction. The use of enantiomerically pure sources of (R)-C7H14N2 forces crystallographic noncentrosymmetry. These materials crystallize in the chiral space group P212121 (No. 19), which exhibits the enantiomorphic crystal class 222 (D2). In the molecular arrangement, the [CuX4]2- anions are linked to the organic cations through N?H ? X and C?H ? X hydrogen bonds to form cation-anion-cation molecular units, which are held together by means of offset face-to-face interactions giving a three-dimensional network. Thermal stability of the crystals was ascertained by TG measurement. Compounds (1) and (2) display several phases transition with higher transition temperature at T = 100 C. The Kurtz and Perry powder method using Nd:YAG laser shows that their second harmonic generation (SHG) efficiencies are about 0.81 and 0.82 times as large as that of KH2PO4 (KDP), respectively. Such a chiral hybrid metal halides skeleton could provide a new platform for future engineering in the areas including information storage, light modulators and optoelectronic functionalities.

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Quinuclidine | C7H145N | ChemSpider

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Compounds

Compounds of formula I: 1 wherein A, D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Quinuclidine | C7H101N | ChemSpider

Electric Literature of 827-61-2, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. Electric Literature of 827-61-2, C9H15NO2. A document type is Article, introducing its new discovery.

95. Inductive Charge Dispersal in Quinuclidinium Ions. Polar Effects, Part 13

Inductive charge dispersal to the alpha-, beta-, and gamma-positions of the solvated quinuclidinium ion has been examined by comparing the pKa and the derived inductivities rho1 of several 2-, 3- and 4-substituted quinuclidinium perchlorates 4, 5, and 6, respectively.The same inductivity is observed at the practically equidistant beta- and gamma-positions.It, therefore, appears that polar substituent effects are transmitted directly through the molecule.As expected, inductivity is considerably higher at the alpha-positions where through-bond and direct induction coincide.The fact that the pKa of all three series of salts correlate linearly with each other points to the common nature of these inductive electron displacements.

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Quinuclidine | C7H59N | ChemSpider

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about Recommanded Product: (R)-3-Aminoquinuclidine dihydrochloride, molcular formula is C7H16Cl2N2, introducing its new discovery. , Recommanded Product: (R)-3-Aminoquinuclidine dihydrochloride

Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease

The invention provides compounds of Formula I: 1wherein W0 is a bicyclic moiety and is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which alpha7 is known to be involved.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, HPLC of Formula: C9H15NO2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2

Design, Synthesis, and Neurochemical Evaluation of 5-(3-Alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 Muscarinic Receptor Agonists

A series of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines (7a-h) was synthesized for biological evaluation as selective agonists for M1 receptors coupled to phosphoinositide (PI) metabolism in the central nervous system.Each ligand bound with high affinity to muscarinic receptors from rat brain as measured by inhibition of <3H>-(R)-quinuclidinyl benzilate (<3H>-(R)-QNB) binding. 5-(3-Methyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine trifluoroacetate (CDD-0098-J; 7a)displayed high affinity (IC50 = 2.7 +/- 0.69 muM) and efficacy at muscarinic receptors coupled to PI metabolism in the rat cortex and hippocampus .Increasing the length of the alkyl substituent increased affinity for muscarinic receptors yet decreased activity in PI turnover assays.The hippocampal PI response of 7a was blocked by lower concentrations of pirenzepine (8) or by higher concentrations of either AF-DX 116 (9) or p-fluorohexahydrosiladifenidol (10), suggesting that a low concentrations 7a selectively stimulates PI turnover through M1 receptors.

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Quinuclidine | C7H53N | ChemSpider

Reference of 123536-14-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article£¬once mentioned of 123536-14-1

Discovery of fused heterocyclic carboxamide derivatives as novel alpha7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation

The alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) has emerged as a promising therapeutic target for schizophrenia. In our previous work, a novel series of alpha7-nAChR agonists bearing scaffold of indolizine were discovered. To explore the effect of aromaticity on the activity and find more active agents, herein, fused heterocyclic carboxamide derivatives were designed and synthesized in this study. Based on the evaluation by two-electrode voltage clamp in Xenopus oocytes, 27 of the synthesized compounds showed obvious agonism of alpha7 nAChR. Particularly, compounds 10a and 10e showed significantly higher Emax than EVP-6124. The result illustrated the importance of aromaticity to the activity of agonism. Compound 10a, which showed EC50 of 1.88 muM and Emax of 72.4%, was further characterized comprehensively, including co-application with type II positive allosteric modulator PNU-120596, selectivity with other closely related ligand-gated ion channel, etc. The results showed that 10a showed moderate selectivity over other subtypes such as alpha4beta2 and alpha3beta4 nAChR. 10a evoked alpha7-like currents that were inhibited by MLA and enhanced in the presence of the alpha7 PAM PNU-120596. The analysis of binding mode and understanding of structure-activity relationship provided insights to develop more potent novel alpha7-nAChR agonists.

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Quinuclidine | C7H158N | ChemSpider

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Novel potent 5-HT3 receptor ligands based on the pyrrolidone structure: Synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities

Novel conformationally constrained derivatives of classical 5-HT3 receptor antagonists were designed and synthesized with the aim of probing the central 5-HT3 receptor recognition site in a systematic way. The newly-synthesized compounds were tested for their potential ability to inhibit [3H]granisetron specific binding to 5-HT3 receptor in rat cortical membranes. These studies revealed subnanomolar affinity in some of the compounds under study. The most potent ligand in this series was found to be quinuclidine derivative (S)-7i, which showed an affinity comparable with that of the reference ligand granisetron. The potential 5-HT3 agonist/antagonist activity of some selected compounds was assessed in vitro on the 5-HT3 receptor-dependent [14C]guanidinium uptake in NG 108-15 cells. Both of the tropane derivatives tested in this functional assay (7a and 9a) showed antagonist properties, while the quinuclidine derivatives studied [the enantiomers of compounds 7i, 8g, and 9g, and compound (R)-8h] showed a full range of intrinsic efficacies. Therefore, the functional behavior of these 5-HT3 receptor ligands appears to be affected by the structural features of both the azabicyclo moiety and the heteroaromatic portion. In agreement with the data obtained on NG 108-15 cells, investigations on the 5-HT3 receptor-dependent Bezold-Jarisch reflex in urethane-anaesthetized rats confirmed the 5-HT3 receptor antagonist properties of compounds 7a and (S)-7i showing for these compounds ID50 values of 2.8 and 181 mug/kg, respectively. Finally, compounds 7a, (S)-7i and 9a (at the doses of 0.01, 1.0, and 0.01 mg/kg ip, respectively) prevented scopolamine-induced amnesia in the mouse passive avoidance test suggestive of a potential usefulness in cognitive disorders for these compounds. Qualitative and quantitative structure-affinity relationship studies were carried out by means of theoretical descriptors derived on a single structure and ad-hoc defined size and shape descriptors (indirect approach). The results showed to be useful in capturing information relevant to ligand-receptor interaction. Additional information derived by the analysis of the energy minimized 3-D structures of the ligand-receptor complexes (direct approach) suggested interesting mechanistic and methodological considerations on the binding mode multiplicity at the 5-HT3 receptors and on the degree of tolerance allowed in the alignment of molecules for the indirect approach, respectively.

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2 SUBSTITUTED CEPHEM COMPOUNDS

The compounds of formula (I) of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.

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Quinuclidine | C7H19N | ChemSpider

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, Product Details of 123536-14-1, molcular formula is C7H16Cl2N2, introducing its new discovery. Product Details of 123536-14-1

Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof

The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the alpha7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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Related Products of 827-61-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a Review£¬once mentioned of 827-61-2

Drug release from porous matrixes based on natural polymers

Background: This review provides a report on recent advances in the field of drug release from matrixes made of natural polymers. Herein, the properties of natural polymers such as proteins and polysaccharides are discussed in general. Selected detailed examples of drug release profiles from biopolymer matrixes have also been collected from scientific literature and practical work, and commented on. In this review, the most common natural polymers, i.e. collagen, elastin, chitosan, hyaluronic acid and sodium alginate have been discussed as biopolymers that can be potentially applied in drug delivery systems. Methodology: The most rapidly developing field of the biomaterials science is the one dealing with their application as matrixes in drug release systems. Such systems show numerous advantages when compared to conventional ones. They improve medical treatment efficiency due to the fact that drugs are placed directly into the infected part. Moreover, the drug release systems reduce toxic reactions because the drug does not pass through the body and, as a result, does not affect the healthy tissues. Such systems also improve the patient?s comfort during the treatment. Result: Biocompatibility, bioresorbability and non-toxicity are the significant properties characteristic for natural polymers. Natural polymers can be used to obtain biomaterials which can further find their applications in the production of bones or soft tissues implants as well as dressing materials placed on damaged skin. Nevertheless, the disadvantages of biomaterials made of natural polymers, e.g., high solubility and low thermal stability, limit the range of their potential applications. Therefore, it is necessary to modify material properties by carrying out the cross-linking process. Conclusion: Recently, a rapidly growing interest in the use of porous materials as controlled drug delivery matrixes has been observed since they present several positive features. The drug release from polymeric matrixes is based on the carrier degradation process which depends on dissolving and diffusion processes. The selection of a polymeric matrix depends on its compatibility with the drug as well as the manufacturing process which needs to be considered. The proper adjustment of the drug release rate is necessary to obtain the best results during medical treatment. Numerous classes of hydrophilic as well as hydrophobic drugs can be released from polymeric matrixes which is beneficial to medical treatment. The research of different drug release systems has already been carried out, and the results can be found in scientific literature.

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