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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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Quinuclidine – Wikipedia,
Quinuclidine | C7H65N | ChemSpider

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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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Quinuclidine – Wikipedia,
Quinuclidine | C7H128N | ChemSpider

Archives for Chemistry Experiments of Quinuclidin-3-yl acetate

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Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonists

The insect muscarinic acetylcholine receptor (mAChR) is evaluated as a potential target for insecticide action. The mammalian M2/M4-selective antagonist radioligand [3H]AF-DX 384 (a pirenzepine analogue) binds to Drosophila mAChR at a single high-affinity site identical to that for the nonselective antagonist [3H]quinuclidinyl benzilate (QNB) and with a pharmacological profile distinct from that of all mammalian mAChR subtypes. Three nonselective antagonists (QNB, scopolamine, and atropine) show the highest affinity (Ki = 0.5-2.4 nM) at the Drosophila target, and AF-DX 384 and M3-selective 4-DAMP (dimethyl-4-(diphenylacetoxy)piperidinium iodide) rank next in potency (Ki = 5-18 nM). Eleven muscarinic antagonists generally exhibit higher affinity than eight agonists. On injection into houseflies, the antagonists 4-DAMP and (S)-(+)-dimethindene produce suppressed movement, the agonist (methyloxadiazolyl)quinuclidine causes knockdown and tremors, and all of them inhibit [3H]-QNB binding ex vivo, indicating possible mAChR-mediated intoxication. The insect mAChR warrants continuing study in lead generation to discover novel insecticides.

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Quinuclidine | C7H62N | ChemSpider

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Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonists

The insect muscarinic acetylcholine receptor (mAChR) is evaluated as a potential target for insecticide action. The mammalian M2/M4-selective antagonist radioligand [3H]AF-DX 384 (a pirenzepine analogue) binds to Drosophila mAChR at a single high-affinity site identical to that for the nonselective antagonist [3H]quinuclidinyl benzilate (QNB) and with a pharmacological profile distinct from that of all mammalian mAChR subtypes. Three nonselective antagonists (QNB, scopolamine, and atropine) show the highest affinity (Ki = 0.5-2.4 nM) at the Drosophila target, and AF-DX 384 and M3-selective 4-DAMP (dimethyl-4-(diphenylacetoxy)piperidinium iodide) rank next in potency (Ki = 5-18 nM). Eleven muscarinic antagonists generally exhibit higher affinity than eight agonists. On injection into houseflies, the antagonists 4-DAMP and (S)-(+)-dimethindene produce suppressed movement, the agonist (methyloxadiazolyl)quinuclidine causes knockdown and tremors, and all of them inhibit [3H]-QNB binding ex vivo, indicating possible mAChR-mediated intoxication. The insect mAChR warrants continuing study in lead generation to discover novel insecticides.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H62N | ChemSpider

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Correlation between pKa and reactivity of quinuclidine-based catalysts in the Baylis-Hillman reaction: Discovery of quinuclidine as optimum catalyst leading to substantial enhancement of scope

The reactivity of a variety of quinuclidine-based catalysts in the Baylis-Hillman reaction has been examined, and a straightforward correlation between the basicity of the base and reactivity has been established, without exception. The following order of reactivity was established with pKa’s of the conjugate acids (measured in water) given in parentheses: quinuclidine (11.3), 3-hydroxyquinuclidine (9.9), DABCO (8.7), 3-acetoxyquinuclidine (9.3), 3-chloroquinuclidine (8.9), and quinuclidinone (7.2). The higher than expected reactivity of DABCO, based on its pKa, was analyzed by comparing the relative basicity of DABCO and 3-acetoxyquinuclidine in DMSO. It was found that in aprotic solvent, DABCO was 0.6 pKa units more basic than 3-acetoxyquinuclidine, thus establishing a direct link between pKa of the amine and its reactivity. In contrast to previous literature work that reported the contrary, quinuclidine, which has the highest pKa, was found to be the most active catalyst. The reaction profile with quinuclidine showed significant autocatalysis, which suggested that the presence of proton donors might further enhance rates. Thus, a series of additives bearing polar X-H bonds were investigated and it was found that methanol, triethanolamine, formamide, and water all provided additional acceleration. Methanol was found to be optimum, and the powerful combination of quinuclidine with methanol was tested with a host of aldehydes and Michael acceptors. Not only were the reactions more efficient and faster than previously reported, but now new substrates that were previously unreactive could be employed. Notable examples include the use of acetylenic aldehydes and the employment of vinyl sulfones, acrylamides, delta-lactones, and even alpha,beta-unsaturated esters bearing a beta-substituent.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H45N | ChemSpider

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CEPHALOSPORIN HAVING CATECHOL GROUP

The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H22N | ChemSpider

The important role of (R)-3-Aminoquinuclidine dihydrochloride

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Chiral polyoxometalate-based materials: From design syntheses to functional applications

Owing to the potential applications in catalysis, analytical chemistry, ion exchange, magnetism, biological chemistry and medicine, tremendous effort has been dedicated to exploring polyoxometalate (POM) chemistry. Chiral POM-based materials are particularly attractive due to the combination of the advantage of POMs with the importance of chirality. Nearly 100 chiral POM-based compounds were reported, which were mainly used as asymmetric catalysts, molecular recognition and nonlinear optical materials. In addition, the chirality within POM systems has attracted the attention of theoretical chemists and research was carried out to explore the origin of chirality by density functional theoretical methods. In this review, we summarize the developments of chiral POM-based materials, including their synthetic strategies, calculations on the origin of chirality and the relevant applications.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H144N | ChemSpider

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Primary open angle glaucoma: an overview on medical therapy

The purpose of this review is to discuss the topics relevant to the use of intraocular pressure-lowering strategies, which remains the first line in the management of glaucoma. Estimates of blindness from glaucoma and identification of risk factors remain of interest for all ophthalmologists. New functional tests offer promise for better detection and more accurate diagnosis of glaucoma. We finally discuss the impact of various glaucoma therapies, the principles of monotherapy and fixed combinations, which offer benefits of convenience, cost, and safety.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H87N | ChemSpider

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Visible-Light-Mediated Metal-Free Difunctionalization of Alkenes with CO2 and Silanes or C(sp3)?H Alkanes

Catalytic alkene difunctionalization via Si?H and C?H activations represents an ideal atom- and step-economic pathway for quick assembly of molecular complexity. We herein developed a visible-light-promoted metal-free difunctionalization of alkenes using abundant CO2 and readily available Si?H and C(sp3)?H bonds as feedstocks. Through the merger of photoredox and hydrogen-atom-transfer catalysis, a variety of value-added compounds, such as beta-silacarboxylic acids and acids bearing a gamma-heteroatom (e.g., N, O, S) could be directly accessed from simple alkenes in a redox-neutral fashion.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H63N | ChemSpider

Top Picks: new discover of (R)-3-Aminoquinuclidine dihydrochloride

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5-SUBSTITUTED IMIDAZOLES

Compounds of formula I: wherein A and R1 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 – Wikipedia,
Quinuclidine | C7H102N | ChemSpider