- Liposome Enhanced Detection of Amyloid Protein Aggregates
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Thioflavin-T is used to image amyloid aggregates because of the excellent turn-on fluorescence properties, but binding affinities are low. By mounting multiple dye units on the surface of a vesicle, the binding affinity for α-synuclein fibrils is increased by three orders of magnitude, and the optical response is increased. Cooperative interactions of the dye headgroup and lipid with the protein provide a general strategy for the construction of multivalent amyloid probes based on vesicles.
- Kocsis, Istvan,Sanna, Elena,Hunter, Christopher A.
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p. 647 - 650
(2021/02/06)
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- N4 - hydroxycytidine derivative as well as preparation method and application thereof
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The invention relates to N4 - hydroxycytidine derivatives as shown in general formula I. A pharmaceutically acceptable salt, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof, and the substituted N4 - hydroxycytidine derivative structure of the structure of Formula I. The pharmaceutical composition is used for preparing medicaments for treating infections such as SARS-CoV, HBV, HCV, H1N1, Ebola and SARS-CoV - 2, can effectively inhibit influenza viruses and SARS-CoV - 2 viruses, and can have the same result on other RNA viruses. The series of compounds can be applied to preparation of anti RNA virus drugs. The medicine is used for preparing a medicine for treating virus infection and is used for preparing a vaccine adjuvant for treating virus infection.
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Paragraph 0089-0093
(2021/09/01)
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- Polycyclic pyridinone compounds and pharmaceutical compositions and uses thereof
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The invention discloses a polycyclic pyridone compound as well as a pharmaceutical composition and application thereof, and the polycyclic pyridone compound is shown as a formula (I). The compound can be used for preparing anti-virus infection drugs.
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Paragraph 0181-0186
(2021/11/06)
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- An N4-hydroxycytoside derivative and its preparation method and use
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The present invention provides an N4- hydroxycytidine derivative as shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof: 。 The compounds of the present invention have the following significant advantages: (1) the N4-hydroxycytidine compounds and their derivatives have a highly efficient inhibitory activity of RNA-dependent RNA polymerases of RNA viruses; (2) the N4-hydroxycytoside compounds and their derivatives and pharmaceutical compositions are widely used, can be prepared to treat / prevent SARS-CoV, HBV, HCV, H1N1, Ebola or SARS-CoV-2 virus infection disease drugs.
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Paragraph 0080-0084
(2021/12/07)
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- Preparation method of higher fatty alcohol 2-alkoxy ethanol
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The invention provides a preparation method of higher fatty alcohol 2-alkoxy ethanol, and relates to the technical field of organic synthesis, higher fatty alcohol and sulfonyl halide are used as raw materials for cascade reaction, the higher fatty alcohol is completely converted into sulfonate under the action of alkali, and then the sulfonate is subjected to phase transfer reaction under the promotion of a phase transfer catalyst (the used phase transfer catalyst comprises quaternary ammonium salt or crown ether), sulfonate directly performs nucleophilic substitution reaction with ethylene glycol, and the reaction temperature is controlled to complete the reaction within half an hour to obtain the corresponding higher fatty alcohol 2-alkoxy ethanol. The method is low in raw material and reagent cost, simple in process operation, small in pollution, high in product yield and purity, and suitable for large-scale preparation.
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Paragraph 0030; 0043; 0045-0048
(2021/08/25)
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- Anion-Selective Cholesterol Decorated Macrocyclic Transmembrane Ion Carriers
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Anion transporters play a vital role in cellular processes and their dysregulation leads to a range of diseases such as cystic fibrosis, Bartter's syndrome and epilepsy. Synthetic chloride transporters are known to induce apoptosis in cancer cell lines. Herein, we report triamide macrocycles that are easily synthesized and externally functionalized by pendant membrane-permeable groups. Among a variety of chains appended onto the macrocycle scaffold, cholesterol is found to be the best with an EC50 value of 0.44 μM. The macrocycle is highly anion-selective and transports ions via an OH-/X- antiport mechanism. The macrocycle is an interesting scaffold for ion-Transport as it is able to discriminate between various anions and shows a preference for SCN- and Cl-. Such anion-selective transporters are highly attractive model systems to study ion-Transport mechanisms and could potentially be of high therapeutic value.
- Behera, Harekrushna,Madhavan, Nandita
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p. 12919 - 12922
(2017/09/26)
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- Containing polyoxyethylene ether hydroxy propyl aniline [...] permanaganate betaine and its preparation method
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The invention relates to polyoxyethylene-ether-containing hydroxypropyl anilino carboxylate betaine and a preparation method thereof, and mainly solves the problems in the prior art that an oil-displacement agent containing a surfactant is bad in oil displacement effect and high in use concentration under the oil reservoir conditions of high temperature and high salinity, and alkalis in alkali-surfactant-polymer flooding pollute and damage stratum and oil wells and severely corrode equipment and conveying pipelines. The polyoxyethylene-ether-containing hydroxypropyl anilino carboxylate betaine has the molecular general formula (I) shown in the specification, and in the formula (I), R1 is any one of C15-C39 alkyl and alkenyl, n is 1-10, R2 is any one of C1-C4 alkylidene and hydroxyl-substituted alkylidene. The technical scheme relatively well solves the problems and is applicable to tertiary oil recovery of oil fields.
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Paragraph 0027; 0029
(2017/05/16)
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- Lipophilic amines as potent inhibitors of N-acylethanolamine-hydrolyzing acid amidase
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N-Acylethanolamines (NAEs) including N-arachidonoylethanolamine (anandamide) and N-palmitoylethanolamine are endogenous lipid mediators. These molecules are degraded to the corresponding fatty acids and ethanolamine by fatty acid amide hydrolase (FAAH) or NAE-hydrolyzing acid amidase (NAAA). Lipophilic amines, especially pentadecylamine (2c) and tridecyl 2-aminoacetate (11b), were found to exhibit potent NAAA inhibitory activities (IC50 = 5.7 and 11.8 μM), with much weaker effects on FAAH. These simple structures would provide a scaffold for further improvement in NAAA inhibitory activity.
- Yamano, Yumiko,Tsuboi, Kazuhito,Hozaki, Yuki,Takahashi, Kiyohiro,Jin, Xing-Hua,Ueda, Natsuo,Wada, Akimori
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experimental part
p. 3658 - 3665
(2012/07/28)
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- Synthesis of fulleropyrrolidine-imidazolium salt hybrids and their solubility in various organic solvents
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Eight types of fulleropyrrolidine-imidazolium hybrids have been synthesized and their solubility determined in various types of organic solvents. The solvent solubility of fullerene derivatives depends on the alky side chain on the imidazolium ring; modification of solvent solubility of the fulleropyrrolidine-imidazolium hybrids has thus been accomplished by introduction of an appropriate alkyl group using imidazoyl moiety as the 'functional group connector'. The imidazolium group seems to act not only as the connector but also as an important functional group that controls the solubility.
- Itoh, Toshiyuki,Mishiro, Makoto,Matsumoto, Kei,Hayase, Shuichi,Kawatsura, Motoi,Morimoto, Minoru
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p. 1823 - 1828
(2008/09/18)
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- Combinatorial synthesis of PEG oligomer libraries
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A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
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Page/Page column 9
(2010/02/15)
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- Synthesis and trichomonacidal activity of perketals and hydroperoxides
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Some perketals were synthesized by the Dussault procedure using simple bromides and 2-methoxyprop-2-yl hydroperoxide. Treatment with acetic acid gave the corresponding hydroperoxides. Both perketals and hydroperoxides were tested in vitro as trichomonacid
- Cointeaux,Berrien,Camuzat-Dedenis,Peyrou,Provot,Bories,Loiseau,Mayrargue
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p. 457 - 462
(2007/10/03)
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- Anchor dependency for non-glycerol based cationic lipofectins: Mixed bag of regular and anomalous transfection profiles
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Although detailed structure-activity, physicochemical and biophysical investigations in probing the anchor influence in liposomal gene delivery have been reported for glycerol-based transfection lipids, the corresponding investigation for non-glycerol based simple monocationic transfection lipids have not yet been undertaken. Towards this end, herein, we delineate our structure-activity and physicochemical approach in deciphering the anchor dependency in liposomal gene delivery using fifteen new structural analogues (lipids 1-15) of recently reported non-glycerol based monocationic transfection lipids. The C14 analogues in both series 1 (lipids 1-6) and series 2 (lipids 7-15) showed maximum efficiency in transfecting COS-1 and CHO cells. However, the C12 analogue of the ether series (lipid 3) exhibited a seemingly anomalous behavior compared with its transfection efficient C10 and C14 analogues (lipids 2 and 4) in being completely inefficient to transfect both COS-1 and CHO cells. The present structure-activity investigation also convincingly demonstrates that enhancement of transfection efficiencies through incorporation of membrane re-organizing unsaturation elements in the hydrophobic anchor of cationic lipids is not universal but cell dependent. The strength of the interaction of lipids 1-15 with DNA was assessed by their ability to exclude ethidium bromide bound to the DNA. Cationic lipids with long hydrophobic tails were found, in general, to be efficient in excluding EtBr from DNA. Gel to liquid crystalline transition temperatures of the lipids was measured by fluorescence anisotropy measurement technique. In general (lipid 2 being an exception), transfection efficient lipids were found to have their mid transition temperatures at or below physiological temperatures (37°C).
- Singh, Rajkumar Sunil,Mukherjee, Koushik,Banerjee, Rajkumar,Chaudhuri, Arabinda,Hait, Samik Kumar,Moulik, Satya Priya,Ramadas, Yerramsetti,Vijayalakshmi, Amash,Rao, Nalam Madhusudhana
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p. 900 - 909
(2007/10/03)
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- Quaternary amine containing ether or ester lipid derivatives and therapeutic compositions
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Quaternary amine-containing ether lipid analogs of the formula are disclosed. R1 represents a hydrophobic group and R2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.
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- 2-picolylamine derivatives
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The present invention relates to novel 2-picolylamine derivatives of general formula I STR1 wherein R1 represents an alkyl or phenylalkyl radical; R2 is hydrogen, C1 -C4 acyl or C1 -C4 alko
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- Microencapsulated agriculturally active material
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Agriculturally active materials, such as pesticides, herbicides and the like and a process for microencapsulating said material. The present invention includes trifluralin having a polymorphic form characterized by a yellow color and a melting point of approximately 41°-43° C. The present invention also includes a method using the yellow polymorphic form of trifluralin as a herbicide. In addition, the present invention includes a method of microencapsulating low-melting agriculturally active materials, such as trifluralin. The microencapsulation process comprises the steps of heating a low-melting, water-immiscible, agriculturally active material to a molten state. The molten active material is then combined with an aqueous solution of a water-soluble, film-forming polymer at a temperature sufficient to maintain the active material in its molten state. The active material is then dispersed or emulsified in the aqueous solution so that the active material has a primary particle size of between approximately 0.1 and 10 microns. The resulting dispersion or emulsion is then spray dried at a temperature between approximately 50° and 220° C. so as to microencapsulate the active material in the polymer. Compounds for promoting the rapid solidification of the active material are also disclosed.
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- Mutarotation of Glucose Derivatives in Solutions of Surfactans in Organic Solvents: Co-operativity and Bimodal Catalytic Behaviour
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The mutarotation of glucose, 2,3,4,6-tetra-O-methylglucose, 3-O-hexyl-, 3-O-dodecyl-, 4,6-O-butylidene, 4,6-O-hexylidene, and 4,6-O-decylidene-glucose has been studied kinetically in aqueous solution and in the following surfactant-solvent systems: AOT-heptane, AOT-CHCl3, CPC-CHCl3, CTAC-CHCl3, CPS-CHCl3 and C16E6-tetradecane.Below a low critical surfactant concentration, mutarotation is undetectably slow, but above it the rate increases, usually in a sigmoidal fashion reaching a maximum value at concentrations above ca. 40 mmol l-1.Maximum rates are usually less than those observed in water except for AOT-containing systems which often, but not always, give higher rates.The dependence of rate on surfactant concentration does not in general fit the pseudophase model of micellar catalysis, but can be treated using Piszkiewicz's co-operativity model.This indicates in a number of cases bimodal catalytic behaviour, a non-co-operative mode at concentrations just above the critical level, and a co-operative mode giving more efficient catalysis at higher concentrations.For AOT-heptane the bimodal pattern is reversed and evidence is presented that the co-operative effects observed at low surfactant concentrations propbably represent catalysis in premicellar aggregates.N.m.r. spectroscopic stiudies (δ, T1) of the protons of water solubilised in the surfactant-solvent systems are reported but do not show helpful correlations with catalytic efficiency in the system studied.A better guide to catalytic efficiency is provided by solvatochromic measurements using N-hexadecylpyridinium iodides incorporated into the catalytic aggregates to report on the polarity in the interior.A possible extension to this approach is discussed.
- Bethell, Donald,Galsworthy, Peter J.,Jones, Keith
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p. 2035 - 2044
(2007/10/02)
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- Synthesis of Hydroxyethyl Ethers from Long Chain Fatty Alcohols
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A two-step facile synthesis of mono- and di-β-hydroxyethyl ethers of long chain fatty alcohols starting from alcohols and chloro/bromo acetic esters is described.These compounds, which are otherwise difficult to obtain in pure state, are of great interest as plant groth promoters.
- Rao, Samala Jagadishwar,Bhalerao, Uday T.,Tilak, Bal Dattatreya
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p. 277 - 278
(2007/10/02)
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- Antihypertensive phosphate derivatives
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Antihypertensive phosphate derivatives are described having the following formula: STR1 wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C1 -C24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C1 -C20 branched or straight chain alkyl, C1 -C20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl; T is selected from the group consisting of hydrogen and STR2 wherein R1 is selected from the group consisting of hydrogen, C1 -C4 branched or straight chain alkyl, C1 -C4 branched or straight chain alkoxy and C1 -C4 branched or straight chain alkylamino, Q is a bivalent radical selected from the group consisting of --(CH2)p -- and --(CHR)p --, where p is an integer from 2 to 12 and the moiety --(CHR)p -- represents an alkylene chain which is substituted by one or more C1 -C10 alkyl groups or phenyl groups; Z is selected from the group consisting of --+ N(R2)3 and STR3 wherein R2 may be the same or different and is selected from the group consisting of hydrogen and C1 -C4 branched or straight chain alkyl and q is an integer from 4 to 7.
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- Analogues of Platelet Activating Factor (PAF). 2. Some Modifications of the Glycerine Backbone
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Racemic analogues of platelet activating factor (PAF) that contain a methylene group between the C2 and C3 carbon atoms (39) or between the C1 and C2 carbon atoms (40) have been synthesized.These compounds show reduced platelet aggregation and hypotensive activity as measured against racemic C16 PAF.Compounds in which the C1 carbon atom of PAF is substituted with one or two methyl groups (41 and 42, respectively) or the C3 carbon is substituted with a single methyl group (43) have been synthesized.Platelet aggregation and hypotensive responses producedby these compounds are significantly less than those obtained with racemic C16 PAF.None of the above compounds exhibit a separation of the platelet aggregation and hypotensive activities.
- Wissner, A.,Schaub, R. E.,Sum, P.-E.,Kohler, C. A.,Goldstein, B. M.
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p. 1181 - 1187
(2007/10/02)
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