- Discovery of 5-(4-hydroxyphenyl)-3-oxo-pentanoic acid [2-(5-methoxy-1H- indol-3-yl)-ethyl]-Amide as a neuroprotectant for Alzheimers Disease by Hybridization of Curcumin and Melatonin
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In our effort to develop effective neuroprotectants as potential treatments for Alzheimer"s disease (AD), hybrid compounds of curcumin and melatonin, two natural products that have been extensively studied in various AD models, were designed, synthesized,
- Chojnacki, Jeremy E.,Liu, Kai,Yan, Xing,Toldo, Stefano,Selden, Tyler,Estrada, Martin,Rodríguez-Franco, María Isabel,Halquist, Matthew S.,Ye, Dexian,Zhang, Shijun
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- Synthesis and evaluation of donepezil-ferulic acid hybrids as multi-target-directed ligands against Alzheimer's disease
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A novel family of donepezil-ferulic acid hybrids were designed, synthesized and biologically evaluated as multi-target-directed ligands against Alzheimer's disease by fusing a fragment of donepezil and ferulic acid. The in vitro assay indicated that some
- Xu, Wei,Wang, Xiao-Bing,Wang, Zhi-Min,Wu, Jia-Jia,Li, Fan,Wang, Jin,Kong, Ling-Yi
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- Synthesis and biological activity of alkylidene-substituted cephems and penams
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The condensation of tert-butyl esters of 3-methyl-7-oxoceph-3-em-4- carboxylic and 6-oxopenicillanic acids with a series of 2- oxoalkylidene(triphenyl)phosphoranes gave tert-butyl esters of new cephalosporin and penicillin analogs with an alkylidene substituent in the β-lactam ring. Most of these products were oxidized by meta-chloroperbenzoic acid to the corresponding sulfones. The cephemes and penams synthesized including the oxidized products displayed high cytotoxicity relative to cancer cells in vitro. Some of the alkylidene-substituted cephems as the free acids, similar to Tazobactam, inhibit the catalytic activity of Enterobacter cloacae penicillinase.
- Potorocina,Vorona,Shestakova,Domracheva,Liepinsh,Veinberg
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- Metal-Free Synthesis of 1,5-Disubstituted 1,2,3-Triazoles
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Abstract: The main synthetic approaches to 1,5-disubstituted 1,2,3-triazoles are considered. It is shown that the cycloaddition of aryl azides to phosphorus ketoylides provide a convenient method for the synthesis of 1,5-disubstituted 1,2,3-triazoles, esp
- Obushak, M. D.,Pokhodylo, N. T.,Tupychak, M. A.
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p. 209 - 218
(2022/04/19)
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- The first chemical synthesis of pyrazofurin 5′-triphosphate
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As an archetype C-nucleoside, pyrazofurin possesses broad-spectrum antiviral and antitumor activities. However, the presence of the acidic enol in the nucleobase of pyrazofurin poses a huge challenge to the conventional NTP synthetic methods. On the basis
- Huang, Hua-Shan,Wang, Rui,Chen, Wei-Jie,Chen, Ji-Zong,Gong, Shan-Shan,Sun, Qi
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supporting information
p. 3423 - 3427
(2018/08/17)
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- HYBRID COMPOUNDS OF CURCUMIN AND MELATONIN AS NEUROPROTECTANTS FOR NEURODEGENERATIVE DISORDERS
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Hybrid compounds of curcumin and melatonin as neuroprotectants are provided. The hybrid compounds are useful for the treatment and/or prevention of Alzheimer's disease (AD), as well as other neurodegenerative diseases. The hybrid compounds exhibited super
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Page/Page column 19
(2015/05/26)
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- Oxone-mediated oxidative cleavage of β-keto esters and 1,3-diketones to α-keto esters and 1,2-diketones in aqueous medium
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A versatile and highly efficient method for the direct synthesis of α-keto esters and 1,2-diketones has been developed. This approach utilizes the oxidative cleavage of a variety of β-keto esters and 1,3-diketones mediated by an Oxone/aluminum trichloride system. The simple one-step oxidation reaction proceeded selectively in aqueous media to afford products in high yields, short reaction times, and environmentally benign conditions.
- Stergiou, Anastasios,Bariotaki, Anna,Kalaitzakis, Dimitris,Smonou, Ioulia
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p. 7268 - 7273
(2013/08/15)
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- Structural, theoretical and multinuclear NMR study of mercury(II) complexes with a new ambidentate phosphorus ylide
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The reaction of the new ambidentate ylide, Ph3PCHCOCH 2COOC2H5 (EAPPY), with HgX2 (X = Cl, Br and I) in equimolar ratios using methanol as the solvent leads to binuclear complexes of the type [EAPPY·H
- Sabounchei, Seyyed Javad,Salehzadeh, Sadegh,Hosseinzadeh, Marjan,Bagherjeri, Fateme Akhlaghi,Khavasi, Hamid Reza
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experimental part
p. 2486 - 2492
(2011/10/18)
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- NOVEL POLYSPIRANE COMPOUNDS, APPLICATION THEREOF IN THE TREATMENT OF MALARIA OR TOXOPLASMOSIS AND METHOD FOR PREPARING SAME
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Novel polyspirane compounds used in the treatment of diseases involving parasites that belong to the phylum of apicomplexae, and a method for preparing the same.
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(2010/12/29)
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- Antitumour polycyclic acridines. Part 13. Synthesis of 2-substituted 7H-pyrido[4,3,2-kl]acridines by thermolysis of 9-(5-alkyltriazol-1-yl)acridines
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Interaction of phosphoranylidene ketones with 9-azidoacridine in refluxing benzene affords 9-(5-substituted triazol-1-yl)acridines, which, on thermolysis in boiling diphenyl ether at 259 °C, yield 2-substituted 7H-pyrido[4,3,2-kl] acridines in high yields. These tetracyclic acridines are less potent inhibitors of human tumour cells in vitro than their pentacyclic analogues.
- Ellis, Michael J.,Stevens, Malcolm F. G.
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- Monocyclic L-Nucleosides, analogs and uses thereof
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Novel monocyclic L-Nucleoside compounds have the general formula STR1 Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.
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- A New Preparative Route to 3-Unsubstituted Cephalosporins from Penicillin V
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p-Nitrobenzyl (2R,3R)-2-(benzothiazol-2'-yldithio)-α-isopropylidene-4-oxo-3-phenoxyacetylaminoazetidine-1-acetate (7), readily prepared from penicillin V, can be converted into the corresponding 2-allylthio compound (2) by addition of allyl bromide and sodium borohydride at a low temperature.This compound (2) on treatment with ozone, followed by cyclization with trimethyl phosphite, produces a 3H-ceph-3-em ester (4).The ester can be easily de-esterified to the free acid (1b).
- Davis, Michael,Wu, Wen-Yang
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p. 1591 - 1600
(2007/10/02)
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- SNTHESIS AND "ANOMERIZATION" OF C-GLYCOSYL COMPUNDS RELATED TO SOME HETEROCYCLIC NATURAL PRODUCTS
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Reaction of 2,3-O-isopropylidene-D-ribofuranose (13) with the stabilized Wittig reagents Ph3P=C(Me)CO2Me (14) and Ph3P=C(Me)CN (15) gave olefinic products which, upon treatment with dilute base, afforded the corresponding anhydro sugars having the β-D-anomer configuration excusively.Treatment of these kinetic products with a strong base did not affect the ester obtained from 14, but the nitrile from 15 gave a β-to-α-anomer ratio at equilibrium of 4:1.Reaction of 13 with Ph3P=CHCOMe led directly to a 7:3 mixture of β- and α-D anomers, and this ratio was changed to 1:4 upon prolonged exposure to base.Treatment of 4,6-O-ethylidene-D-glucopyranose with the Wittig reagent Ph3P=CHCOCH2CO2Et led directly to a 1:1 mixture of the anomers of the anhydro sugar in which a β-keto ester residue is attached at the (original) anomeric center.This ratio of anomeric forms coud not be changed by treatment with base, but the ethylidene-protecting group could be removed, and the resulting tetrol tritylated at the primary position.
- Sun, King Mo,Dawe, Robert D.,Fraser-Reid, Bert
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