- Synthesis, antimicrobial and in vitro antitumor activities of a series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives
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Three derivatives of substituted 1,2,3-thia- or 1,2,3-selenadiazole (4ac) were prepared and characterized by different chemical techniques. These compounds were evaluated for their antimicrobial and antitumor activities. Compounds 4a (propenoxide derivati
- Mhaidat, Nizar M.,Al-Smadi, Mousa,Al-Momani, Fouad,Alzoubi, Karem H.,Mansi, Iman,Al-Balas, Qosay
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- Regioselective Copper-Catalyzed Oxidative Coupling of α-Alkylated Styrenes with Tertiary Alkyl Radicals
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A radical-mediated oxidative cross-coupling of readily accessible α-alkylated styrenes with 1,3-dicarbonyl compounds utilizing a combination of Cu(OAc)2 and air as a catalytic system is described. Rather than requiring α-halocarbonyl compounds, this efficient approach enables direct installation of tertiary functionalized alkyl motifs to olefins with simple carbonyl derivatives. The novel protocol is characterized with high allylic selectivities via a competing β-H elimination. Both radical-clock and -trapping experiments provided clear-cut evidence for the intermediacy of an α-keto carbon-centered radical.
- Wang, Cong,Liu, Rui-Hua,Tian, Ming-Qing,Hu, Xu-Hong,Loh, Teck-Peng
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supporting information
p. 4032 - 4035
(2018/07/15)
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- Synthesis, pharmacological activity, and chromatographic enantioseparation of new heterocyclic compounds of the aryloxyaminopropanol type derived from 4-hydroxyphenylalkanones
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Abstract: In the paper, a series of six pharmacologically active compounds (β-adrenolytics) derived from 4-hydroxyphenylethanone and 4-hydroxyphenylpropan-1-one are reported. The compounds incorporate pyrrolidin-1-yl and 4-methylpiperazin-1-yl substituent
- ?i?máriková, Ru?ena,Némethy, Andrej,Habala, Ladislav,Ra?anská, Eva,Valentová, Jindra,Hroboňová, Katarína
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p. 969 - 976
(2018/05/07)
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- Synergistic dual activation catalysis by palladium nanoparticles for epoxide ring opening with phenols
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Synergistic dual activation catalysis has been devised for epoxide phenolysis wherein palladium nanoparticles induce electrophilic activation via coordination with the epoxide oxygen followed by nucleophilic activation through anion-π interaction with the aromatic ring of the phenol, and water (reaction medium) also renders assistance through 'epoxide-phenol' dual activation.
- Seth, Kapileswar,Roy, Sudipta Raha,Pipaliya, Bhavin V.,Chakraborti, Asit K.
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supporting information
p. 5886 - 5888
(2013/07/25)
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- Thermally activated, single component epoxy systems
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A single component epoxy system in which the resin and hardener components found in many two-component epoxies are combined onto the same molecule is described. The single molecule precursor to the epoxy resin contains both multiple epoxide moieties and a
- Unruh, David A.,Pastine, Stefan J.,Moreton, Jessica C.,Frechet, Jean M. J.
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experimental part
p. 6318 - 6325
(2012/06/18)
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- ANALGESIC THAT BINDS FILAMIN A
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A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
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Page/Page column 105
(2010/05/14)
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- The hERG potassium channel and drug trapping: Insight from docking studies with propafenone derivatives
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The inner cavity of the hERG potassium ion channel can accommodate large, structurally diverse compounds that can be trapped in the channel by closure of the activation gate. A small set of propafenone derivatives was synthesized, and both use-dependency and recovery from block were tested in order to gain insight into the behavior of these compounds with respect to trapping and non-trapping. Ligand-protein docking into homology models of the closed and open state of the hERG channel provides the first evidence for the molecular basis of drug trapping.
- Thai, Khac-Minh,Windisch, Andreas,Stork, Daniela,Weinzinger, Anna,Schiesaro, Andrea,Guy, Robert H.,Timin, Eugen N.,Hering, Steffen,Ecker, Gerhard F.
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scheme or table
p. 436 - 442
(2010/11/17)
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- Conversion of epoxides to β-chlorohydrins with thionyl chloride and β-cyclodextrin in water
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Several epoxides are efficiently converted to the corresponding β-chlorohydrins in impressive yields with thionyl chloride in the presence of β-cyclodextrin using water as solvent at room temperature. Copyright Taylor & Francis, Inc.
- Surendra,Srilakshmi Krishnaveni,Nageswar,Rama Rao
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p. 2195 - 2201
(2007/10/03)
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- Synthesis, anorexigenic activity and QSAR of substituted aryloxypropanolamines
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Substituted aryloxypropanolamines (6-20) were synthesized and evaluated for their anorexigenic activity. Among them 4-cyanoaryloxy (7), 2-methylaryloxy (9), 2-methoxyl aryloxy (10), 4-acetamidoaryloxy (15), 4-bromoaryloxy (16) and 4-ethylaminoaryloxy (20) exhibited potent anorexigenic activity. According to QSAR studies, the electronic parameter 'σ' plays an important role in describing the variance in activity. Birkhaeuser Boston 2004.
- Srivastava, Shipra,Bhandari, Kalpana,Shankar, Girija,Singh,Saxena, Anil K.
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p. 631 - 642
(2007/10/03)
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- Transformation of terminal diols of cyclic and acyclic saccharides to epoxides and alkenes by reaction with triphenylphosphine, imidazole and iodine
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Reaction of various terminal diols 1,4,6,8-12, derived from cyclic and acyclic monosaccharides, with 2 mol equivalents each of TPP-imidazole-I2 between -8 °C and 15 °C in THF afforded the corresponding epoxides 2,5,7,13-17, respectively, with 4
- Mereyala, Hari Babu,Goud, P. Mallikarjun,Gadikota, Rajendrakumar Reddy,Reddy, K. Ramasubba
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p. 1211 - 1222
(2007/10/03)
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- Microwave enhanced synthesis of epoxypropoxyphenols
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Phenols were condensed with epichlorohydrin under microwave irradiation. Dramatic reduction in reaction time was observed with excellent yields.
- Khadilkar, Bhushan M.,Bendale, Pravin M.
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p. 2051 - 2056
(2007/10/03)
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- Synthesis of the highly cardioselective β-sympathicolytic pacrinolol
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The synthesis is described of the enantiomerically pure (-)-3-(3,4-dimethoxyphenylethylamino-2-hydroxypropoxy] phenyl]-cis-crotonic acid nitrile (13b) (free base) and its hydrochloride (13c) (pacrinolol, Hoe 224 A) starting from p-hydroxyacetophenone (1) and racemic epichlorohydrin (2). The p-(2,3-oxidopropoxy)acetophenone (2) resulting from this reaction is C-homologisized to (8); reactions of this with homoveratrylamine (9) leads to (10a), the racemic structural analog of (13b). Resolution of the racemate is achieved by fractional crystallisation of the diastereoisomeric mandelates (13a) and (14a) to afford the enantiomerically pure title compound (13c) and its dextrarotatory optical antipode (14c). Structural confirmation of (13b) and (13c) was achieved through physicochemical and spectroscopic data especially from the 1H-NMR- and MS-spectra. Pacrinolol (13c) is a highly cardioselective β-sympathicolytic with significant and long acting blood pressure lowering properties (intravenous and oral in the dog).
- Stache,Fritsch,Fehlhaber
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p. 1217 - 1221
(2007/10/02)
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