- 1,2-NAPHTHOQUINONE DERIVATIVE AND METHOD FOR PREPARING SAME
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Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: wherein R1to R6, X1 to X4, and n are the same as defined in Claim 1.
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Paragraph 0302; 0304
(2016/11/21)
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- Novel Isobaric Tandem Mass Tags for Quantitative Proteomics and Peptidomics
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Compositions and methods of tagging peptides and other molecules using novel isobaric tandem mass tagging reagents, including novel N,N-dimethylated amino acid 8-plex and 16-plex isobaric tandem mass tagging reagents. The tagging reagents comprise: a) a reporter group having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an amine reactive group. The tagging reagents disclosed herein serve as attractive alternatives for isobaric tag for relative and absolute quantitation (iTRAQ) and tandem mass tags (TMTs) due to their synthetic simplicity, labeling efficiency and improved fragmentation efficiency.
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- Resolution of racemic N-benzyl α-amino acids by liquid-liquid extraction: A practical method using a lipophilic chiral cobalt(III) salen complex and mechanistic studies
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The efficient resolution of racemic N-benzyl α-amino acids (N-Bn-AA) has been achieved by a liquid-liquid extraction process using the lipophilic chiral salen-cobalt(III) complex [CoIII(3)(OAc)]. As a result of the resolution by extraction, one enantiomer (S) of the N-benzyl α-amino acid predominated in the aqueous phase, while the other enantiomer (R) was driven into the organic phase by complexation to cobalt. The complexed amino acid (R) was then quantitatively released by a reductive (CoIII→Co II) counter-extraction with aqueous sodium dithionite or L-ascorbic acid in methanol. The reductive cleavage allowed to recover the [Co II(3)] complex in good yield, which could be easily re-oxidized to [CoIII(3)(OAc)] with air/AcOH and reused with essentially no loss of reactivity and selectivity. Investigation on the nitrogen substitution indicates that the presence of a single benzyl group on the amino acid nitrogen is important to obtain high enantioselectivity in the extraction process. The kinetic vs. thermodynamic nature of the resolution process was also investigated with an enantiomeric exchange experiment, which shows that the liquid-liquid extraction with [CoIII(3)-(OAc)] is an equilibrium process operating under thermodynamic control. In the absence of a suitable crystal structure of the [CoIII(3)(N-Bn-AA)] complexes, computational and spectroscopic studies were used to investigate how the N-benzyl α-amino acids are accommodated in the "binding pocket" of the chiral cobalt complex. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Dzygiel, Pawel,Reeve, Toby B.,Piarulli, Umberto,Krupicka, Martin,Tvaroska, Igor,Gennari, Cesare
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supporting information; experimental part
p. 1253 - 1264
(2009/04/07)
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- Synthesis and anticonvulsant activity of some amino acid derivatives. Part 1: Alanine derivatives
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Fifteen amides of N-substituted D-Ala, DL-Ala and βAla have been designed and synthesized as potential anticonvulsants. All obtained amides as well as one intermediate (8) were evaluated in the maximal electroshock seizure (MeS) test, the subcutaneous Metrazol seizure threshold (sc Met) test and the rotorod neurotoxicity (Tox) test in mice. According to the classification of the Anticonvulsant Screening Project (ASP) of the Antiepileptic Drug Development Program (ADDP) eight compounds received class I, three class II and five class III designations. Two of the most active compounds (20, 24) were tested quantitatively. They exhibited, after i.p. administration in mice, a large protective index (PI) 3.2 for 20 and 4.3 for 24 and after oral administration in rat PI >18 for 20 and >14 for 24.
- Paruszewski,Rostafinska-Suchar,Strupinska,Jaworski,Stables
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p. 145 - 148
(2007/10/03)
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- Studies on the Stereochemical Characterization of N-Methylated Amino Acids
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Various methods that could be to determine the absolute configuration of N,N-dimethylated amino acids were investigated.Two methods utilizing 1H nuclear magnetic resonance (n.m.r.) spectroscopy were successful.The first involved the conversion of the N,N-
- Ang, Siau-Gek,Low, Siew Hsien
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p. 1591 - 1601
(2007/10/02)
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- Structure Elucidation of a Glycopeptide Antibiotic, OA-7653
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The structure of a vancomycin-type antibiotic, OA-7653, isolated from Streptomyces hygroscopicus subsp. hiwasaensis subsp. nov.Nishida, has been elucidated by a combination of classical chemical methods, mass spectrometry, and nuclear magnetic resonance spectroscopy.The interaction of OA-7653 with the peptide cell wall analogues N-acetyl-D-alanyl-D-alanine, and di-N-acetyl-L-lysyl-D-alanyl-D-alanine, in solution in aqueous dimethyl sulphoxide, has been examined by n.m.r. and u.v. difference spectroscopy.
- Ang, Siau-Gek,Williamson, Michael P.,Williams, Dudley H.
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p. 1949 - 1956
(2007/10/02)
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