- Hydrolysis of N-Substituted Phthalimides Using Anion Exchange Resins. Synthesis of Hydroxy-Substituted Aliphatic Primary Amines (Amino Alcohols)
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N-Substituted phthalimides were successfully hydrolyzed to the corresponding hydroxy-substituted aliphatic primary amines (amino alcohols) using anion exchange resins.This method has been proved to be extremely useful for water soluble products, which are
- Kuriyama, Naohiro,Inoue, Yoshiharu,Kitagawa, Keishi
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- Chiral linkers to improve selectivity of double-headed neuronal nitric oxide synthase inhibitors
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To develop potent and selective nNOS inhibitors, new double-headed molecules with chiral linkers that derive from natural amino acids or their derivatives have been designed. The new structures contain two ether bonds, which greatly simplifies the synthesis and accelerates structure optimization. Inhibitor (R)-6b exhibits a potency of 32 nM against nNOS and is 475 and 244 more selective for nNOS over eNOS and iNOS, respectively. Crystal structures show that the additional binding between the aminomethyl moiety of 6b and the two heme propionates in nNOS, but not eNOS, is the structural basis for its high selectivity. This work demonstrates the importance of stereochemistry in this class of molecules, which significantly influences the potency and selectivity of the inhibitors. The structure-activity information gathered here provides a guide for future structure optimization.
- Jing, Qing,Li, Huiying,Chreifi, Georges,Roman, Linda J.,Martasek, Pavel,Poulos, Thomas L.,Silverman, Richard B.
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- EIN NEUES ANTIFUNGISCHES β-LACTAM-ANTIBIOTICUM DER CLAVAM-REIHE
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The novel β-lactam-antibiotic (-)-2-(2-hydroxyethyl)clavam (1) originates from cultures of Streptomyces antibioticus.The structure is shown by spectroscopic and degradative methods.
- Wanning, Martin,Zaehner, Hans,Krone, Bernd,Zeeck, Axel
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- 2-Aminopyridine-based Selective Neuronal Nitric Oxide Synthase Inhibitors
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Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.
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Paragraph 0028; 0029; 0030
(2014/09/29)
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- PROCESS FOR THE PREPARATION OF OXAZOLIDINONES AND METHOD OF USE THEREOF
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A process for preparing N-(substituted)-C-- (substituted methyl)-oxazolidinones, C-(substituted methyl)-oxazolidinones, and N-(substituted)-C-- (substituted ethyl)-oxazolidinones, preferably chiral, from optically active C-(protected oxymethyl)- oxazolidi
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- Solid support for synthesis of 3'-tailed oligonucleotides
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A solid support for oligonucleotide synthesis has the structure STR1 where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytri
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- Absolute configuration of C(1)-C(5) fragment of AAL-toxin: Conformationally rigid acyclic aminotriol moiety
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Degradation of AAL-toxin 1 a host-specific phytotoxin and synthesis of model aminotriol 7a-7d allowed us to determine the absolute configuration of C(1)-C(5) fragment as 2S, 4S and 5R. Unusually rigid conformation of this acyclic fragment was also discussed.
- Oikawa, Hideaki,Matsuda, Isamu,Ichihara, Akitami,Kohmoto, Keisuke
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p. 1223 - 1226
(2007/10/02)
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- Substituted pyridines
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This invention relates to substituted pyridines prepared by reacting aldehydes, amines, lower carboxylic acids such as acetic acid in the presence of oxygen. The N-substituted pyridinium salts formed can be converted to pyridines by thermal dealkylation. The reactions can be summarized by the following equations: STR1
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