10494-75-4Relevant academic research and scientific papers
Solid phase synthesis of oligoethylene glycol-functionalized quinolinecarboxamide foldamers with enhanced solubility properties
Tsiamantas, Christos,Dawson, Simon J.,Huc, Ivan
, p. 132 - 142 (2016)
A series of octameric quinoline oligoamide foldamers has been synthesized consisting exclusively of monomers which display mono-, di-, tri- or tetra-ethylene glycol side-chains. These oligomers adopt stable helical conformations. New Fmoc-acid monomer precursors were first developed. The microwave assisted solid-phase synthesis (SPS) methodology for oligomer preparation is described, and it is demonstrated that small adjustments in side-chain length translate into large differences in the solubility profile of the oligomers. The impact of such modifications on foldamer preparation, handedness inversion kinetics and potential applications is also discussed.
Solvent Isotope Effects on Formation of Protease Complexes with Inhibitory Aldehydes, with an Appendix on the Determination of Deuterium Fractionation Factors by NMR
Bone, Roger,Wolfenden, Richard
, p. 4772 - 4777 (1985)
In both CCl4 and water, equilibria of addition of thiols to acetaldehyde are strongly favored by the presence of deuterium at exchangeable positions, whereas equilibria of addition of hydroxylic compounds are hardly affected.To test the possibility of using solvent isotope effects for diagnosing the structure of enzyme-inhibitor complexes, we examined the influence of D2O on the interaction of proteases with inhibitory aldehydes.Equilibrium constants for binding of inhibitory aldehydes showed enhancements in D2O of 1.32+/-0.12 for α-chymotrypsin and 2.65+/-0.14 for papain, slightly in excess of those expected for covalent addition of an alcohol or thiol, respectively.In an Appendix, hydroxylic solutes are shown to alter the magnetic susceptibilities of solutions, resulting in systematic errors in apparent fractionation factors of their exchangeable protons as determined by conventional NMR procedures.As a result, apparent fractionation factors change with the orientation of the magnetic field.Corrected values for hydroxylic protons, determined by other methods, differ only slightly from unity.
Cationic [99mTcIII(DIARS)2(SR)2]+ complexes as potential myocardial perfusion imaging agents (DIARS = o-phenylenebis(dimethylarsine);SR- = thiolate).
Tisato,Maina,Shao,Heeg,Deutsch
, p. 1253 - 1261 (1996)
Reduction-substitution reactions on [99mTcO4]- with both o-phenylenebis(dimethylarsine) (DIARS) and various thiols produce a series of monocationic [99Tc(DIARS)2(SR)2]+ complexes. Addition of [99gTcO4]- to the above reaction mixtures allows the characterization of the "carrier-added" complexes by means of reverse-phase high-performance liquid chromatography with radiometric and optical detection systems. The identity of the [99mTc(DIARS)2(SR)2]+ complexes is confirmed by fast atom bombardment mass spectroscopy; equivalence of the [99gTc(DIARS)2-(SR)2]+ and [99mTc(DIARS)2(SR)2]+ species is demonstrated by identical HPLC retention times. All the [99mTc(DIARS)2(SR)2]+ complexes tested accumulate in the myocardium of Sprague-Dawley rats with an average uptake of 1.5-2.0% of injected dose/g at 30 min. Thus, as designed, these nonreducible Tc(III) complexes do not exhibit the rapid myocardial washout observed for reducible Tc(III) complexes. These [99mTc(DIARS)2(SR)2]+ complexes also exhibit an initially high liver uptake, but the presence of ether groups within the thiolate ligands causes this liver uptake to decrease over time without affecting the heart uptake, thereby improving the heart/liver ratio.
BORON CONTAINING COMPOUNDS AND THEIR USES
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Paragraph 0251; 0252, (2020/03/29)
The present disclosure contemplates novel boron-containing compounds and their uses as active agents that exhibit pesticidal activity such as antimicrobial, insecticidal, arachnicidal, and/or anti parasitic activity. An agrochemical composition containing such a compound and its use in, animal health, agriculture, or horticulture is also contemplated. A method for promoting plant performance and/or controlling, reducing, preventing, ameliorating, or inhibiting microbes, insects, arachnids, and/or parasites on or in an animal, a plant, a plant part, plant propagation material, and/or harvested fruits or vegetables is also contemplated.
As tyrosine kinase inhibitors of the nitrogen-containing heteroaromatic ring derivatives
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Paragraph 0404; 0405; 0409; 0410; 0411, (2018/09/02)
The present invention relates to compounds as represented by general formula (I) as tyrosine kinase inhibitors, preparation method thereof, pharmaceutical compositions containing the compounds, and uses thereof for preventing and/or treating instances of B-cell related leukemia, inflammatory diseases and autoimmune diseases, wherein A, ring B, L1, L2, R1, R2, R3, a, b, c, d, e, p and q are as defined in the specification.
A general and mild synthesis of thioesters and thiols from halides
Zheng, Tu-Cai,Burkart, Maureen,Richardson, David E.
, p. 603 - 606 (2007/10/03)
The conversion of a wide variety of halides to thioesters by reaction with potassium thiocetate under mild conditions is described, and the generality of the method is demonstrated.
EFFICIENT AND/OR SELECTIVE METHYLATION BY DIAZOMETHANE OF ALCOHOLS, HALO ALCOHOLS, GLYCOLS, AMINO ALCOHOLS AND MERCAPTO ALCOHOLS WITH THE USE OF A PROTON-EXCHANGED X-TYPE ZEOLITE AS AN ACID-BASE BIFUNCTIONAL CATALYST
Takeuchi, Hiroshi,Kishioka, Hiroaki,Kitajima, Kunio
, p. 121 - 126 (2007/10/02)
Reactions of diazomethane with butanol, allyl alcohol and β- and γ-halo alcohols led to efficient methylation (giving the corresponding methyl ethers) with the use of a proton-excahnged X-type zeolite compared with H2SO4.The reactions with propylene and isobutylene glycols using the zeolite provided regioselective methylation of the primary OH rather than the secondary or tertiary OH, whereas regioselectivity was not observed in the reactions using H2SO4.The reactions with 2-aminoethanol and 2-mercaptoethanol showed high chemoselective S-methylation and N-monomethylation, respectively, in the presence of the zeolite instead of H2SO4.The mechanism for the reactions is proposed to involve acid-base bifunctional catalysis of the zeolite in which the acidic site reacts with diazomethane to form its conjugate acid, and the nucleophilicity of OH and SH groups is enhanced by the interaction of the basic site with the proton of the groups.
