10021-77-9Relevant academic research and scientific papers
QUINOLYL-CONTAINING COMPOUND AND PHARMACEUTICAL COMPOSITION, AND USE THEREOF
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Paragraph 0529-0530, (2022/02/19)
Provided is a quinolyl-containing compound as shown in general formula (I) or (II) or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an isotopic label, or an isomer thereof, and further provided are a pharmaceutical composition comprising the compound and use of the compound and the pharmaceutical composition. The provided compound has a dual molecule function, can serve as multi -target inhibitors of novel tyrosine kinase/histone deacetylase, can simultaneously achieve the effect of two inhibitors, has excellent biological activity and pharmacokinetic properties, and has the application potential particularly in the field of treatment of tumors.
Rapid assembly of a library of lipophilic iminosugars via the thiol-ene reaction yields promising pharmacological chaperones for the treatment of Gaucher disease
Goddard-Borger, Ethan D.,Tropak, Michael B.,Yonekawa, Sayuri,Tysoe, Christina,Mahuran, Don J.,Withers, Stephen G.
supporting information; experimental part, p. 2737 - 2745 (2012/06/01)
A highly divergent route to lipophilic iminosugars that utilizes the thiol-ene reaction was developed to enable the rapid synthesis of a collection of 16 dideoxyiminoxylitols bearing various different lipophilic substituents. Enzyme kinetic analyses revea
Exploiting enzymatic regioselectivity: A facile methodology for the synthesis of polyhydroxylated hybrid compounds
Magrone, Pietro,Cavallo, Francesco,Panzeri, Walter,Passarella, Daniele,Riva, Sergio
experimental part, p. 5583 - 5590 (2011/02/18)
Polyhydroxylated hybrid molecules have been synthesized using a protocol based on the regioselective acylation of the target compounds with activated dicarboxylic acids catalyzed by Novozym-435. The procedure implies that the mixed ester derivatives prepared and isolated from the first esterification step act as acylating agents in the second esterification step.
STYRYL SULFIDE DYES
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Page/Page column 28-30, (2009/08/14)
Disclosed are composition and method for dyeing keratin-containing fibers comprising or utilizing styryl sulfide dyes of formula (1), their salts, isomers, hydrates and other solvates, wherein R1, R′1, R2, R′2, R3, R′3, W1, W′1, W2, W′2, W3, W′3, W4, W′4, Q, Q′, Y1 and Y2 are defined in claims and disclosure.
Designer ligands. Part 4. Synthesis of acyclic and macrocyclic platinum group metal-specific ligands
Hagemann, Justin P.,Kaye, Perry T.
, p. 341 - 348 (2007/10/03)
Synthetic pathways to a range of novel, polydentate, sulfur-containing, mono-amide ligands, designed to coordinate platinum group metals, have been developed.Access to the tetradentate systems was facilitated by the extensive use of disulfide linkages as a protection strategy.
14α,14'β-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8- dihydromorphinone) and 14α,14'β-[dithiobis[2-oxo-2,1- ethanediyl]imino]]bis[7,8-dihydro-N-(cyclopropyl-methyl)normorphinone]: Chemistry and opioid binding properties
Archer,Seyed-Mozaffari,Jiang,Bidlack
, p. 1578 - 1585 (2007/10/02)
14α,14'β-[Dithiobis[2-oxo-2,1-ethanediyl)imino]]bis(7,8- dihydromorphinone) (TAMO) (13) was synthesized by condensing 14β-amino-7,8- dihydromorphinone (4) with acetylthioglycolyl chloride and hydrolyzing the resulting ester with mild base to give a mixture of the thiol 9 and the disulfide 13. Chromatography of the mixture resulted in conversion of the bulk of the thiol 9 to the disulfide 13 by air oxidation. The disulfide 13 was also prepared by condensing the tert-butyldimethylsilyl ether of 4 with the dithiodiglycolyl chloride and treating the resulting product with F- to give the desired product. The pure thiol 9 free of contamination with the disulfide was prepared by treating 13 with excess N-acetyl-L-cysteine and processing the reaction mixture without resorting to chromatography for purification. The corresponding N-(cyclopropylmethyl) nor compound 15 was prepared from the silyl ether 6 and acetylthioglycolyl chloride followed by hydrolysis, treatment with F-, and air oxidation. Incubation of bovine striatal membranes with 13 and 15 resulted in wash-resistant inhibition of the binding of the μ-selective peptide[3H][D-Ala2,(Me)Phe4,Gly(ol)5]- enkephalin (DAMGO). Incubation of membranes with μ but not κ or δ ligands protected the μ binding sites from alkylation by 13 and 15. The wash- resistant inhibition of μ opioid binding was partially reversed by the addition of the reducing reagent dithiothreitol (DTT). A Scatchard plot of the effect of 13 and 15 on [3H]DAMGO binding showed that these affinity ligands caused a marked decrease in the B(max) value without affecting the K(d) value. The wash-resistant inhibition of binding, the reduction in the number of binding sites, the partial reversal of wash-resistant inhibition of binding by DTT, and previously observed long-term antagonism of μ opioid receptors in vivo support the conclusion that 13 and 15 bind covalently to the μ opioid receptor.
SULFINIC ACIDS AND RELATED COMPOUNDS. 22. DERIVATIVES OF 2-HYDROXYETHANE-SULFINIC ACID
Lee, Chew,Stidham, D. Brian,Field, Lamar
, p. 53 - 59 (2007/10/02)
Sodium 2-hydroxyethanesulfinate (3) could be converted to the unstable methyl ester 8 by acidification followed by reaction with diazomethane (although the acid 4, itself, could not be isolated as reported).The ester 8 was esterified with 2,2'-dithioacetyl dichloride (10) to afford the desired convergent synthesis of a disulfide bissulfinate ester (11), but 11 was even less stable than 8; efforts to esterify the sulfinate salt 3 with 10 to give a more stable sulfinate salt counterpart (12) of the ester 11 were unpromising.The salt 12 also was sought by reduction of a sulfonyl chloride 13, which was obtained by coupling 10 with 2-hydroxyethanesulfonyl chloride (2) and for which the structure was confirmed by reaction with p-bromoaniline; 12 evidently was obtained, but greater purity not be obtained than ca. 83-95percent.In other reactions, 2-hydroxyethanesulfonyl chloride (2) reacted with p-bromoaniline, and the hydroxysulfonanilide (6) produced could be esterified with 10 to give 9 by use of special conditions.
Diazaestrones and analogs. I. Pharmacological study and synthesis of heterosteroid analogs to establish structure-analgesic activity relationships
Hocquaux,Marcot,Redeuilh,et al.
, p. 319 - 329 (2007/10/02)
With the intention of showing the effect, about pharmacological properties, in replacing two estron asymetric carbon by nitrogen atoms and removal of angular methyl from steroid, stereospecific synthesis of 8,13-diazaestron and several substituted similar compounds was realized from β-1-(succinimidoethyl)-dihydroisoquinolines, precursors of a C open ring synthesis. The splitting of the 2-methoxydiazaestron methyl ester was carried out by mean of binaphthylphosphoric acid, and synthesis of several modified analogs of heterosteroid, was carried out to determine the effect of aromatic ring reduction, lactamic carbonyl reduction, and distance between 8 and 13 nitrogen atoms, about pharmacological activity. Hormonal, spasmolytic and analgesic activities were studied, good results were observed in analgesic activity.
