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PubMed1981

[Heterocyclic compounds containing a 4-aminophenylalkanoic acid group with potential antiinflammatory activity. II. 2-Substituted morpholine derivatives].

Derivatives of 4-aminophenylalkanoic acids where the amino groups is part of a 3-morpholinone or a 2-morpholine ring, substituted in position 2 with a methyl, phenyl, 2-thienyl or (2-cyclohexyl)phenoxymethyl residue are described. Pharmacological evaluation aimed at evidencing analgesic and anti-inflammatory activity gave no noteworthy results.

Animals↗
PubMed2003

Evidence for the intermediacy of arylbenzylnitrenium ions in the thermal rearrangement of isoxazolidines derived from C,N-diarylnitrones and 2-morpholin-4-yl-acrylonitrile.

In contrast to the diaryl, dialkyl, alkylaryl, and parent series, nothing is known about the generation and chemical behavior of arylbenzylnitrenium ions. Herein, we report that these species can be generated by a process involving an unprecedented thermal rearrangement of isoxazolidines derived from C,N-diarylnitrones and 2-morpholin-4-yl-acrylonitrile. The products from these reactions are dramatically dependent upon the nature of the nitrone. Most of the observed chemistry originates from the singlet state.

Journal Article↗
PubMed1984

Fractionation techniques in a hydro-organic environment. II. Acryloyl-morpholine polymers as a matrix for electrophoresis in hydro-organic solvents.

The properties of gels prepared either from acryloyl-morpholine (ACM) or from its mixtures with acrylamide and crosslinked either with bisacrylylpiperazine or with methylenebisacrylamide have been described. ACM-containing gels are compatible with organic solvents. If polymerized in water and dried, they are able to reswell, e.g., in dimethyl sulfoxide or dimethylformamide. If polymerized in presence of dimethylformamide, they form perfectly clear gels, whose mechanical properties are by far superior than those of similar plain polyacrylamide formulations.

Acrylic Resins↗
PubMed2005

Pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones.

Synthesis, biological evaluation and structure-activity relationships for a series of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines are described. These compounds represent a new chemotype of nonpeptide small molecule inhibitors of caspase-3. Among the studied compounds, several potent inhibitors with IC50 in the range of 3-10 nM have been identified. The most active compound within this series, 7{49} and 7{58}, inhibited caspase-3 with IC50=3 nM.

Caspase 3↗
PubMed2006

Ester aminolysis by morpholine in AOT-based water-in-oil microemulsions.

A kinetic study of the aminolysis of p-nitrophenyl acetate (NPA) by morpholine (MOR) in AOT/isooctane/water (w/o) microemulsions was conducted. Based on the solubilities of NPA and MOR in water and isooctane, both compounds partition between the continuous medium, interface and water microdroplets of the microemulsion. Because the rate of the aminolysis reaction decreases with decreasing polarity of the solvent, the reaction must take place to a negligible extent in the continuous medium relative to the interface and the aqueous microdroplets. We used the pseudo-phase model to determine the rate constants at the interface, k(2)(i), and in the water microdroplets, k(2)(w). Both k(2)(i) and k(2)(w) were found to be independent of W in the aminolysis of NPA by MOR. This is a result of the expected increase in k(2)(w) on decreasing W being offset by the decrease in k(2)(i) with increase in the water content of the system. Based on the results, the reaction takes place to an extent of only 16% in the water microdroplets at W=40, the proportion decreasing with decreasing water content.

Journal Article↗
PubMed2004

Low melting inorganic salts of alkyl-, fluoroalkyl-, alkyl ether-, and fluoroalkyl ether-substituted oxazolidine and morpholine.

N-Alkyl- and N-fluoroalkyl-substituted oxazolidinium- and morpholinium-based quaternary salts and ionic liquids have been synthesized and characterized. Reactions of N-methyloxazolidine (1) or N-methylmorpholine (2) with 3-fluoropropyl bromide or iodopropane in THF at 25 degrees C gave the quaternary salts (3a,b, 4a,b). These salts were metathesized with various metal salts to yield the corresponding ionic liquids (5a-h, 6a-i). N-Alkoxyethyl- and N-(fluoroalkoxy)ethyl-substituted morpholines (8-11) were prepared and quaternized with methyl iodide (8a-11a). Their corresponding ionic liquids (12-18) were obtained by anion exchange and characterized. For both series of compounds, nitrate, hexafluorophosphate, perchlorate, triflate, and bis(trifluoromethanesulfonyl)amide were utilized. Most of the final products are liquids at 25 degrees C and are thermally stable with long liquid ranges as determined by thermal gravimetric analyses. For compounds 12, 16, and 18, thermal stabilities of > or =400 degrees C were observed. All the new compounds were characterized by spectroscopic and elemental analyses. Their densities and viscosities were also determined.

Journal Article↗
PubMed2006

Diastereoselective synthesis of enantiopure morpholines by electrophilic selenium-induced 6-exo cyclizations on chiral 3-allyl-2-hydroxymethylperhydro-1,3-benzoxazine derivatives.

Enantiopure morpholine derivatives have been prepared by selenocyclofunctionalization of chiral 3-allyl-2-hydroxymethyl-substituted perhydro-1,3-benzoxazine derivatives. The cyclization occurs in high yields and diastereoselection, although the temperature of the reaction and the structure of the substituent at C-2 and the substitution pattern of the double bond can modify the regio- and stereochemistry of the final products.

Journal Article↗
PubMed2002

Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 6-chloro-7-[corrected](2-morpholin-4-ylethylamino)-quinoline-5,8-dione.

The Cdc25 dual specificity phosphatases coordinate cell cycle progression, but potent and selective inhibitors have generally been unavailable. In the present study, we have examined one potential inhibitor, 6-chloro-7-(2-morpholin-4-ylethylamino)-quinoline-5,8-dione (NSC 663284), that was identified in the compound library of the National Cancer Institute [corrected]. We found that NSC 663284 arrested synchronized cells at both G(1) and G(2)/M phase, and blocked dephosphorylation and activation of Cdk2 and Cdk1 in vivo, as predicted for a Cdc25 inhibitor. Using the natural Cdc25A substrate, Tyr(15)-phosphorylated Cdk2/cyclin A, we demonstrated that NSC 663284 blocked reactivation of Cdk2/cyclin A kinase by Cdc25A catalytic domain in vitro. In-gel trypsin digestion followed by capillary liquid chromatography-electrospray ionization mass spectrometry and tandem mass spectrometry revealed the direct binding of NSC 663284 to one of the two serine residues in the active site loop HCEFSSER of the Cdc25A catalytic domain. Cdc25 binding and inhibition could contribute to the anti-proliferative activity of NSC 663284 and its ability to arrest cell cycle progression. Moreover, NSC 663284 should be a valuable reagent to probe the actions of Cdc25 phosphatases within cells and may also be useful structure for the design of more potent and selective antiproliferative agents.

Animals↗
PubMed1997

Synthesis and pharmacokinetic behaviour of ester derivatives of 4-isobutylphenyl-2-propionic acid (Ibuprofen) with end-hydroxylated poly(N-vinyl pyrrolidinone) and poly(N-acryloyl morpholine) oligomers.

Four derivatives of 4-isobutylphenyl-2-propionic acid (Ibuprofen), in which the drug was bound by ester linkages to poly(ethylene glycols) (PEG 2000-I), monomethoxy poly(ethylene glycols) (PEG 1900-I), poly(N-vinyl pyrrolidinone) (PVP-I) and poly(N-acryloyl morpholine) (PACM-I), all having approximatively the same number average molecular weight (Mn congruent equal to 2000), were prepared and tested for their pharmacokinetic properties after oral administration. It was found that the two end-hydroxylated amphiphilic oligomers of polyvinylic structure, PACM and PVP, whose physico-chemical properties are comparable to those of PEGs especially as regards solvent affinity, have in principle a similar potential as promoieties for preparing oligomeric prodrugs.

Acrylic Resins↗
PubMed2004

[Synthesis of 2-(4-dimethylaminophenyl)-5-fluoro-6-(morpholin-4-yl)-1H-benzimidazole and its spectroscopic research].

A new potential pharmaceutical compound, 2-(4-dimethylaminophenyl)-5-fluoro-6-(morpholin-4-yl)-1H-benzimidazole (4) was synthesized. The effect of the pH value of aqueous solution on the absorption spectrum of compound 4 and its interaction with beta-cyclodextrin (beta-CD) were investigated by UV-Vis spectrum, steady-state fluorescence and time-resolved spectroscopic measurements. The results indicate that compound 4 mainly exists in neutral molecular state when pH value of the aqueous phase is above 7.0. In the pH range from 7.0 to 3.8 the neutral molecular state and protonated univalent cationic form coexist. As the pH value decreases, the content of univalent cationic form increases. When 2.76 < pH < 3.8, the protonated univalent cationic form is the predominant species. With further decrease of the pH value, the univalent cation is protonated by another H+ to form a bivalent cation, and both univalent and bivalent cations coexist in the solution. The steady-state fluorescence and time-resolved spectroscopic measurements revealed that compound 4 is a sensitive molecular probe. The interaction of compound 4 and beta-CD is very strong. The guest:host ratio of inclusion complex between compound 4 and beta-CD formed in the aqueous solution (pH = 9.50) is 1:1, and the association constant was determined to be (1.02 +/- 0.04) x 10(3) mol x L(-1).

Absorption↗
PubMed1994

p-Aminobenzene sulphonyl morpholine, compound 82/208 a new anticonvulsant agent.

p-Aminobenzene sulphonyl morpholine, compound 82/208, was evaluated for acute toxicity and anticonvulsant action in mice against tonic seizures induced by supramaximal electroshock and pentylene tetrazole and strychnine induced seizures and for its effect on blood pressure and respiration in cat. Diphenyl hydantoin (DPH) was used as reference standard. Compound 82/208 exhibited anticonvulsant activity against electroshock induced seizures and PTZ induced tonic seizures in mice. The compound had several distinct advantages over DPH in experimental evaluation in mice.

Animals↗