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The alkylation of (4-fluorophenyl)acetonitrile with dibrompentane and 2,2'-dichlorodiethyl ether gave the corresponding nitriles, which were reduced with lithium aluminium hydride to obtain [1-(4-fluorophenyl)cyclohexyl]- and [1-(4-fluorophenyl)tetrahydro-2H-pyran-4-yl]methanamines. Treatment of the latter products with aryloxymethyloxiranes substituted in the aromatic ring resulted in the synthesis of. Some of the synthesized aryloxypropanolamines were transformed into the corresponding oxazolidines under the action of formalin. [ABSTRACT FROM AUTHOR]

The condensation of 2-alkylsulfanyl-substituted 2-en-4-ynals with N,N- and N,O-binucleophiles gives the corresponding 1,3-perhydrodiazines, 1,3-imidazolidines, and 1,3-oxazolidines with the original combination of substituents. [ABSTRACT FROM AUTHOR]

In the last decade, the number of transcatheter heart valve replacement for severe heart valve disease has increased exponentially. Although the bioprosthetic artificial heart valve (BHV) has similar fluid dynamics performance to the original heart valve compared with mechanical heart valve so that there is no need to take long-term anticoagulant drugs to prevent thromboembolism, transcatheter BHV replacement are still at risk for thrombosis during the first few months according to the clinical data. However, the use of antithrombotic drugs can also increase the risk of bleeding. Therefore, it is particularly important to improve the anticoagulant properties for the BHV itself. In this work, a kind of non-glutaraldehyde cross-linked BHV material with excellent antithrombotic ability has been prepared from carboxylated oxazolidine treated porcine pericardium (consisting of collagen, elastin and glycoprotein) with the further graft of the anticoagulant heparin sodium via hydrophilic modified chitosan. Along with the similar mechanical properties and collagen stability comparable to the glutaraldehyde cross-linked porcine pericardium (PP), these functional non-glutaraldehyde cross-linked PPs exhibit better biocompatibility, promoted endothelial proliferation and superior anti-calcification ability. More importantly, excellent anticoagulant activity can be observed in the hematological experiments in vivo and in vitro. In summary, these excellent performances make these functional non-glutaraldehyde cross-linked PPs great potentialities in the BHV applications. [ABSTRACT FROM AUTHOR]

A series of reactions between an oxazolidine ligand 2-(2-(pyridin-2-yl)oxazolidin-3-yl)-N-(pyridin-2-ylmethylene)ethanamine (POPME) and CdX2 (X = Cl, Br, I) salts with different M:L molar ratios (1:1 and 2:1) is experimentally studied to determine the most stable product of these reactions. All products are characterized by the elemental analysis, FTIR, Raman, and 1H NMR spectroscopy, and single crystal X-ray diffraction. Examinations reveal that only one product is formed from 1:1 and 2:1 M:L reactions between each cadmium(II) halide with POPME. The thermodynamic stability and charge distribution patterns of the compound containing bromide are analyzed by DFT and NBO. [ABSTRACT FROM AUTHOR]

Reactions of acetylene glycidyl ethers with butylamine and ethylene diamine lead to the oxirane ring opening according to the Krasusky rule with the formation of acetylene aminoalcohols. In reaction with thiourea the oxygen atom in the ring is replaced by sulfur leading to the corresponding thiiranes in a high yield. The synthesized compounds possess high antimicrobial activity. [ABSTRACT FROM AUTHOR]

A novel series of thiourea, carbamimidothioic acid, 4, 5-dihydrooxazole-2-thiol, oxazolidine-2thine, and 2-amino-1-phenylpropyl-2-chloroacetate derivatives was designed and synthesized using 2-amino-1-phenylpropan-1-ol (L-norephedrine) as a strategic starting material. The structures of the newly synthesized compounds were established by elemental analyses, IR, and H NMR and C NMR spectral data. The compounds were evaluated for their in vitro anticancer activity against various cancer cell lines. The corresponding acetamide, carbamimidothioic acid, and 2-2-amino-1-phenylpropyl-2-chloroacetate derivatives showed almost the same activity as the standard drug doxorubicin against human breast cancer cell line (MCF-7). Also, the acetamide and 2-thioxoimidazolidin-4-one derivatives exhibited higher activity than the reference drug doxorubicin against human colon cancer cell line (HCT 116). [ABSTRACT FROM AUTHOR]

number of compounds have been prepared in order to improve pharmacological roles of antihyperglycemic activity. In the present paper, a series of 3-benzyl-2-(4′-substituted phenyl)-4(5 H)-(4″-nitrophenyl amino)-1,3-oxazolidines ( 6a-e) were tested against hyperglycemia. Their antihyperglycemic activity was evaluated by streptozotocin (STZ) and sucrose-loaded (SLM) models. Compounds 6a, b, c, d, and e displayed significant reductions in blood glucose in the streptozotocin and sucrose loaded rat models. The purity of the synthesized compounds was characterized by means of IR, H-NMR, mass spectral and elemental analysis. [ABSTRACT FROM AUTHOR]

We have synthesized a series of (1R,2R,4S,5S,8S)-2,8-diaryl-4-(4-nitrophenyl)-1-aza-3,7-dioxabicyclo[3.3.0]octanes as a result of reaction of (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol with aromatic aldehydes. The structure of the compounds obtained was established on the basis of 1H NMR data. [ABSTRACT FROM AUTHOR]

The interaction of (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol with a series of symmetrical ketones has been studied. As a result isomeric oxazolidines are formed in a ratio of 85:15. These oxazolidines were shown to decompose readily under the action of hydrazine. [ABSTRACT FROM AUTHOR]