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The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I STR1 wherein Ar, R, R 1 and R. sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1637NO – PubChem

 

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Organocatalytic conjugate addition of thiols to R-substituted N-acryloyloxazolidin-2-ones followed by asymmetric protonation has been studied in the presence of cinchona alkaloid derived thioureas. Both of the enantiomers are accessible with the same level of enantioselectivity using pseudoenantiomeric quinine/quinidine derived catalysts. The addition/protonation products have been converted to useful biologically active molecules. 2011 American Chemical Society.

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1,3-N,O-Chelating ligands are ubiquitous in nature owing to their occurrence as alpha-chiral amino acids in metalloproteins. These structural units also display diverse coordination modes, which lend themselves to applications in catalysis as well as novel fundamental stoichiometric reactivity, including the activation of inert bonds. This review comments on recent developments in N,O-ligated late transition metal complexes with an emphasis on preparation, characterization, and reactivity.

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Application of 22625-57-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 22625-57-6, molcular formula is C4H6ClNO2, introducing its new discovery.

Objective: The main objective of our present study, is to potentiate the antibacterial activity of biphenyl chalcones and oxazolidinones, thus in order to achieve the potent antibacterial agents, we coupled both derivatives by using green chemistry approach for Buchwald?s protocol under ultrasound irradiation. Methodology: Ultrasonication technique was used to couple a series of 24 novel bromo-biphenyl-chalcone derivatives and 5-chloromethyl-oxazolidinone in the presence of copper iodide (CuI) (10 mol %) for the amidation of chalcones and (±)-trans-1,2-diaminocyclohexane was used to solubilize CuI and potassium carbonate (K2CO3) as base, which provided the products in good yields after short reaction times under mild conditions. Results and Discussion: Herewith we report the synthesis of 24 novel oxazolidinone-biphenyl chalcone hybrid derivatives (7a-7x). All the synthesized compounds were characterized by spectral data and evaluated for in vitro antibacterial and antifungal activities. Antibacterial and antifungal activities were tested using the serial dilution method. From the screening studies it was observed that compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria at 3.125 mug/ml when compared to the standard drugs ciprofloxacin and linezolid and were as other compounds showed moderate to weak activities. In case of antifungal studies the compounds 7e-7g showed moderate activities at 12.5 mug/ml compared to standard fluconazole and whereas other compounds showed weak activities. Conclusion: We have developed an experimentally simple, efficient, short time and high yielding CuI-mediated N-arylation of oxazolidinones under ultrasound irradiation with a simple set up at room temperature. This approach would be a worthwhile in the development of green chemistry protocols. Compounds 7c to 7g have shown significant antibacterial activities against the both the strains of gram-positive and gram-negative bacteria.

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Reference:
Oxazolidine – Wikipedia,
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Compounds, compositions, methods of making, and methods of using analogues of (-)-picropodophyllin, as well as a transgenic animal model and its use for identifying anticancer agents.

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Electric Literature of 189028-93-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.189028-93-1, Name is (S)-1-(4-Fluorophenyl)-5-(2-oxo-4-phenyloxazolidin-3-yl)pentane-1,5-dione, molecular formula is C20H18FNO4. In a Patent,once mentioned of 189028-93-1

This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity at large scale production. Aromatic ketones represented by formula (I) [wherein, R1 are selected from hydrogen atom, halogen atom, lower alkyl group etc. R2 is -(CH2)n-R3 [wherein, n is 1 to 5 integer. R3 are selected from hydrogen atom, halogen atom, lower alkoxycarbonyl group etc. and formula (II) and (III). {wherein, R4 is selected from lower alkyl group (1 to 5 carbon atom) etc. R5 and R6 are the same or different and are selected from hydrogen atom, halogen atom, lower alkyl group etc.}]] are reduced by sodium borohydride, chlorotrimethylsilane and optically active 2-[bis(4-methoxyphenyl)hydroxymethyl]pyrrolidine represented by formula (IV) to give optically active alcohol represented by formula (V) stereoselectively. (wherein, R1 and R2 are as defined above.)

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Oxazolidine – Wikipedia,
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The molecular determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogues. All three leads are based on an N-methylglycinamide scaffold, with its two amine groups condensed with three different functionalities. The three functionalities and the CH2 group of the glycinamide scaffold were separately modified. The replacement of the pentafluorobenzene or cyclohexylbenzene, or replacing the benzene ring of the aromatic carboxylic or hydroxamic acid motif with heterocyclic components (containing nitrogen and oxygen elements) all decreased potency. Notably, the Ala-linker analogues, 1a and 2v, and the Pro-based derivative 5d, all with (R)-configuration at the chiral center, had improved inhibitory activity and selectivity against STAT3 DNA-binding activity in vitro, with IC50 of 3.0 ± 0.9, 1.80 ± 0.94, and 2.4 ± 0.2 muM, respectively. Compounds 1a, 2v, 5d, and other analogues inhibited constitutive STAT3 phosphorylation and activation in human breast cancer and melanoma lines, and blocked tumor cell viability, growth, colony formation, and migration in vitro. Pro-based analogue, 5h, with a relatively polar tetrahydropyranyl (THP) ring, instead of the cyclohexyl, showed improved permeability. In general, the (R)-configuration Pro-based analogs showed the overall best profile, including physicochemical properties (e.g., microsomal metabolic stability, Caco-2 permeability), and in particular, 5d showed improved tumor-cell specificity.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H1918NO – PubChem

 

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(Chemical Equation Presented) The Midas touch: 1,3-Dienes undergo hydroamination with carbamates and sulfonamides in the presence of Ph 3PAuOTf catalyst under mild conditions (see scheme). The carbobenzyloxy (Cbz) group is readily removed from the product, and the reaction is thus an efficient method to prepare allylic amines.

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Oxazolidine – Wikipedia,
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The invention relates to the compounds of formula I STR1 pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.

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Oxazolidine – Wikipedia,
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Hydroamination and hydrothiolation are the most efficient and completely atom-economical process to construct important enamine and vinyl sulfide intermediates in pharmaceutical and organic chemistry. The cyclic trimeric phosphazene base (CTPB) showed great catalytic activity for the anti-Markovnikov stereoselective hydroamination and hydrothiolation of alkynes in good to excellent yields. A broad substrate scope of alkynes and nucleophiles was demonstrated, including aryl and heteroaryl alkynes, terminal and internal alkynes, different N-heterocycles, thiols and thiophenols. This versatile and cost-efficient approach with good stereoselectivity and excellent functional group tolerance provided new opportunity for the organocatalyzed hydrofunctionalization of alkynes.

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