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A library of novel naphthyl bearing 2-iminothiazolidin-4-ones (2-ITZDs) (2 a?2 q) was designed and synthesized through a facile route involving regioselective heterocyclization of unsymmetrical thioureas (1 a?1 q). The synthesis was achieved at ambient temperature in good to excellent yields under catalyst free conditions. The molecular structures of 2-ITZDs were elucidated by spectroscopic techniques such as FT-IR, 1H-NMR and 13C-NMR. X-ray structural data was used to establish the structure (2 o) unequivocally and to define the geometry of exo double bond. The in vitro anticancer activity of 2-ITZDs (2 a?2 q) was investigated in several human cancer cell lines (A549, LNCap, PC-3, MDA-MB-231, BxPC3, MIA PaCa2). All compounds showed cytotoxicity with IC50 values ranging from 6?23 muM in the tested cancer cell lines except MDA-MB-231. Compound 2 k (IC50=7 muM) and the homologous analog 2 q (IC50=6 muM) were found to be equipotent to 2 k and showed moderate cytotoxicity against human breast cell line (DA-MB-231). Furthermore, compound 2 k exhibited a medium permeability, enough metabolic stability and no significant inhibition of hERG channel. Compound 2 k inhibited cytochrome P450 activity below 50 % in 1 A2, 3 A4 and 2 C19, but not in 2 C9 and 2D6 at 10 muM. Structure-activity relationships (SAR) provided useful insights towards this class of compounds and tiled a way to design novel analogues with increased potency.

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Schiff bases [1]a,b were prepared from the reaction of 2-amino-5-mercapto-1,3,4-thiadiazole with aromatic aldehydes. In the present study a series of some four, five-and seven-membered heterocyclic compounds have been synthesized by the reaction of schiff bases [1]a,b with thioglycolic acid, chloroacetyl chloride, sodium azide or various anhydrides to give thiazolidinone [2]a, azetidinone [6]b, tetrazole [7]b and 1,3-oxazepine derivatives [14-16]b respectively, then compounds[2]a, [6,7]b and[14-16]b were reacted with Na2CO3 of distilled water as a solvent, then of ClCH2COOH was added to produce [3]a, [8,9]band[17-19]b. The compounds [3]a, [8,9]b and [17-19]b reacted with SOCl2 in the presence of Benzene to producing the compounds [4]a, [10,11]b and [20-22]b. Chemical modification of Poly(vinyl alcohol) were obtained by reaction of PVA with compounds [4]a, [10,11]b and [20-22]b using the Dimethyl formamide to produce compounds [5]a,[12,13]b and [23-25]b. The structure of the synthesized compounds were set by their analytical and spectral data such as, FTIR spectra,1H-NMR., UV-Vis Spectroscopy and Elemental analysis (CHNS). Finally study antibacterial activity screened via two types of bacteria. Anticancer activity also examined for all modifier polyvinyl alcohol.

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Compounds having the following formula (I) and methods of their use and preparation are disclosed:

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A highly efficient three-component reaction has been developed for the synthesis of thiazolidinones involving the reaction of 2-amino-1-phenylethanone hydrochloride with an aromatic aldehyde and mercaptoacetic acid in the presence of diisopropylethylamine in a single pot. Critically, this reaction exhibited excellent chemoselectivity, with the nitrogen atom of the 2-amino-1-phenylethanone component reacting selectively with the aromatic aldehyde to give the corresponding Schiff base. Nucleophilic attack at the carbon of the Schiff base by the sulfur atom of mercaptoacetic, followed by a cyclocondensation reaction between the nitrogen and the carboxylic acid moiety afforded the desired thiazolidinones, which were fully characterized by spectroscopic techniques.

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The ongoing spread of multidrug-resistant bacteria demands an intensive search for new antibacterial agents. In the present study, a series of new 1,3-thiazolidin-4-ones has been synthesized and investigated for its in vitro antibacterial activity. The most potent antibacterial compound 4c was found to be active, at low micromolar range, against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and the pneumonic plague causative agent Yersinia pestis with minimum inhibitory concentrations of 5 muM, 2.5 muM, 2.5 muM and 5 muM, respectively. Compound 4c showed the ability to kill E. faecalis JH212 strain with a minimum bactericidal concentration of 5 muM. Furthermore, compounds 9b and 10a inhibited the biofilm formation in S. epidermidis, where they showed 70% to 80% inhibition at a concentration of 40 muM.

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The invention discloses a […] his preparation method. Ealy grewe department he a kind of effective specific glucose ceramide synthase inhibitor, can be used for treating I treat Gaucher spear. The invention provides a method for synthesizing […] he, the preparation method comprises: 1, 4 – benzodioxane – 6 – formaldehyde with a chiral ligand generating diastereoselective Aldol reaction, of after the reduction reaction, and then by the substitution and Staudinger reaction, then by the amidation reaction ealy grewe department he. The method raw materials are easy, simple operation, high yield and purity, and is easy for industrial production. (by machine translation)

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Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer’s disease, atherosclerosis. Also disclosed are processes for making such novel compounds.

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The present invention relates to a process for preparing cyanimino-1,3-thiazolidines, which are important building blocks for the preparation of crop protection active ingredients and pharmaceuticals, by the following scheme: where A is an alkali metal and X represents an acid radical.

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The present invention provides a including fluorine cyanogen imine thiazolidine substituted wicked two zuozuo kinds insecticide, the structure shown in formula I: The formula I compound Diamondback moth, Spodoptera exigua insecticidal, rice and the galenical, hot pepper anthrax bacteria, rice sheath blight fungus, Chinese rose inhibition of downy mildew and the like, can be used as agricultural or forestry plant pest control of the saw. (by machine translation)

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Maresin 1 is a potent anti-inflammatory and pro-resolving lipid mediator derived from docosahexaenoic acid. The total synthesis of maresin 1 is achieved in 10 steps and in 7% overall yield. The Evans-Nagao aldol reaction between (2E,4E)-5-bromopenta-2,4-dienal and different chiral auxiliaries is investigated. The reported synthesis is efficient and highly stereoselective, affording multi-milligram quantities of this biologically interesting lipid mediator.

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