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Novel bifunctional thiourea-ammonium salt catalysts derived from amino acids: Application to highly enantio- and diastereoselective aza-Henry reaction

The development of new efficient and easily accessible catalysts has been one of the focuses in asymmetric phase-transfer catalysis. In this paper, a novel class of chiral bifunctional thiourea-ammonium phase-transfer catalysts were synthesized from commercially available alpha-amino acids. The structural modularity of these catalysts permits facile tunings to achieve optimum results, which was demonstrated in catalyzing the aza-Henry reaction with excellent enantioselectivities (up to 99.5% ee) and diastereoselectivities (up to >25:1 dr).

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IMIDAZOPYRIDINE DERIVATIVES AS ACID PUMP ANTAGONISTS

This invention relates to newly identified imidazopyridine compounds of formula (I), to the use of such compounds in therapy and to their production.

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HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER’S DISEASE

The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer’s disease.

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Syntheses, characterization and evaluation of some 3-(Benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-ones as antimicrobial agents

Background: The increasing predominance of microbial resistance towards available antimicrobial drugs urges the need to develop novel antimicrobial agents that will be effective against resistant bacteria and fungi. Objective: A series of 3-(benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-one derivatives were synthesized as pharmacophore hybrid of benzothiazole and thiazolidin-4-one moieties as exclusive antimicrobial agents. Methods: Proposed compounds were synthesized by four step reactions. First three steps involved synthesis of phenylthiourea, benzothiazol-2-ylamine and Schiff?s base srespectively. Finally, Schiff`s baseswere cyclized in the presence of thioglycolic acid to yield 4-thiazolidinone derivatives (2a-g), characterized by spectroscopic and elemental analysis. Resulted compounds were evaluated for their in vitro antimicrobial activities against four bacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and two fungal (A. niger and P. crysogenum) strains using agar diffusion method. The minimum inhibitory concentrations (MIC) of the synthesized compounds were also determined by tube dilution method. Results: All the compounds displayed good to moderate antimicrobial activity. Compound 2d was found most potent against Bacillus subtilis (MIC25mug/ml), whereas compound 2e was most active (MIC 25mug/ml) against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Conclusion: The compounds having electron-withdrawing groups in the phenyl ring exhibited promising activity. A correlation between the antimicrobial activity and Log P was also established. Most active compounds can be considered as the potential antibacterial agents and deserve further investigation for their pharmacological and toxicological profiling.

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STRUCTURAL CHARACTERIZATION OF SOME SUBSTITUTED AZOLIDINE MOLECULES: UPS PHOTOELECTRON SPECTROSCOPIC STUDIES

The He(I) photoelectron spectra of some heterocyclic penta-atomic rings containing carboamido, thiocarbamido or selenocarbamido groups are reported.Ab initio and CNDO/2 computational methods have been used to assign the first four ionized molecular orbitals, by comparison with previously studied related molecules.Structural effects in homologous series of compounds, particularly conjugation between N and C=Y (Y=O, S, Se) moiety, and the through-space interaction between ring heteroatoms are analyzed.

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BROMODOMAIN INHIBITORS

Provided are compounds of formula (I), wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I)

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5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, biological evaluation, and molecular docking studies

Background: Infectious diseases symbolize a global consequential strain on public health security and impact on the socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in crucial need for the discovery and development of novel entity for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using classical methods of organic synthesis. Results: All 20 synthesized compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species. It should be mentioned that all compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Furthermore, 18 compounds appeared to be more potent than streptomycin against Staphylococcus aureus, Enterobacter cloacae, Pseudomonas aeruginosa, Listeria monocytogenes, and Escherichia coli. Three the most active compounds 4h, 5b, and 5g appeared to be more potent against MRSA than ampicillin, while streptomycin did not show any bactericidal activity. All three compounds displayed better activity also against resistant strains P. aeruginosa and E. coli than ampicillin. Furthermore, all compounds were able to inhibit biofilm formation 2- to 4-times more than both reference drugs. Compounds were evaluated also for their antifungal activity against eight species. The evaluation revealed that all compounds exhibited antifungal activity better than the reference drugs bifonazole and ketoconazole. Molecular docking studies on antibacterial and antifungal targets were performed in order to elucidate the mechanism of antibacterial activity of synthesized compounds. Conclusion: All tested compounds showed good antibacterial and antifungal activity better than that of reference drugs and three the most active compounds could consider as lead compounds for the development of new more potent agents.

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Progress and prospects on DENV protease inhibitors

New treatments are desperately required to combat increasing rate of dengue fever cases reported in tropical and sub-tropical parts of the world. Among the ten proteins (structural and non-structural) encoded by dengue viral genome, NS2B-NS3 protease is an ideal target for drug discovery. It is responsible for the processing of poly protein that is required for genome replication of the virus. Moreover, inhibitors designed against proteases were found successful in Human Immuno-deficiency Virus (HIV) and Hepatitis C Virus (HCV). Complete molecular mechanism and a survey of inhibitors reported against dengue protease will be helpful in designing effective and potent inhibitors. This review provides an insight on molecular mechanism of dengue virus protease and covers up-to-date information on different inhibitors reported against dengue proteases with medicinal chemistry perspective.

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Electric Literature of 26364-65-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.26364-65-8, Name is 2-Cyanoimino-1,3-thiazolidine, molecular formula is C4H5N3S. In a Patent£¬once mentioned of 26364-65-8

An antibiotic anticancer activity method for the preparation of compounds (by machine translation)

An antibiotic anticancer active compound preparation method, comprising: cooling the ice, compound HRB-1365-0 : C4H6N2 S2, compound HRB-1365-1 : C2H7NS, and water, stirring reaction in alkaline conditions, filtration to obtain white solid, that is, for the compound HRB-1365-2 : C4H5N3S; under ice cooling, compound HRB-1365-2 : C4H5N3S, compound HRB-1365-1 : C2H7NS, triethylamine, stirring reaction in the methanol, after the completion of reaction, methanol concentrated under reduced pressure, the residue is washed with water, filtered, to obtain yellow solid is the compound HRB-1365: C6H9N3 S2; compound HRB-1365: C6H9N3 S2 of ethanol solution under stirring in the ice bath to cool down, to the drying to obtain the hydrogen chloride gas is introduced, after the saturation, continuing to stir, filtering and drying the obtained product. (by machine translation)

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Bis(benzofuran?thiazolidinone)s and bis(benzofuran?thiazinanone)s as inhibiting agents for chikungunya virus

There are currently still no approved antiviral drugs to treat or prevent chikungunya virus (CHIKV) infections despite the fact that this arbovirus continues to cause outbreaks in Africa, Asia, and South- and Central-America. Thus 20 new conjugated compounds in the families of bis(benzofuran?1,3-thiazolidin-4-one)s and bis(benzofuran?1,3-thiazinan-4-one)s were designed based on the structural features of suramin. These new compounds were synthesized by chemical methods and their structures were confirmed spectroscopically. In CPE reduction assays, six of these new bis-conjugates inhibited CHIKV replication in Vero E6 cells with EC50 in the range of 1.9?2.7 muM and selectivity index values of ?75 or higher. These results and compounds provide a starting point for further optimization, design, and synthesis of new antiviral agents for this (re)emerging disease.

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