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Chlamydocin-hydroxamic acid analogues were designed and synthesized as histone deacetylase (HDAC) inhibitors based on the structure and HDAC inhibitory activity of chlamydocin and trichostatin A. Chlamydocin is a cyclic tetrapeptide containing an epoxyketone moiety in the side chain that makes it an irreversible inhibitor of HDAC. We replaced the epoxyketone moiety of chlamydocin with hydroxamic acid to design potent and reversible inhibitors of HDAC. In addition, a number of amino-cycloalkanecarboxylic acids (Acc) are introduced instead of the simple amino-isobutric acid (Aib) for a variety of the series of chlamydocin analogues. The compounds synthesized were tested for HDAC inhibitory activity and the results showed that many of them are potent inhibitors of HDAC. The replacement of Aib residue of chlamydocin with an aromatic amino acid enhances the in vivo and in vitro inhibitory activity. We have carried out circular dichroism and molecular modeling studies on chlamydocin-hydroxamic acid analogue and compared it with the solution structure of chlamydocin.

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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I) wherein R1, A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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The development and synthesis of potent p38alpha MAP kinase inhibitors containing a pyridazinone platform is described. Evolution of the p38alpha selective pyridopyridazin-6-one series from the p38alpha/beta dual inhibitor 2H-quinolizin-2-one series will be discussed in full detail.

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The palladium-catalyzed cross-coupling of highly functionalized organobismuthanes with 2-halo(or 2-triflyl)pyridines, -pyrimidines, -pyrazines, and -pyridazines is reported. The reaction tolerates numerous functional groups, including aldehydes. The synthesis of a shelf-stable (formylphenyl)bismuth reagent and its use in a cross-coupling reaction is also described. The palladium-catalyzed cross-coupling of highly functionalized organobismuthanes with 2-halo(or 2-triflyl)pyridines, -pyrimidines, -pyrazines, and -pyridazines is reported. The reaction tolerates numerous functional groups, including aldehydes. The synthesis of a shelf-stable (formylphenyl)bismuth reagent and its use in cross-coupling reactions is also described. Copyright

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The present invention provides a hepatitis c inhibitor spiro compound and its use in medicine. The compound of formula (I) compound shown by the formula (I) as shown in the stereo isomers, geometric isomers, tautomers, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug. In addition, the invention also provides a pharmaceutical composition, said compound and said pharmaceutical composition for inhibiting HCV replication and inhibit HCV virus protein function of at least one of the use, and the compounds and pharmaceutical composition useful for the prevention, treatment, treatment or alleviation of patient’s HCV infection or hepatitis c treatment of diseases. (by machine translation)

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wherein R1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino, R2 is hydroxy, protected hydroxy, halogen, amino or protected amino, R3 is hydrogen or an organic group, R4 R is hydrogen or lower alkyl, R8 is hydrogen or lower alkyl, and –Z– is –O– or a group of the formula: STR2 (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.

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The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

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The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

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14-Sep-2021 News Our Top Choice Compound: 2164-61-6

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The possible use of some dinuclear rhenium complexes as sensitizers for dye sensitized solar cells (DSSCs) has been investigated. They have general formula [Re2(mu-X)(mu-Y)(CO)6(mu-pyridazine-4-COOH)], with X = Y = Cl (1), X = H, Y = benzoato (2), and X = H, Y = 4-diphenylaminobenzoato (3). An original synthetic strategy has been set for preparing the hydrido-carboxylato derivatives 2 and 3. They have been indicated by DFT and TD-DFT computations as the most promising dyes, endowed with good light harvesting capability. The complexes have absorption maxima in the range of 405-443 nm, on TiO2 films, arising from metal-to-ligand-charge transfer transitions. Cyclic voltammetry experiments have been performed on the derivatives containing the methyl ester of the pyridazine-4-COOH acid, showing electrochemical band gaps in the range of 2.25-1.63 eV. The best DSSC results have been obtained using complex 3, with an overall solar-to-electric conversion efficiency of 1.0%. Noteworthy the presence of a hydrido ligand did not show any detrimental effect on the stability of the sensitizers under the operating conditions.

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Disclosed are compounds having the formula: (I) wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

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