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Ultrasound assisted site-selective alkynylation of 2,3,5,6-tetrachloropyridines under Pd/C[sbnd]Cu catalysis

A convenient synthetic method has been developed for accessing 2,6-dialkynyl-3,5-dichloropyridine derivatives in acceptable to good yields. The methodology involved ultrasound assisted site-selective alkynylation of 2,3,5,6-tetrachloropyridines under Pd/C[sbnd]Cu catalysis. A variety of terminal alkynes were employed in this C[sbnd]C coupling reaction to afford the corresponding 2,6-dialkynyl-3,5-dichloropyridine derivatives.

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Discovery of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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4-THIO SUBSTITUTED QUINOLINE AND NAPHTHYRIDINE COMPOUNDS

The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative.

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Discovery of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Agent for the control of plant-pathogenic organisms

Methods employing and compositions comprising, for the control of plant-pathogenic organisms, specified s-triazolo(4,3-a)quinoline compounds, some of which are claimed as novel compounds.

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Synthesis and evaluation of thiazolidinone-pyrazole conjugates as anticancer and antimicrobial agents

Aim: To synthesize a series of new thiazolidinone-pyrazole hybrids (5a-o) and assess their anticancer (in vitro and in vivo) and antimicrobial activities. Results: The compounds 5h (against Ehrlich ascites carcinoma cells), 5e and 5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except 5g and 5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency. The derivatives also showed moderate antimicrobial activity. Conclusion: The halogen atoms on various positions of the N-arylamino ring played an advantageous role in elevating the potency of the molecules. Thus, these conjugates could be used as a lead for further optimization to achieve promising therapeutics.

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Synthesis, characterization and anticonvulsant evaluation of new derivatives derived from 5-methoxy-2-mercapto benzimidazole

A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated for their anticonvulsant activity against yohimbine hydrochloride- induced epilepsy in comparison with 2mg/kg diazepam as a reference drug. The anticonvulsant effect of the intended compounds was assessed by their ability to delay the onset of seizure attack and by a reduction in the number of attacks. All of the synthesized compounds were found to have anticonvulsant activity.

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Isoxazole?a potent pharmacophore

Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group and found in many beta-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to possess significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, anti-inflammatory activity, antioxidant activity, anticancer activity, CNS (central nervous system) activity, antitubercular activity and miscellaneous activities like GABA (gamma-amino butyric acid) agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.

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Substituted quinolines and cinnolines as fungicides

A fungicidal method which comprises applying to the locus of a plant pathogen a fungicidally effective but non-phytotoxic amount of a compound of the formula (1) STR1 wherein: R1 to R4 are independently H, halo, (C1 -C4) alkyl, branched (C3 -C4) alkyl, halo (C1 -C4) alkyl, (C1 -C4) alkoxy, NO2, or HN2, at least two of R1 to R4 being H, or one of R2 to R4 is –NR7 –Y–Ar or O–Y–Ar and the rest of R1 to R4 are H; W is N, or CR5 ; R5 is H, CH3, Cl, O–Y–Ar, or –NR7 –Y–Ar; R6 is H, CH3, Cl, or Br; A is –O–Alk or –X–Y–Ar; Alk is a C2 -C18 saturated or unsaturated hydrocarbon chain, straight chain or branched, optionally substituted with halo, halo (C1 -C4) alkoxy, (C3 -C8) cycloalkyl, hydroxy, or acetyl; X is O, NR7, or CR8 R9, provided that if one of R2 to R5 is NR7 –Y–Ar or O–Y–Ar, then X–Y–Ar is an identical group; R7 is H, (C1 -C4) alkyl, or acetyl; R8 and R9 are independently H, (C1 -C4) alkyl, halo, or OH, or R8 and R9 combine to form a saturated or unsaturated carbocyclic ring comprising three to seven carbon atoms; Y is an alkylene chain 2 to 8 carbon atoms long that optionally includes an O, S, SO, SO2, or NR7 group, and optionally includes a saturated or unsaturated carbocyclic ring comprising three to seven carbon atoms, and optionally is substituted with (C1 -C3) alkyl, (C1 -C4) alkenyl, phenyl, (C3 -C8) cycloalkyl, hydroxy, halo, or acetyl; and Ar is an aryl group.

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Awesome Chemistry Experiments For (R)-2-Oxothiazolidine-4-carboxylic acid

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Ethanol ingestion impairs alveolar epithelial barrier function in rats

Alcohol abuse increases the incidence and severity of the Acute Respiratory Distress Syndrome (ARDS) in critically ill patients. In this study we examined a potential mechanism by which ethanol ingestion predisposes to acute lung injury by measuring alveolar epithelial barrier function in vivo as well as in cultured alveolar type II cells from ethanol-fed rats. We determined that rats fed the Lieber-DeCarli diet containing ethanol (36% of total calories) for 6 wks had decreased (p<0.05) net vectorial fluid transport, and increased (p<0.05) bi-directional protein permeability, across the alveolar epithelium in vivo compared to rats pair-fed an isocaloric Lieber-DeCarli diet without ethanol. However, ethanol-fed rats increased (p<0.05) fluid transport in response to epinephrine (10-5M) stimulation, suggesting that transcellular sodium transport was intact. In parallel, type II cells isolated from ethanol-fed rats and cultured in vitro for 6 days formed a more permeable monolayer, as reflected by increased (p<0.05) leak of 14C-inulin, compared to type II cells from control-fed rats that were cultured under identical conditions. However, type II cells from ethanol-fed rats had more (p<0.05) apical cation channel activity than type II cells isolated from control-fed rats, consistent with the preserved response to epinephrine in vivo. Finally, the alveolar epithelium of ethanol-fed rats that were supplemented with L-2-oxothiaxolidine-4-carboxylate (Procysteine), a glutathione precursor, had the same (p<0.05) net vectorial fluid transport and bi-directional protein permeability in vivo, and permeability to chronic ethanol ingestion increases alveolar epithelial permeability. Although the mechanism is unknown, it appears to involve predominantly intercellular rather than transcellular barrier disruption, and is mediated at least in part by glutathione depletion. This has important implications in understanding the pathogenesis of ARDS. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, SDS of cas: 19771-63-2, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 19771-63-2

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Properties and Exciting Facts About Thiazolidin-2-one

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COMPOSITION FOR MAINTAINING CHROMOSOMAL STABILITY OF PLURIPOTENT STEM CELLS, CONTAINING SMALL-MOLECULE COMPOUND

The present invention relates to a composition for maintaining the chromosomal stability of pluripotent stem cells, which contains a small-molecule compound, and more particularly, to a composition for maintaining the chromosomal stability of induced pluripotent stem cells, which contains a ROCK inhibitor, a MEK inhibitor, an ALK5 inhibitor or an antioxidant, which is capable of inhibiting chromosomal structural and numerical mutations or DNA damage during induction of induced pluripotent stem cell and the subsequent culture of the cells. The small-molecule compound-containing composition for maintaining the chromosomal stability of induced pluripotent stem cells increases the reprogramming rate and efficiency during production of induced pluripotent stem cells and exhibits excellent effects on the inhibition of chromosomal structural and numerical mutations or DNA damage. Thus, the composition of the present invention is very useful for the development of induced pluripotent stem cell therapeutic agents having excellent chromosomal stability.

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Reference of 7025-19-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.7025-19-6, Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, molecular formula is C6H7NO3S2. In a Article£¬once mentioned of 7025-19-6

Design, synthesis and biological evaluation of benzimidazole-rhodanine conjugates as potent topoisomerase II inhibitors

In this study, a series of benzimidazole-rhodanine conjugates were designed, synthesized and investigated for their topoisomerase II (Topo II) inhibitory and cytotoxic activities. The results from Topo II-mediated pBR322 DNA relaxation and cleavage assays showed that the synthesized compounds might act as Topo II catalytic inhibitors. Certain compounds displayed potent Topo II inhibition at 10 muM. The cytotoxic activities of these compounds against HeLa, A549, Raji, PC-3, MDA-MB-201, and HL-60 cancer cell lines were evaluated. The results indicated that these compounds exhibited strong antiproliferative activity. A good relationship was observed between the Topo II inhibitory potency and the cytotoxicity of these compounds. The structure-activity relationship revealed that the electronic effects, the phenyl group, and the rhodanine moiety were particularly important for the Topo II inhibitory potency and cytotoxicity.

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