Heterocyclic Building Blocks-Thiazolidine

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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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Quinuclidine – Wikipedia,
Quinuclidine | C7H249N | ChemSpider

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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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Quinuclidine – Wikipedia,
Quinuclidine | C7H845N | ChemSpider

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, SDS of cas: 19771-63-2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S

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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Quinuclidine – Wikipedia,
Quinuclidine | C7H676N | ChemSpider

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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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Quinuclidine – Wikipedia,
Quinuclidine | C7H184N | ChemSpider

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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Quinuclidine – Wikipedia,
Quinuclidine | C7H809N | ChemSpider

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Design, synthesis, anticancer screening, docking studies and in silico ADME prediction of some beta-carboline derivatives

Background: Medicinal interest has focused on beta-carbolines as anticancer agents. Methodology/Results: Several beta-carbolines were designed, synthesized and evaluated for their cytotoxic activity against MCF-7 and A-549 cancer cell lines using MTT assay. Compounds 13a, 13c, 13d and 20a were the most promising showing high selectivity indices. Compounds 13c and 20a showed potent inhibition of topoisomerase (topo-I) and kinesin spindle protein (KSP/Eg5 ATPase) which was confirmed by their docking results into the active site of both enzymes. In silico physicochemical calculations predicted that compounds 13a, 13d and 20a obeyed Lipinski’s rule of five. Conclusion: Compounds 13c and 20a are multitarget anticancer leads that act as potent inhibitors for both topo-I and/or KSP ATPase.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H204N | ChemSpider

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New progress in azole compounds as antimicrobial agents

The increasing incidence of microbial resistance and newly emerging pathogens have become a serious challenge for public health. More and more efforts have been directed to the development of new antimicrobial agents with distinct mechanisms from the well-known classes of clinical drugs. The extensive clinical utilization of azole-based medicinal drugs has evoked numerous attentions, and their researches and developments have been a quite rapid developing and active highlight topic with an infinite space. Consideration of our researches on azole compounds and other literature in recent three years, this review scientifically reviewed the new progress of azole derivatives as antibacterial, antifungal, antitubercular and antiviral agents, including mono-nitrogen azoles (oxazoles, thiazoles and carbazoles), bis-nitrogen azoles (imidazoles, pyrazoles and benzimidazoles) and tri-nitrogen azoles (triazoles and benzotriazoles) as well as tetrazole derivatives. It was hoped that this review would be helpful for the design and development of highly efficient azole derivatives with high bioactivity and low toxicity.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H494N | ChemSpider

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Investigations on 1,3-Thiazines, 43. – Newman-Kwart Rearrangement in the Course of Thiocarbazoylation of Tetrahydro-2H-1,3-thiazin-2-one and Thiazolidin-2-one

Thiocarbazoylation of tetrahydro-2H-1,3-thiazin-2-one (1) with thiocarbazic acid chlorides leads to N-thiocarbazoyl derivatives 5 and N-carbazoyl-tetrahydro-2H-1,3-thiazin-2-thiones 8, which are interpreted as products of an O-thiocarbazoylation to 6, subsequent Newman-Kwart rearrangement to 7 and final S->N transcarbazoylation.Thiocarbazoylation of thiazolidin-2-one (9) yields an isolable Newman-Kwart rearrangement product 12 and its product 13 of S->N transcarbazoylation.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H306N | ChemSpider

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Design, synthesis and application of a new type of bifunctional Le-Phos in highly enantioselective gamma-addition reactions of N-centered nucleophiles to allenoates

A novel class of cyclic phosphine derived bifunctional catalysts (Le-Phos) is reported, which can be readily prepared from inexpensive and commercially available starting materials and exhibit good performances in enantioselective gamma-addition reactions of N-centered nucleophiles and allenoates under mild conditions. The salient features of this reaction include high product yields, good enantioselectivity, mild reaction conditions, and broad substrate scope and gram-scale scalability.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H417N | ChemSpider

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Mannich bases in medicinal chemistry and drug design

The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H429N | ChemSpider