Heterocyclic Building Blocks-Thiazolidine

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Crystal structures of two 1,3-thiazolidin-4-one derivatives featuring sulfide and sulfone functional groups

The crystal structures of two closely related compounds, 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one, C15H18N2O3S, (1) and 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one 1,1-dioxide, C15H18N2O5S, (2), are presented. These compounds are comprised of three types of rings: thiazolidinone, nitrophenyl and cyclohexyl. In both structures, the rings are close to mutually perpendicular, with interplanar dihedral angles greater than 80 in each case. The thiazolidinone rings in both structures exhibit envelope puckering with the S atom as flap and the cyclohexyl rings are in their expected chair conformations. The two structures superpose fairly well, except for the orientation of the nitro groups with respect to their host phenyl ring, with a difference of about 10 between 1 and 2. The extended structure of 1 has two kinds of weak C – H?O interactions, giving rise to a closed ring formation involving three symmetry-related molecules. Structure 2 has four C – H?O interactions, two of which are exclusively between symmetry-related thiazolidinone dioxide moieties and have a parallel ‘give-and-take-fashion’ counterpart. In the other two interactions, the nitrophenyl ring and the cyclohexane ring each offer an H atom to the two O atoms on the sulfone group. Additionally, a C – H?pi interaction between a C – H group of the cyclohexane ring and the nitrophenyl ring of an adjacent molecule helps to consolidate the structure.

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Quinuclidine | C7H489N | ChemSpider

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Design, Synthesis and Biological Evaluation of 2-(naphthoyl) iminothiazolidin-4-ones as Potential Anticancer Agents

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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Quinuclidine | C7H234N | ChemSpider

Chemistry can be defined as the study of matter and the changes it undergoes. COA of Formula: C4H5NO3S. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.COA of Formula: C4H5NO3S, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S, introducing its new discovery.

In Vivo Selective Modulation of Tissue Glutathione in a Rat Mammary Carcinoma Model

Glutathione (GSH) is known to play a role in cellular sensitivity to some chemotherapeutic agents and to radiation. Depletion of cellular GSH has been demonstrated to result in enhanced toxicity of these drugs, and this approach is being explored in the clinic as a form of biochemical modulation, using the drug buthionine sulfoximine (BSO). The fact that some drug-resistant cell lines have increased glutathione levels, and that enhancing GSH concentrations in animal tissues protects against a variety of xenobiotic agents, suggest a different potential approach to improving anti-cancer therapy. We have examined the efficacy of the cysteine “pro-drug” L-2-oxothiazolidine-4-carboxylate (OTZ) at enhancing normal tissue versus tumor GSH. Animals were treated with OTZ or BSO, and the concentrations of GSH in normal tissues and tumor were measured. We found that the presence of the tumor itself decreased bone marrow GSH, but that OTZ significantly increased it in this setting. Interestingly, OTZ administration significantly depleted tumor GSH levels to the same level as did BSO. OTZ could offer a selective biochemical modulation of GSH.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C3H7NO2S, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 5908-62-3, name is 1,1-Dioxo-isothiazolidine. In an article£¬Which mentioned a new discovery about 5908-62-3

NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HBV INFECTION

The present invention provides novel compounds having general formula (I), wherein R1 to R4, A, W, Q and Y are as described herein, compositions including the compounds and methods of using the compounds.

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Electric Literature of 76186-04-4, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. Electric Literature of 76186-04-4, Name is (S)-4-Isopropylthiazolidine-2-thione,introducing its new discovery.

A versatile synthesis of various substituted taurines from vicinal amino alcohols and aziridines

Taurine and structurally diverse substituted taurines have been synthesized by peroxyformic acid, oxidation of the thiazolidine-2-thione intermediates generated from, vicinal amino alcohols or aziridines and carbon disulfide. The stereochemistry and mechanisms of the reactions are disscussed. The method is a salt-free and versatile route, convenient in terms of purification, and can be used to synthesize optically active substituted taurines.

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Quinuclidine | C7H722N | ChemSpider

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. Recommanded Product: 2682-49-7, C3H5NOS. A document type is Article, introducing its new discovery., Recommanded Product: 2682-49-7

Synthesis, characterization and acute anti-inflammatory evaluation of new mefenamic acid derivatives having 4-thiazolidinone nucleus

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug’s potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: Acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Recommanded Product: 2682-49-7, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2682-49-7

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Quinuclidine | C7H221N | ChemSpider

Chemistry can be defined as the study of matter and the changes it undergoes. Product Details of 18331-34-5. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.Product Details of 18331-34-5, Name is 5-Benzylidene-3-ethyl-2-thioxothiazolidin-4-one, molecular formula is C12H11NOS2, introducing its new discovery.

Introduction of Selenium to Heterocyclic Compounds. Part VII. Synthesis of 3-Alkyl-5-benzylidene- and 3-Alkyl-5-cinnamylidene-2-selenorhodanines

Five new 3-alkyl-5-benzylidene- and five new 3-alkyl-5-cinnamylidene-2-selenorhodanines were obtained by treatment of methylation products of appropriate rhodanines with H2Se. The stability of 2-thiazolinium salts with SCH3 or RNHCH3 group formed during methylation (cf. Scheme 2) is determined by substituents at C-5 and N-3 atoms.

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Quinuclidine | C7H827N | ChemSpider

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like name: 1,1-Dioxo-isothiazolidine, Name is 1,1-Dioxo-isothiazolidine. In a document type is Patent, introducing its new discovery., name: 1,1-Dioxo-isothiazolidine

BENZAZEPINE DERIVATIVES AS HISTAMINE H3 ANTAGONISTS

The present invention relates to novel benzazepine derivatives of structure (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. These compounds act as histamine H3 antagonists.

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Regioselective preparation and NMR spectroscopy study of 2-chloro-4-ethoxy-quinoline for the synthesis of 2-((3-aminopropyl)amino)quinolin-4(1H)-one

Herein, we describe the C4-ethoxylation of 2,4-dichloroquinoline to prepare 2-chloro-4-ethoxy-quinoline (3), which is a prominent intermediate used for the synthesis of 2-substituted quinolones. To achieve this goal, we studied different conditions for the reaction between 2,4-dichloroquinoline and sodium ethoxide. We discovered that the use of 18-crown-6 ether as an additive and dimethylformamide as the reaction solvent allowed us to obtain the desired product 3 in very good yield and selectivity. In addition, a definitive distinction between the C2 and C4 ethoxylation products was achieved using 1H?15N heteronuclear multiple bond correlation. Compound 3 is an intermediate used for the synthesis of 2-((3-aminopropyl)amino)quinolin-4(1H)-one, which displays peculiar behavior during 1H nuclear magnetic resonance analysis, such as the broadening of the H8 singlet and unexpected deuteration at the C8-position. Effort has been dedicated to understand these findings.

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Quinuclidine | C7H943N | ChemSpider

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Biosynthesis of galactan in mycobacterium tuberculosis as a viable TB drug target?

While target-based drug design has proved successful in several therapeutic areas, this approach has not yet provided compelling outcomes in the field of antibacterial agents. This statement remains especially true for the development of novel therapeutic interventions against tuberculosis, an infectious disease that is among the top ten leading causes of death globally. Mycobacterial galactan is an important component of the protective cell wall core of the tuberculosis pathogen and it could provide a promising target for the design of new drugs. In this review, we summarize the current knowledge on galactan biosynthesis in Mycobacterium tuberculosis, including landmark findings that led to the discovery and understanding of three key enzymes in this pathway: UDP-galactose mutase, and galactofuranosyl transferases GlfT1 and GlfT2. Moreover, we recapitulate the efforts aimed at their inhibition. The predicted common transition states of the three enzymes provide the lucrative possibility of multitargeting in pharmaceutical development, a favourable property in the mitigation of drug resistance. We believe that a tight interplay between target-based computational approaches and experimental methods will result in the development of original inhibitors that could serve as the basis of a new generation of drugs against tuberculosis.

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