Can You Really Do Chemisty Experiments About 1,1-Dioxo-isothiazolidine

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USE OF AZABICYCLO HEXANE DERIVATIVES

The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof, wherein: G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxyl, cyano, C1-4alkyl, haloC1-4alkyl, C1-4 alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4 alkyl; R3 I s C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; in the manufacture of a medicament for the treatment of a somatoform disorder such as body dysmorphic disorder or hyperchondriasis, bulimia nervosa, anorexia nervosa, binge eating, paraphilia and nonparaphilic sexual addictions, Sydeham’s chorea, torticollis, autism, a movement disorder including Tourette’s syndrome; and in the manufacture of a medicament for the treatment of premature ejaculation.

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

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MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators

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Properties and Exciting Facts About 26364-65-8

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Anomalous One-pot Transformation of 3-Dimethoxymethyl-2-(N-cyanoimino)thiazolidine into 6-Unsubstituted 2,4-Diamino-s-triazines by the Reaction with Amines

3-Dimethoxymethyl-2-(N-cyanoimino)thiazolidine 1e reacts with secondary amines to afford 2,4-diamino-s-triazines 4 unexpectedly, while the triazine 5 bearing different amino groups at 2 and 4 positions is selectively obtained by the reaction with a mixture of two kinds of amines.

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More research is needed about Thiazolidin-2-one

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Nitroimidazoles: Part V – 1-(1-Methyl-5-nitroimidazol-2-yl)-1,2,4-triazolidin-3,5-diones and Analogues

Condensation of 1-methyl-2-methylsulphonyl-5-nitroimidazole (1) with the sodium salts of triazolindiones affords the derivatives 2a-i; similiar reaction with the sodium salts of thiazolidinone, 2-iminothiazolidine, pyrrolidinone, oxazolidinone and its 2-methyl and 2-chloromethyl analogues leads to the formation of products 3-8 respectively.Under the reaction conditions 3 is opened by dimethylamide ion to form 10, and 6 by methyl sulfinate ion to provide 13 respectively.Additionally, 6 is hydrolysed to the amine (12).Cyclic sulphamides undergo reaction with 1 to provide nitroimidazoles (23-28).

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Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives

In this study, a novel benzothiazol- and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure-activity relationship analysis displayed that compound 8t with a 5,6-difluorosubstituted benzothiazole was found to be a potent inhibitor of Gram-positive pathogens, and exhibited some potential against drug-resistant bacteria and without cytotoxicity in therapeutic concentrations. In addition, molecular docking studies indicated that Staphylococcus aureus methionyl-tRNA synthetase might be the possible target of these compounds. Taken together, the present study provides an effective entry to the synthesis of a good lead for subsequent optimization and a new small molecule candidate drug for antibacterial therapeutics.

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Extended knowledge of Thiazolidin-2-one

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Synthesis, characterization and biological evaluation of thioureas, acylthioureas and 4-thiazolidinones as anticancer and antiviral agents

In this study, thiourea derivatives [1-4] were synthesized by using 2-amino-4-substituted pyridine compounds and these compounds have been used as the starting materials for synthesis of 2-imino-1,3-thiazolidin-4-one ring [5, 6]. Two different procedures for 4-thiazolidinone ring closure and synthesis method were optimized. The synthesized compounds were identified by the help of elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectral data while the purities of them were proved with TLC. Synthesized compounds were evaluated for their antiviral and anticancer activity. Antiviral activity against Murine norovirus, Yellow fever, Enterovirus and Chikungunya strains of the test compounds were investigated and EC50 values of these compounds were determined higher than 0,3 muM. Cytotoxicity of test compounds was examined on NIH3T3 cell line. When the anticancer activity of test compounds was examined against PC-3, A549, HeLa, HT-29, MCF-7, SJSA1 and K562 cell lines, the percent proliferation values of these compounds were observed over 61% for all cell lines.

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More research is needed about Thiazolidin-2-one

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Modified Mg: Al hydrotalcite in the synthesis of oxazolidin-2-ones

The modified Mg: Al (3: 1) hydrotalcite has been found to be an efficient catalyst in the conversion of carbamates into oxazolidin-2-ones under mild reaction conditions. A wide variety of oxazolidin-2-ones were obtained with excellent chemical yield. The Royal Society of Chemistry 2005.

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A hydrogen peroxide responsive prodrug of Keap1-Nrf2 inhibitor for improving oral absorption and selective activation in inflammatory conditions

Transcription factor Nuclear factor erythroid 2-related factor 2 (Nrf2) and its negative regulator, the E3 ligase adaptor Kelch-like ECH-associated protein 1 (Keap1), control the redox and metabolic homeostasis and oxidative stress. Inhibitors of Keap1-Nrf2 interaction are promising in oxidative stress related inflammatory diseases but now hit hurdles. By utilizing thiazolidinone moiety to shield the key carboxyl pharmacophore in Keap1-Nrf2 inhibitor, a hydrogen peroxide (H2O2)-responsive prodrug pro2 was developed. The prodrug modification improved the physicochemical properties and cell membrane permeability of the parent drug. Pro2 was stable and stayed inactive under various physiological conditions, while became active by stimulation of H2O2 or inflammation derived reactive oxygen species. Moreover, pro2 exhibited proper pharmacokinetic profile suitable for oral administration and enhanced anti-inflammatory efficiency in vivo. Thus, this novel prodrug approach may not only provide an important advance in the therapy of chronic inflammatory diseases with high level of H2O2, but also offer a fresh solution to improve the drug-like and selectivity issues of Keap1-Nrf2 inhibitors.

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Archives for Chemistry Experiments of Thiazolidin-2-one

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Synthesis, characterization, antibacterial and antiepileptic studies of some novel thiazolidinone derivatives

In the quest of finding new drug leads with potential antibacterial and antiepileptic activities, synthesis of thiazolidinone derivatives 6(a?c) is reported which are obtained from 5-(4-chlorobenzylidine)-3-[4-(7-chloroquinoline-4-ylamino]propyl)-2-imino-thiazolidin-4-one derivatives by applying appropriate synthetic route. These compounds 6(a?c) were evaluated for antibacterial and antiepileptic activities. Compound 6a having good lipophilicity is found to be most active.

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Something interesting about 19771-63-2

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Carvacrol codrugs: A new approach in the antimicrobial plan

Objective: The increasing prevalence of antibiotic-resistant bacterial infections led to identify alternative strategies for a novel therapeutic approach. In this study, we synthesized ten carvacrol codrugs – obtained linking the carvacrol hydroxyl group to the carboxyl moiety of sulphur-containing amino acids via an ester bond – to develop novel compounds with improved antimicrobial and antibiofilm activities and reduced toxicity respect to carvacrol alone. Method: All carvacrol codrugs were screened against a representative panel of Gram positive ( S. aureus and S. epidermidis), Gram negative (E. coli and P. aeruginosa) bacterial strains and C. albicans, using broth microdilution assays. Findings: Results showed that carvacrol codrug 4 possesses the most notable enhancement in the anti-bacterial activity displaying MIC and MBC values equal to 2.5 mg/mL for all bacterial strains, except for P. aeruginosa ATCC 9027 (MIC and MBC values equal to 5 mg/mL and 10 mg/mL, respectively). All carvacrol codrugs 1-10 revealed good antifungal activity against C. albicans ATCC 10231. The cytotoxicity assay showed that the novel carvacrol codrugs did not produce human blood hemolysis at their MIC values except for codrugs 8 and 9. In particular, deepened experiments performed on carvacrol codrug 4 showed an interesting antimicrobial effect on the mature biofilm produced by E. coli ATCC 8739, respect to the carvacrol alone. The antimicrobial effects of carvacrol codrug 4 were also analyzed by TEM evidencing morphological modifications in S. aureus, E. coli, and C. albicans. Conclusion: The current study presents an insight into the use of codrug strategy for developing carvacrol derivatives with antibacterial and antibiofilm potentials, and reduced cytotoxicity.

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