Properties and Exciting Facts About 1,1-Dioxo-isothiazolidine

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PYRAZOLO [1,5-A] PYRIMIDINES AS ANT1VIRAL AGENTS

The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections

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Efficient synthesis of five and six member sultam

A robust approach for the synthesis of five and six member sultam is achieved employing commercially available starting materials and reagents. The use of simplest reactions without any critical parameter is the key strength of this route applicable on large scale synthesis.

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Heterocycle compounds with antimicrobial activity

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple re-sistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Methods: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadia-zole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

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Development of a novel sulfonate ester-based prodrug strategy

A self-immolative gamma-aminopropylsulfonate linker was investigated for use in the development of prodrugs that are reactive to various chemical or biological stimuli. To demonstrate their utility, a leucine-conjugated prodrug of 5-chloroquinolin-8-ol (5-Cl-8-HQ), which is a potent inhibitor against aminopeptidase from Aeromonas proteolytica (AAP), was synthesized. The sulfonate prodrug was considerably stable under physiological conditions, with only enzyme-mediated hydrolysis of leucine triggering the subsequent intramolecular cyclization to simultaneously release 5-Cl-8-HQ and form gamma-sultam. It was also confirmed that this gamma-aminopropylsulfonate linker was applicable for prodrugs of not only 8-HQ derivatives but also other drugs bearing a phenolic hydroxy group.

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Synthesis, characterization and antimicrobial evaluation of novel quinoline based 2-azetidinones and 4-thiazolidinones

The present work describes the synthesis of a series of quinoline based 4-thiazolidinone and 2-azetidinone derivatives from Schiff bases obtained from the condensation of 2-chloro-3-formylquinoline and 3-4-aminoacetophenones. Quinoline based 4-thiazolidinone and 2-azetidinone derivatives have been prepared by the reaction of various substituted Schiff base with thioglycholic acid and chloroacetyl chloride, respectively. The intermediate Schiff bases were synthesized by the condensation of different quinoline aldehydes with amino acetophenones. The starting compound i.e aldehyde was synthesized through Vilsmeier reaction from respective acetanilides. The synthesized compounds were characterized by their physical and spectral data. The synthesized compounds were screened for their antibacterial and antifungal activities by using cup plate method against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa, 25, 50, 100 mug/mL concentration using ciprofloxacin as reference standard drug and Aspergillus Niger, Candida albicans as same concentration using clotrimazole as reference drug, respectively. The spectral data of synthesized compounds of (3a-f), (4a-e) and (5a-f) were characterized by ES Mass, 1H-NMR, IR spectrophotometric methods. The antimicrobial results revealed that the quinoline based Schiff bases, azitidinone and thiazolodinones analogues showed good activity towards Gram (+) bacteria as compared to ciprofloxacin. These compounds showed decent activity against Gram (-) bacteria.

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Discovery of a COX-2 selective inhibitor hit with anti-inflammatory activity and gastric ulcer protective effect

Aim: A novel series of 2-arylimino-5-arylidenethiazolidin-4-ones 12a-n were synthesized and all the target compounds were fully characterized by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analysis. Materials & methods: All the target compounds were evaluated for their COX inhibition by enzyme immunoassay kit and in vivo anti-inflammatory activity. Results: Tested compounds were found more potent inhibitors of COX-2 (IC50 = 0.54-3.14 M) than COX-1 (IC50 = 4.97-11.52 M). The ulcerogenic liability of compounds 12(d, e, f, h, k, m) was performed and showed gastric safety more than or comparable to celecoxib. Conclusion: In addition, docking study of the most potent and selective compound 12h into COX-2 active site revealed that this target compound assumed interactions and binding pattern similar to that of as a cocrystallized ligand bromocelecoxib (S-58).

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Development of promising thiopyrimidine-based anti-cancer and antimicrobial agents: Synthesis and QSAR analysis

Objective & Methodology: New hybrids of thiopyrimidine-five/six heterocyclic rings were synthesized and in vitro evaluated for their antiproliferative activity against three human cancer cell lines, namely HCT116 (human colorectal carcinoma), PC-3 (human prostate adenocarcinoma) and HepG2 (human liver carcinoma) cell lines. The most potency was elicited by the target candidates against the viability of HCT116 cell lines. It was higher than that obtained by the positive control 5-Fluorouracil (IC50 range; 0.11-0.49 muM, IC50, 5-FU; 1.10 muM). Results: Cell cycle analysis and apoptosis activation revealed that compound 20 induced G2/M phase arrest and apoptosis in HCT116 cells. In addition, compound 20 activates the caspases-9 and -3, a process which might mediate the apoptosis of HCT116 cells. Quantitative structure activity relationship study was done and revealed a high predictive power R2 suggesting goodness of the models. Conclusion: Furthermore, there is a good agreement between the observed pIC50 and the predicted pIC50 values, in addition, the low RMSD and standard error values indicate the accuracy of the model. Antimicrobial evaluation revealed that some of these compounds exhibited significant activities against the tested pathogenic bacteria and fungi, wherein compounds 7a, 14, 15a, 21a, produced the most potent and broad spectrum antibacterial and antifungal potency that was equivalent to that revealed by Vibramycin and Ketoconazole (MIC; 125 mug/mL). Moreover, compounds 15a, 21c, investigated dual potent antimicrobial and anticancer activity.

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Extracurricular laboratory:new discovery of 1,1-Dioxo-isothiazolidine

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HETEROCYCLYLMETHYL-THIENOURACILE AS ANTAGONISTS OF THE ADENOSINE-A2B-RECEPTOR

The present application relates to novel thieno[2,3-d]pyrimidine-2,4-dione (?thienouracil?) derivatives bearing a particular type of (azaheterocyclyl)methyl substituent, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of pulmonary and cardiovascular disorders and of cancer.

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Synthesis of C2-symmetric bisthiazolidine ligands derived from L-cysteine

Treatment of L-cysteine esters and thiazolidine-4-carboxylic esters with an excess of paraformaldehyde in the presence of trifluoroacetic acid provides C2-symmetric N,N?-methylene-bisthiazolidines in good yield.

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Something interesting about 76186-04-4

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 76186-04-4, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 76186-04-4, name is (S)-4-Isopropylthiazolidine-2-thione. In an article£¬Which mentioned a new discovery about 76186-04-4

Asymmetric transfer hydrogenation of ketones using Ru(0) nanoparticles modified by Chiral Thiones

The catalytic asymmetric transfer hydrogenation (ATH) of acetophenone in isopropanol by Ru(0) nanoparticles (NPs) obtained by the in-situ reduction of Ru (II) half-sandwich complexes of chiral 2-oxazolidinethiones and 2-thiozolidinethiones was examined and compared with the catalytic activity of Ru(0) NPs formed in-situ by the reduction of [Ru(p-cymene)(Cl)2]2 in presence of optically active ligands such as (S)-4-isobutylthiazolidine-2-thione, (S)-4-Isopropyl-2(?2-pyridinyl)-2-oxazoline, (8S, 9R)-(?)-cinchonidine, (S)-leucinol, (S)-phenylalaninol, and (S)-leucine. Three of the best catalytic systems were then examined for ATH of thirteen aromatic ketones with different electronic and steric properties. A maximum of 24% ee was obtained using NPs generated from the Ru (II) half-sandwich complex with (S)-4-isobutylthiazolidine-2-thione in the TH of acetophenone. The NPs were characterized by TEM and DLS measurements. Kinetic studies and poisoning experiments confirmed that the reaction is catalyzed by the chiral NPs formed in-situ. Complete characterization of the complexes, including the X-ray crystallographic characterization of two complexes, was also carried out.

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