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Synthesis, characterization and evolution of biological activity for new heterocyclic derivatives Schiff bases

The search included synthesis of some Schiff bases by condensation reactions of sulfadiazine with four aldehydes (2-bromo-5-hydroxybenzaldehyde, 4-N,N-dimethylaminobenzaldehyde,na phthaldehyde, 4-bromobenzaldehyde) to obtain Schiff bases (1-4), then synthesis of four new Thiozolidinones from reaction of 2-mercapto acetic and Schiff bases was carried out. The target compounds were characterized by spectral means including (FT-IR, and Uv-visible in adding of CHN elemental analysis, and some chemo-physical properties, the biological activity study toward two types of bacteria.

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REACTIVE OXYGEN SPECIES-BASED PRODRUGS

Provided herein are ROS-sensitive prodrug compositions and methods of treating ROS-associated diseases by administering the ROS-sensitive prodrug compositions.

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Construction of sulfur-containing moieties in the total synthesis of natural products

Covering: January 2013 to September 2018 Sulfur-containing natural products are a large class of significant functional molecules. Many of these compounds exhibit potent biological activities and pharmacological properties; in fact, some of them have been developed into important drugs. The total synthesis of sulfur-containing natural products is a subject that has long attracted significant attention from synthetic organic chemists; to achieve this goal, various methods have been developed over the past years. This review surveys total syntheses of sulfur-containing natural products that introduce sulfur atoms using different sulfurization agents to construct related sulfur-containing moieties.

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Thiazolidinones: Synthesis, Reactivity, and Their Biological Applications

Thiazolidinone is a biologically important five-membered heterocyclic ring having almost all types of biological activities. This review covers various types of thiazolidinones, such as 2-thiazolidinones, 4-thiazolidinones, 5-thiazolidinones, 2-thioxo-4-thiazolidinones, and thiazolidiene-2,4-dione. The literature related to the physical properties, chemical reactions, and synthesis for these derivatives has been included. Recent advances in the biological activities reported for 4-thiazolidinone derivatives, such as peroxisome proliferator-activated receptor gamma binders, follicle-stimulating hormone agonists, cystic fibrosis transmembrane conductance regulator inhibitors, and antioxidants, have been covered in this review. Thus, this study may help in further optimizing these thiazolidinone derivatives as more effective drug agents.

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Synthesis and evaluation of novel oxazinyl thiazolidinone derivatives antioxidant agent as potent antidiabetic

A new series of 2-(4-chlorophenyl)-3-(4-(4-chlorophenyl)-6-(9H-fluoren-7-yl)-4H-1,3-oxazin-2-yl)thiazolidin-4-one are synthesized due to its more biological activities such as antidiabetic,anti-inflammatory,antioxidant,anticancer,antimicrobial.The structure of the newly synthesized compounds established based on the spectral data and basic analysis. All the synthesized compounds have moderate activity when all the compounds subjected to antioxidant activity. Anti-diabetic screening revealed that six compounds (7m-7r) with IC50 ranging from 6.8 to 57.29 mug/ml Molecular docking studies were carried out 2HRY protein.

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Microwave-assisted synthesis, characterization and antimicrobial potencies of n-substituted iminothiazodin-4-one derivatives

The biggest and most multifaceted class of organic compounds includes heterocyclic compounds. Currently, several heterocyclic compounds are iden-tified, and persistently gratefulness to tremendous synthetic work and synthetic usefulness, the number is increasing exponentially. In most fields of science, including medicinal, pharmaceutical, and agro-chemistry, heterocyclic compounds have a function, and biochemistry is also another area. In this research article, the green approach is administered for achieving the nitrogen, oxygen and sulphur centered five-membered heterocyclic derivatives. By taking the whole thing in to account of hetero-chemistry, the moderately effective analog for gram-positive and gram-negative bacterial strains was shown for the five-membered heterocyclic compound series of N-substituted iminothiazodine-4-one and N-(benzylideneamino)thiazol-4(5H). Throughout the synthesized series of the compound 6c revealed very much active potent against the gram-negative Escherichia coli bacterial strain and the compound 6b point out moderately active against the gram-positive Bacillus subtilis bacteria strains in accordance with the standard drug. The 5a and 6a compounds showed very strong activity against the fungal strain of Candida albicans and 6b as well as 6c were more active and highly potent than the standard drugs against Aspergillus niger species. In the view of this research drive states that all the synthesized compounds might be used for the development for further heterocyclic entities.

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Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders

The NLRP3 inflammasome has been implicated in the pathogenesis of a wide variety of human diseases. A few compounds have been developed to inhibit NLRP3 inflammasome activation, but compounds directly and specifically targeting NLRP3 are still not available, so it is unclear whether NLRP3 itself can be targeted to prevent or treat diseases. Here we show that the compound CY-09 specifically blocks NLRP3 inflammasome activation. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation. Importantly, treatment with CY-09 shows remarkable therapeutic effects on mouse models of cryopyrin-associated autoinflammatory syndrome (CAPS) and type 2 diabetes. Furthermore, CY-09 is active ex vivo for monocytes from healthy individuals or synovial fluid cells from patients with gout. Thus, our results provide a selective and direct small-molecule inhibitor for NLRP3 and indicate that NLRP3 can be targeted in vivo to combat NLRP3-driven diseases.

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Design, synthesis of biologically active heterocycles containing Indol- Thiazolyl- Thiazolidinone derivatives

Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c). Methods: All the newly synthesized compounds were characterized by infrared,1H,13C nuclear magnetic resonance and mass spectral data and elemental analysis and evaluated for in vitro antimicrobial activity. Results: Novel compounds N-((5-Substituted-2-phenyl-1H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethyl benzo[d]thiazol-2-yl)thiazolidin-4-one (6a-c) have been made and characterized using spectral and analytical data. The results of antibacterial and antifungal activities showed that some of the synthesized compounds exhibited promising activities. Conclusion: All the newly synthesized compounds were carried out by the broth microdilution method (NCCLS. 2002) in a DMF concentration of 500, 250, 125, and 62.5 mug/ml. Gentamycin and fluconazole are used as reference standards for antibacterial and antifungal activity, respectively. The final results revealed that compounds 4b, 5b, and 6b exhibited potent antimicrobial activity when compared to the standard drugs.

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Quinuclidine – Wikipedia,
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A NEW SYNTHESIS OF HETEROCYCLES VIA CARBONILATION OF AMINES WITH CARBON MONOXIDE IN THE PRESENCE OF SELENIUM

Amines which contain a second functional group in the appropriate position react with carbon monoxide in the presence of selenium to form heterocyclic derivatives in which carbon monoxide is incorporated.For instance, diamines, aminoalcohols, and their related compounds undergo carbonylation to give cyclic ureas, urethanes and the corresponding carbonylated compounds.For diamines and amino alcohols with more than two carbon atoms between the functional groups, intermolecular carbonylative coupling takes place competing with the intramolecular reaction.High selectivity has been attained under specified reaction conditions.Anilines having cyano or acetyl groups on the ortho position afford new classes of selenium-containing heterocycles.In these reactions, carbamoselenoate has been suggested as the common key intermediate.

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Electrochemical Oxidative C(sp3)?H/N?H Cross-Coupling for N-Mannich Bases with Hydrogen Evolution

N-Mannich bases are an important structure in various functional molecules. A new protocol to synthesize N-Mannich bases was established through electrochemical external-oxidant-free C(sp3)?H/N?H cross-coupling with hydrogen evolution. Various N-methylanilines were explored in this transformation. Moreover, simple amides, heteroatom-containing amides, and succinimides were well tolerated in moderate-to-good yields. In addition, the electrochemical dehydrogenative C(sp3)?H/N?H cross-coupling could be scaled up to 5 mmol. By using triethyl phosphite as trapping agent, the phosphorylation product was detected. At the same time, kinetic isotope effect experiments showed that the cleavage of the C?H bond is the rate-limiting step.

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