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Triazine as a promising scaffold for its versatile biological behavior

Among all heterocycles, the triazine scaffold occupies a prominent position, possessing a broad range of biological activities. Triazine is found in many potent biologically active molecules with promising biological potential like anti-inflammatory, anti-mycobacterial, anti-viral, anti-cancer etc. which makes it an attractive scaffold for the design and development of new drugs. The wide spectrum of biological activity of this moiety has attracted attention in the field of medicinal chemistry. Due to these biological activities, their structure-activity relationship has generated interest among medicinal chemists and this has culminated in the discovery of several lead molecules. The outstanding development of triazine derivatives in diverse diseases within very short span of time proves its magnitude for medicinal chemistry research. Therefore, these compounds have been synthesized as target structure by many researchers, and were further evaluated for their biological activities. In this review, we have compiled and discussed the biological potential of s-triazine derivatives, which could provide a low-height flying bird’s eye view of the triazine derived compounds to a medicinal chemist, for a comprehensive and target oriented information for the development of clinically viable drugs.

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Can You Really Do Chemisty Experiments About (R)-2-Oxothiazolidine-4-carboxylic acid

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The role of metabotropic glutamate receptors in addiction: Evidence from preclinical models

Addiction is a chronic disorder characterised by repeated bouts of drug taking, abstinence and relapse. The addicted state may be in part due to drug-induced neuroadaptations in the mesocorticolimbic and corticostriatal pathways. Recently focus has been on the role of aberrant glutamate transmission and its contribution to the hierarchical control over these systems. This review will expand our current knowledge of the most recent advances that have been made in preclinical animal models that provide evidence that implicate metabotropic glutamate receptors (mGluRs) in contributing to the neuroadaptations pertinent to addiction, as well as the role of Homer proteins in regulating these responses. The recent discovery of receptor mosaics will be discussed which add an additional dimension to the complexity of understanding the mechanism of glutamate mediated behaviours. Finally this review introduces a new area related to glutamatergic responses, namely microRNAs, that may become pivotal in directing our future understanding of how to best target intervention strategies to prevent addictive behaviours.

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Synthetic approaches, structure activity relationship and biological applications for pharmacologically attractive pyrazole/pyrazoline-thiazolidine-based hybrids

The features of the chemistry of 4-thiazolidinone and pyrazole/pyrazolines as pharmacologically attractive scaffolds were described in a number of reviews in which the main approaches to the synthesis of mentioned heterocycles and their biological activity were analyzed. However, the pyrazole/pyrazoline-thiazolidine-based hybrids as biologically active compounds is poorly discussed in the context of pharmacophore hybrid approach. Therefore, the purpose of this review is to summarize the data about the synthesis and modification of heterocyclic systems with thiazolidine and pyrazoline or pyrazole fragments in molecules as promising objects of modern bioorganic and medicinal chemistry. The description of biological activity was focused on SAR analysis and mechanistic insights of mentioned hybrids.

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New explortion of 2-Cyanoimino-1,3-thiazolidine

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A group of thio phosphorylation compound (by machine translation)

The present invention provides a group of thio phosphorylation compound, the compound of the formula Wherein X is or S O; R 1 is an ethyl or 2-chloro-4-bromophenyl; for R S-3-methyl-2 – (4-chlorophenyl) d acyl, 4- asian methoxy -2 – (P-chlorophenyl) – 3-cyano-5 – (trifluoromethyl) pyrrolyl, 4- asian methylthio- -2 – (P-chlorophenyl) – 3-cyano-5 – (trifluoromethyl) pyrrolyl, ethyl-(1-methylamino-2-nitro-vinyl) amino, 2-cyanoimino -1,3-thiazole alkyl in any one of; the invention discloses the structure of the compound to the agricultural insect pests and control effect, also discloses the use of these compounds as the application of the insecticide. (by machine translation)

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A new application about (R)-2-Oxothiazolidine-4-carboxylic acid

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Application of 19771-63-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article£¬once mentioned of 19771-63-2

Thiazolidine prodrugs as protective agents against gamma-radiation-induced toxicity and mutagenesis in V79 cells

Representatives of two classes of thiazolidine prodrug forms of the well-known radioprotective agents L-cysteine, cysteamine, and 2-[(aminopropyl)amino]ethanethiol (WR-1065) were synthesized by condensing the parent thiolamine with an appropriate carbonyl donor. Inherent toxicity of the prodrugs was assessed in V79 cells using a clonogenic survival assay. Protection against radiation-induced cell death was measured similarly after exposure to 0-8 Gy gamma (137Cs) radiation. Antimutagenic activity was determined at the hypoxanthine-guanine phosphoribosyltransferase (HGPRT) locus. All thiazolidine prodrugs exhibited less toxicity than their parent thiolamines, sometimes dramatically so. Protection against radiation-induced cell death was observed for the 2-alkylthiazolidine, 2(R,S)-D-ribo-(1?,2?,3?,4?-tetrahydroxybutyl) thiazolidine (RibCyst), which produced a protection factor at 8 Gy of 1.8; the cysteine analogue, 2(R,S)-D-ribo-(1?,2?,3?,4?-tetrahydroxybutyl) thiazolidine-4(R)-carboxylic acid (RibCys), was less active. RibCyst also exhibited excellent antimutational activity, rivaling that of WR-1065. The 2-oxothiazolidine analogues showed little activity in either determination under the conditions tested, perhaps due to their enhanced chemical and biochemical stability.

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Brief introduction of 2682-49-7

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Recent progress on anti-Toxoplasma drugs discovery: Design, synthesis and screening

Toxoplasma gondii severely threaten the health of immunocompromised patients and pregnant women as this parasite can cause several disease, including brain and eye disease. Current treatment for toxoplasmosis commonly have high cytotoxic side effects on host and require long durations ranging from one week to more than one year. The regiments lack efficacy to eradicate T. gondii tissue cysts to cure chromic infection results in the needs for long treatment and relapsing disease. In addition, there has not been approved drugs for treating the pregnant women infected by T. gondii. Moreover, Toxoplasma vaccine researches face a wide variety of challenges. Developing high efficient and low toxic agents against T. gondii is urgent and important. Over the last decade, tremendous progress have been made in identifying and developing novel compounds for the treatment of toxoplasmosis. This review summarized and discussed recent advances between 2009 and 2019 in exploring effective agents against T. gondii from five aspects of drug discovery.

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Awesome Chemistry Experiments For 2682-49-7

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Reference of 2682-49-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS. In a Article£¬once mentioned of 2682-49-7

Synthesis and antimicrobial evaluation of 2-(Substituted-phenyl)-3-(4-(4-nitrophenyl)thiazol-2-yl)thiazolidin-4-one derivatives

Background: Diseases caused by microbial infections are very common worldwide. Although the search of innovative antimicrobial agents is the current focus for the researchers, the treatment of infectious diseases remains an important public health issue and a challenging problem in front of medicinal chemist. Methods: A series of 2-(4-hydroxyphenyl)-3-(4-(4-nitrophenyl) thiazol-2-yl)thiazolidin-4-one derivatives (T1-T10) was designed and synthesized. All the titled compounds were evaluated for their antimicrobial potential. Antimicrobial activity was performed by tube dilution methods against Gram negative Escherichia coli MTCC 443 (E. Coli), Gram positive bacteria: Staphylococcus aureus MTCC 3160 (S. aureus) and Bacillus subtilis MTCC 441 (B. Subtilis), and fungal strains: Aspergillus niger MTCC 281 (A. niger) and Candida albicans MTCC 227 (C. albicans). Results: Among the synthesized derivatives, compounds 2, 4 and 10 were found to be most active antimicrobial agents. Conclusion: In conclusion, a series of 2-(phenyl)-3-(4-(phenyl)thiazol-2-yl)thiazolidin-4-ones have been designed and synthesized. All the titled compounds were evaluated for their in vitro antimicrobial activity against five representative microorganisms. The results of antimicrobial study indicated that the presence of nitro and chloro groups in aromatic ring improved antibacterial activity, whereas the presence of hydroxy group improved antifungal activity of substituted 4-thiazolidinone derivatives.

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The important role of 19771-63-2

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Application of 19771-63-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article£¬once mentioned of 19771-63-2

Preparation and characterization of new In(III), Re(III), and Re(V) complexes with thenoyltrifluoroacetone and some bidentate heterocyclic ligands

New In(III), Re(III) and Re(V) complexes with the thenoyltrifluoroacetone ligand (HTTA) of the general formulae [In -(TTA)(H2O)4]SO4, [Re(TTA)n(H2O)x]Cl3-n and [ReO(TTAn-(H2O)x]Cl3-n (where n and x refer to the number of [TTA]- moieties and H2O molecules, respectively) have been prepared and characterized by spectroscopy, thermogravimetry, elemental analyses and X-ray diffraction. The charge densities on the ligand atoms were calculated via CNDO-SCF calculations. The newly prepared complexes [In(TTA)(H2O)4]SO2 and [ReO(TTA)(H2O)2]CL2 were employed as precursors for the synthesis of the mixed-ligand complexes [In(TTA)(HOCTA)2], [In(TTA)(TZT)2] and [ReO(TTA)(HOTCA)]Cl using R(-)-2-oxothiazolidine 4-carboxylicacid (H2OTCA) and 1H-1,2,4-triazole-3-thiol (H2TZT) as ligands. The synthesized mixed-ligand complexes were characterized by the conventional physical and chemical methods of analysis applied earlier for the characterization of the precursors. The investigated complexes are soluble in water, ethanol and acetonitrile, insoluble in non-polar solvents and could be of potential use for clinical studies. The antibacterial activity of the investigated complexes has been tested and evaluated.

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The Absolute Best Science Experiment for 185137-29-5

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Related Products of 185137-29-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.185137-29-5, Name is (S)-4-Phenylthiazolidine-2-thione, molecular formula is C9H9NS2. In a Article£¬once mentioned of 185137-29-5

Kinetic resolution of N-acyl-thiolactams via catalytic enantioselective deacylation

Methanolysis of N-acyl-thiazolidin-2-thiones and -oxazolidin-2-thiones in the presence of acyl transfer catalyst benzotetramisole (BTM) proceeds in a highly enantioselective fashion thus enabling kinetic resolution of these substrates.

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Brief introduction of Thiazolidin-2-one

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Synthesis and evaluation of thiazolidine-2,4-dione/benzazole derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B): Antihyperglycemic activity with molecular docking study

This work presents the synthesis of two hybrid compounds (1 and 2) with thiazolidine-2,4-dione structure as a central scaffold which were further screened in combo (in vitro as PTP-1B inhibitors, in vivo antihyperglycemic activity, in silico toxicological profile and molecular docking). Compound 1 was tested in the enzymatic assay showing an IC50 = 9.6 ¡À 0.5 muM and compound 2 showed about a 50% of inhibition of PTP-1B at 20 muM. Therefore, compound 1 was chosen to test its antihyperglycemic effect in a rat model for non-insulin-dependent diabetes mellitus (NIDDM), which was determined at 50 mg/kg in a single dose. The results indicated that compound showed a significant decrease of plasma glucose levels that reached 34%, after a 7 h post-administration. Molecular docking was employed to study the inhibitory properties of thiazolidine-2,4-dione derivatives against Protein Tyrosine Phosphatase 1B (PDB ID: 1c83). Concerning to the two binding sites in this enzyme (sites A and B), compound 1 has shown the best docking score, which indicates the highest affinity. Finally, compounds 1 and 2 have demonstrated an in silico satisfactory pharmacokinetic profile. This shows that it could be a very good candidate or leader for new series of compounds with this central scaffold.

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