Can You Really Do Chemisty Experiments About 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Long range 13C-1H-coupling constants at bridgehead carbons in some naphthalene and quinoline derivatives, “cross” ring and “through” ring interactions

The 3JCH couplings at bridgehead carbons in naphthalene and quinoline derivatives have been classified as “through” ring and “cross” ring interactions.Further divisions of the couplings have been introduced in an attempt to rationalize the interactions such that they may be used for structural assignments.The influence of central ?-bond order and of the heterocyclic nitrogen atom on the couplings has been discussed.From a study of the 3J couplings at C-9 and C-10 in 45 quinoline derivatives the coupling constant ranges observed were “through” ring (via 9,10-bond): J94 4.9-6.1 Hz, J95 5.5-7.3 Hz, J10.8 4.1-5.3 Hz; “cross” ring: J92 11.0-13.5 Hz, J97 6.7-9.8 Hz, J10.3 4.4-7.3 Hz, J10.6 5.2-9.1 Hz.

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THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

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1055361-35-7, Name is 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, belongs to thiazolidine compound, is a common compound. Application In Synthesis of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrileIn an article, once mentioned the new application about 1055361-35-7.

Synthesis and characterization of substituted 4-methoxy-1H-quinolin-2- thiones

The synthesis of various substituted 4-methoxy-1H-quinolin-2-thiones from various substituted aniline with malonic acid, phosphorousoxychloride, sodium methoxide glacial acetic acid and thiourea under different conditions is described. All these substituted 4-methoxy-1H-quinolin-2-thiones were synthesized from four steps; the first step involved the synthesis of substituted 2,4-dichloro quinoline from aniline (substituted), with malonic acid and phosphorous-oxychloride. In the second step, the substituted 2,4-dichloro compound was heated with freshly prepared methanolic sodium methoxide solution to give 2,4-dimethoxy quinoline compounds, it was then refluxed with glacial acetic acid and hydrochloric acid to get the substituted 4-methoxy-1H-quinolin- 2-one. The final steps involves with an objective of introducing a chloro in the position 2 of the quinolone system, the substituted 4-methoxy-1H-quinolin-2-one was refluxed with distilled PoCl3 chloroform. The substituted 2-chloro-4-methoxy quinoline was then refluxed with thiourea and alcohol to get substituted 4-methoxy-1H-quinolin-2-thiones. The purity of the synthesized compound was judged by their C, H and N analysis and the structure was analyzed on the basics of mass, FT-IR and 1H NMR.

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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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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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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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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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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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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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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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