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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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The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), STR1 wherein A stands for hydrogen, halogen or a C1-4 alkyl, C1-4 alkoxy or nitro group; and n is 0 or 1. The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.

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New tetrahydro-1H-pyrazolo[3,4-b]quinoline derivatives were designed, synthesized and characterized as dual anticholinestrase and cyclooxygenase-2 inhibitors. The in vitro and in vivo anti-cholinesterase evaluation exhibited promising activities with lower hepatotoxicity for many candidates compared to tacrine as a reference. Furthermore, their anti-inflammatory activity using in vitro (COX-1/COX-2) inhibitory assay demonstrated superior activity to celecoxib with higher selectivity indices for some compounds. In addition, some candidates showed extended anti-inflammatory activity by inhibiting COX-2 protein induction. Besides, in silico docking experiments of the active compounds against hAChE rationalized the observed in vitro AChE inhibitory activity. In conclusion, this work provides an extension of the chemical space of tetrahydro-1H-pyrazolo[3,4-b]quinoline chemotype for the anticholinestrase and anti-inflammatory activity. This would aid to minimize the possible neuroinflammation linked to the pathogenesis of Alzheimer’s disease.

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New explortion of 19771-63-2

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The present disclosure relates to methods and compositions for providing at least broad spectrum photo protection to skin, which includes protection from at least infrared (IR) radiation and/or visible light. The methods typically entail applying to skin a cosmetic composition comprising: (a) one or more antioxidants selected from the group consisting of baicalin, Venuceane, ferulic acid, polydatin, silymarin, punica granatum extract, mango leaf extract, soliprin, catechin, hesperetin, astilbin, and DHC V; (b) optionally, one or more solubilizers; and (c) a cosmetically acceptable carrier; wherein the combination of (a), optional (b), and (c) alone, provide at least broad spectrum protection from both infrared (IR) radiation and visible light. UV filters can also optionally be included to provide additional protection from UV light.

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The electronic structure of a series of organic molecules of general formula <*>RN-(CH2)2-X-C=Y, which are also of interest in inorganic chemistry because of their properties as ligands towards metals, have been investigated by X-ray photoelectron spectroscopy.The results suggest a general picture of atomic charge distribution within the investigated molecules, and allow an assessment of the effect of the different substituent groups X, Y, R (X=NR’, O, S, CH2; Y=O, S, Se; R, R’=H, alkyl) on the electronic structure of the ligands.Satisfactory correlation is foundbetween experimental binding energies and computed CNDO/2 atomic charges, after correction for intramolecular Madelung potentials.

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QSAR (Quantitative Structure-Activity Relationship) relate biological activity data along with the physiochemical and structural properties of a group of compounds. In general, most of the medicinal compounds involve heterocyclic compounds containing nitrogen and sulphur especially thiazolidinones they possess a broad spectrum antimicrobial activity. In the present study, we have carried out the QSAR studies of antimicrobial thiazolidinones using Hansch analysis. The results of QSAR studies indicated that the antimicrobial activity of thiazolidinones are mainly governed by the topological parameters, kiers 3rd order alpha shape index (kappa alpha 3) and second order valence connectivity index (2chinu) along with the lipophilic parameter, log of octanol water partition coefficient (log P).

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New discoveries in chemical research and development in 2021. Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. In a patent, 1055361-35-7, name is 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, introducing its new discovery. category: thiazolidine

2,4-Dichloroquinolines and 2,4-dichloroquinazolines were synthesized from 2-ethynylanilines and anthranilonitriles, respectively, using diphosgene in acetonitrile and heating at 130 C or 150 C for 12 hours. This reaction was applied to the synthesis of 4,6-dichloropyrazolo[3,4-d]pyrimidine (dichloro-9H-isopurine). The postulated mechanism is also described. Georg Thieme Verlag Stuttgart.

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In past decades, interdisciplinary research has been of great interest for scholars. Thiazolidine motifs behave as a bridge between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. Thiazolidine motifs are very intriguing heterocyclic five-membered moieties present in diverse natural and bioactive compounds having sulfur at the first position and nitrogen at the third position. The presence of sulfur enhances their pharmacological properties, and, therefore, they are used as vehicles in the synthesis of valuable organic combinations. They show varied biological properties viz. anticancer, anticonvulsant, antimicrobial, anti-inflammatory, neuroprotective, antioxidant activity and so on. This diversity in the biological response makes it a highly prized moiety. Based on literature studies, various synthetic approaches like multicomponent reaction, click reaction, nano-catalysis and green chemistry have been employed to improve their selectivity, purity, product yield and pharmacokinetic activity. In this review article, we have summarized systematic approaches for the synthesis of thiazolidine and its derivatives, along with their pharmacological activity, including advantages of green synthesis, atom economy, cleaner reaction profile and catalyst recovery which will help scientists to probe and stimulate the study of these scaffolds.

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A facile procedure for the preparation in good yield of L-2-oxothiazolidine-4-carboxylic acid and other 2-oxothiazolidines of biological interest is described, involving reaction of suitable aminothiols with 1,1′-carbonyldiimidazole in an organic solvent.

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Provided herein is a composition, method of manufacture, and method for treating a disease condition and/or raising cellular levels of glutathione, the composition comprising L-2-oxothiazolidine-4-carboxylate, (procysteine) having a purity of at least 99 to 99.5 percent.

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