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Journal articles on the topic 'Thiazolidine Derivative'

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Published: 4 June 2021

Last updated: 2 February 2022

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1

Fawzi, Mourad, Aziz Auhmani, Moulay Youssef Ait Itto, Abdelkhalek Riahi, Sylviane Chevreux, and El Mostafa Ketatni. "Crystal structure of methyl (Z)-2-[(Z)-3-methyl-2-({(E)-1-[(R*)-4-methylcyclohex-3-en-1-yl]ethylidene}hydrazinylidene)-4-oxothiazolidin-5-ylidene]acetate." Acta Crystallographica Section E Crystallographic Communications 73, no. 11 (2017): 1626–29. http://dx.doi.org/10.1107/s2056989017014311.

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The new title 4-thiazolidinone derivative, C16H21N3O3S, was obtained from the cyclization reaction of 4-methyl-3-thiosemicarbazone and dimethyl acetylenedicarboxylate (DMAD). The cyclohexylidene ring has an envelope conformation with the stereogenic centre C atom as the flap. Its mean plane makes a dihedral angle of 56.23 (9)° with the thiazolidine ring mean plane. In the crystal, molecules are linked by C—H...O hydrogen bonds forming chains propagating in the [001] direction. Within the chains there are offset π–π interactions between the thiazolidine rings of inversion-related molecules [cen

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2

Almeida, Marcel L., Douglas C. F. Viana, Valécia C. M. da Costa, et al. "Synthesis, Antitumor Activity and Molecular Docking Studies on Seven Novel Thiazacridine Derivatives." Combinatorial Chemistry & High Throughput Screening 23, no. 5 (2020): 359–68. http://dx.doi.org/10.2174/1386207323666200319105239.

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Aim and Objective: In the last decades, cancer has become a major problem in public health all around the globe. Chimeric chemical structures have been established as an important trend on medicinal chemistry in the last years. Thiazacridines are hybrid molecules composed of a thiazolidine and acridine nucleus, both pharmacophores that act on important biological targets for cancer. By the fact it is a serious disease, seven new 3-acridin-9-ylmethyl-thiazolidine-2,4-dione derivatives were synthesized, characterized, analyzed by computer simulation and tested in tumor cells. In order to find ou

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3

PAYNE, David J., John H. BATESON, David TOLSON та ін. "Phosphonamidate analogues of dipeptides with carboxypeptidase A and β-lactamase-inhibitory activity: elucidation of the mechanism of β-lactamase inhibition by electrospray mass spectrometry". Biochemical Journal 314, № 2 (1996): 457–61. http://dx.doi.org/10.1042/bj3140457.

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A series of phosphonamidate compounds with different P1´ amino acid residues have been shown to be irreversible inactivators of the serine β-lactamase from Enterobacter cloacae P99. The efficiency of inhibition (based on k2/K values) of P99 by these derivatives, ordered in decreasing potency, is: β-phenyl-β-Ala> L-Phe> β-Ala> Gly>D-Phe>D-Pro> D-thiazolidine. The D- and L-Phe compounds also inhibit carboxypeptidase A. The proline and thiazolidine derivatives were phosphonamidate methyl esters, whereas the others were salts of diacids. Electrospray mass spectrometry showed that

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4

Moreno-Fuquen, Rodolfo, Juan C. Castillo, Rodrigo Abonia, Javier Ellena, and Carlos A. De Simone. "Crystal structure of (±)-3-[(benzo[d][1,3]dioxol-5-yl)methyl]-2-(3,4,5-trimethoxyphenyl)-1,3-thiazolidin-4-one." Acta Crystallographica Section E Structure Reports Online 70, no. 12 (2014): o1235—o1236. http://dx.doi.org/10.1107/s160053681402340x.

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In the title thiazolidine-4-one derivative, C20H21NO6S, the central thiazolidine ring is essentially planar (r.m.s. deviation for all non-H atoms = 0.0287 Å) and forms a dihedral angle of 88.25 (5)° with the methoxy-substituted benzene ring and 74.21 (4)° with the 1,3-benzodioxole ring. The heterocyclic ring (with two O atoms) fused to benzene ring adopts an envelope conformation with the non-ring-junction C atom as the flap. In the crystal, the molecules are linked into chains along [001] through weak C—H...O interactions, formingR44(28) edge-fused rings.

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5

Cambie, RC, GR Clark, TC Jones, PS Rutledge, GA Strange та PD Woodgate. "vic-Iodo Thiocyanates and Iodo Isothiocyanates. IX. A Synthesis of Penam and Other Polycyclic Β-Lactams". Australian Journal of Chemistry 38, № 5 (1985): 745. http://dx.doi.org/10.1071/ch9850745.

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Penam (4-thia-1-azabicyclo[3.2.0]heptan-7-one) and 2,3-disubstituted penams are prepared conveniently from vic-iodo isothiocyanates beginning with the facile cyclization of the latter with di -t-butyl sodiomalonates. Treatment of the resulting di -t-butyl 2-(thiazolidin-2- ylene ) malonates with trifluoroacetic acid gives t-butyl 2-thiazolin-2- ylacetate derivatives which are reduced to the corresponding thiazolidines with aluminium amalgam. Cleavage of these t-butyl esters with hydrogen chloride affords β-amino acid hydrochlorides, which are cyclized to penam and its derivatives with 1-[3-( d

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6

Hayashi, Tateki, Clayton A. Reece, and Takayuki Shibamoto. "Gas Chromatographic Determination of Formaldehyde in Coffee Via Thiazolidine Derivative." Journal of AOAC INTERNATIONAL 69, no. 1 (1986): 101–5. http://dx.doi.org/10.1093/jaoac/69.1.101.

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Abstract Thiazolidine formed from trace quantities of formaldehyde in an aqueous solution containing cysteamine at pH 8 was extracted with chloroform and subsequently analyzed by a gas chromatograph equipped with a fused silica capillary column and a thermionic nitrogen-phosphorus specific detector. Recoveries of formaldehyde from the aqueous solutions at levels lower than 1 ppm were slightly over 100%. Quantitative analysis of formaldehyde in commercial brewed and instant coffees showed 3.4-4.5 ppm in the brewed and 10-16.3 ppm in the instant coffee.

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7

Chande, Madhukar S., and Vijay Suryanarayan. "Synthesis of Spirocyclohexanone Ring Containing Thiazolidine Nucleus: A Regioselective Approach." Journal of Chemical Research 2005, no. 6 (2005): 345–47. http://dx.doi.org/10.3184/0308234054506749.

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The paper highlights the Michael addition reactions of 2-arylimino-3-aryl-thiazolidin-4-one 1 with acceptors like methyl acrylate and acrylonitrile to furnish the diadducts 5 and 8. Dieckmann condensation of 5 affords the spirocyclohexanone derivative. Also discussed is the interaction of 1 with 1,5-diarylpenta-1,4-dien-3-ones 9.

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8

Gyertyán, István, Lujza Petöcz, István Gacsályi, Márton I. K. Fekete, Kornélia Tekes, and László Kápolnai. "Psychopharmacological effects of an imino-thiazolidine derivative antidepressant candidate, EGYT-4201." Drug Development Research 22, no. 4 (1991): 385–99. http://dx.doi.org/10.1002/ddr.430220410.

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9

Norisada, Nobuyoshi, Hiroaki Masuzaki, Muneya Fujimoto, et al. "Antidiabetic and adipogenic properties in a newly synthesized thiazolidine derivative, FPFS-410." Metabolism 53, no. 12 (2004): 1532–37. http://dx.doi.org/10.1016/j.metabol.2004.06.020.

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10

Journal, Baghdad Science. "Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine." Baghdad Science Journal 7, no. 2 (2010): 1014–22. http://dx.doi.org/10.21123/bsj.7.2.1014-1022.

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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine

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11

Khandebharad, Amol, Swapnil Sarda, Pravin Kulkarni, and Brijmohan Agrawal. "Visible Light Assisted Synthesis of 5-Aryl-1,2,4-thiazolidine-3-thiones Under Catalyst-free Condition." Current Green Chemistry 7, no. 3 (2020): 326–33. http://dx.doi.org/10.2174/2213346107999200729131533.

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Abstract: Light energy can be considered as an ideal eco-friendly source of energy for green chemistry. This perspective was used to synthesize 5-aryl-1,2,4-thiazolidine-3-thiones derivative as a quick, efficient and highly improved protocol. The present method developed an energy competent and integrated technique by one-pot condensations of aromatic aldehyde and thiosemicarbazide under the catalyst-free condition in aqueous-alcoholic media. The impact of light on reaction along with mechanical stirring provided a prominent yield of the product. The mild reaction conditions, short reaction ti

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12

Chis, Irina C., Doina Baltaru, Simona Clichici, Ovidiu Oniga, Ileana Cojocaru, and Cristina Nastasa. "The Effects of a 5-Chromene-yl-thiazolidin-2,4-dione Derivative in Alleviating Oxidative Stress in Adjuvant-Induced Arthritis." Revista de Chimie 69, no. 9 (2018): 2361–65. http://dx.doi.org/10.37358/rc.18.9.6534.

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Rheumatoid arthritis (RA) is a chronic inflammatory disease that reduces life quality and requires long-life therapy. Quercetin (Que) is a natural flavonoid with antioxidant and anti-inflammatory effects. (3-(2-(4-Chlorophenyl)-2-oxoethyl)-5-((6-methyl-4-oxo-4H-chromen-3-yl)methylene) thiazolidine-2,4-dione (TZD) is a thiazolidinedione derivative synthesized in our laboratory. This study was designed to investigate the antioxidant effects of the Que and TZD derivative administration in adjuvant-induced arthritic (AIA) rats. AIA was induced in Wistar rats by the intraplantar injection of Freund

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13

Radomska, Barbara, Tomasz Tatarowski, Jan P. Morawiec, and Henryk Kozłowski. "Interaction of Pd(II) with thiazolidine-4-carboxylic acid and its 4-acetyl derivative." Inorganica Chimica Acta 106, no. 4 (1985): L29—L31. http://dx.doi.org/10.1016/s0020-1693(00)82261-6.

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14

Khan, Neelam, Girendra Gautam, and Arun K. Gupta. "Synthesis and Biological Evaluation of Some New Rhodanine Analogues as Aldose Reductase Inhibitors (ARIs)." Journal of Drug Delivery and Therapeutics 9, no. 1-s (2019): 161–67. http://dx.doi.org/10.22270/jddt.v9i1-s.2284.

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Diabetes mellitus is a metabolic disorder characterized by hyperglycemia resulting long-term secondary complication. Aldose reductase, the rate-limiting enzyme of the polyol pathway, plays a key role in the treatment of diabetic complications. Appropriately, inhibition of this enzyme is emerging as a major therapeutic strategy for the pathogenesis of secondary complication. In this study, we describe a series of 5 aryl benzylidene -thiazolidine, 4-dione derivatives, F3 synthesized as aldose reductase inhibitors. Besides inhibiting efficiently the target enzyme, F4 and F5 showed additional AR i

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15

Volkova, Tatyana V., Olga R. Simonova та German L. Perlovich. "Thiazolidine-2,4-dione derivative in 2-hydroxypropyl-β-cyclodextrin solutions: Complexation/solubilization, distribution and permeability". Journal of Molecular Liquids 333 (липень 2021): 115931. http://dx.doi.org/10.1016/j.molliq.2021.115931.

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16

da Silva, Ivanildo Mangueira, João da Silva Filho, Priscila Brandão Gomes da Silva Santiago, et al. "Synthesis and Antimicrobial Activities of 5-Arylidene-thiazolidine-2,4-dione Derivatives." BioMed Research International 2014 (2014): 1–8. http://dx.doi.org/10.1155/2014/316082.

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Antibiotic resistance is considered one of the world's major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity w

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17

Neda, Ion, Thomas Kaukorat, Peter G. Jones, Reinhard Schmutzler, Harald Grögerh та Jürgen Marte. "Chemistry of the 1,3,5-Triaza-2-phosphorin-4,6-diones, Part XI*. Base-Catalyzed Addition Reactions of 2-Oxo-2-hydro-1,3,5-trimethyl-1,3,5-triaza-2λ4-phosphorine-4,6-dione to the C=N Double Bond of 3-Thiazoline Heterocycles". Zeitschrift für Naturforschung B 51, № 10 (1996): 1486–93. http://dx.doi.org/10.1515/znb-1996-1020.

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The base-catalyzed reaction of 2-oxo-2-hydro-1,3,5-trimethyl-1,3,5-triaza-2λ4-phosphorine- 4,6-dione (1) and of its trimethylsiloxy phosphorus(III) derivative (10) with various 3-thiazolines (2 -5 ) via five different pathways is described. In all cases, the corresponding 3-thiazoline adducts were formed. The different routes are compared with regard to reaction conditions and yields. In the reaction of 1 with 5,5-dimethyl-2-isopropyl-3-thiazoline (3) two diastereomers of 7 were formed, as established by 1H , 13C and 31P NMR spectroscopy. The structures of the products 6 and 8 were confirmed b

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18

Nuriye, Ahmed, Hemant Yennawar, Kevin Cannon, and John Tierney. "Crystal structures of two thiazolidinone derivatives bearing a trichloromethyl substituent at the 2-position." Acta Crystallographica Section E Crystallographic Communications 74, no. 10 (2018): 1509–12. http://dx.doi.org/10.1107/s2056989018013257.

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The title compounds 2-trichloromethyl-3-phenyl-1,3-thiazolidin-4-one (C10H8Cl3NOS),1and 3-(4-chlorophenyl)-2-trichloromethyl-1,3-thiazolidin-4-one (C10H7Cl4NOS)2, are structurally related with one atom substitution difference in theparaposition of the benzene ring. In both structures, the thiazolidinone ring adopts an envelope conformation with the S atom as the flap. The dihedral angles between the rings [48.72 (11) in1and 48.42 (9)° in2] are very similar and the molecules are almost superimposable. In both crystal structures, C—H...O `head-to-tail' interactions between the chiral carbon atom

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19

Blokhina, Svetlana V., Angelica V. Sharapova, Marina V. Ol'khovich, Igor B. Levshin, and German L. Perlovich. "Solid–liquid phase equilibrium and thermodynamic analysis of novel thiazolidine-2,4-dione derivative in different solvents." Journal of Molecular Liquids 326 (March 2021): 115273. http://dx.doi.org/10.1016/j.molliq.2020.115273.

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20

Trotsko, Nazar, Adrian Bekier, Agata Paneth, Monika Wujec, and Katarzyna Dzitko. "Synthesis and In Vitro Anti-Toxoplasma gondii Activity of Novel Thiazolidin-4-one Derivatives." Molecules 24, no. 17 (2019): 3029. http://dx.doi.org/10.3390/molecules24173029.

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Recent findings on the biological activity of thiazolidin-4-ones and taking into account the lack of effective drugs used in the treatment of toxoplasmosis, their numerous side effects, as well as the problem of drug resistance of parasites prompted us to look for new agents. We designed and synthesized a series of new thiazolidin-4-one derivatives through a two-step reaction between 4-substituted thiosemicarbazides with hydroxybenzaldehydes followed by the treatment with ethyl bromoacetate; maleic anhydride and dimethyl acetylenedicarboxylate afforded target compounds. The thiazolidin-4-one d

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21

Islip, P. J., and M. V. Bogunović-Batchelor. "5-(Hydroxyimino)-4-methoxy-2-(pivaloylimino)thiazolidine-3-acetamide, a reduced nitroheterocyclic derivative with potent schistosomicidal properties." Experientia 41, no. 10 (1985): 1353–54. http://dx.doi.org/10.1007/bf01952092.

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22

Kumar, Harsh, Aakash Deep, and Rakesh Kumar Marwaha. "Chemical Synthesis, Mechanism of Action and Anticancer Potential of Medicinally Important Thiazolidin-2,4-dione Derivatives: A Review." Mini-Reviews in Medicinal Chemistry 19, no. 18 (2019): 1474–516. http://dx.doi.org/10.2174/1389557519666190513093618.

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Thiazolidin-2,4-dione (TZD) possessing an active methylene constitute an important chemical class of compounds for the development of new drugs. So, many scholars have synthesized these derivatives as target molecules and evaluated their biological potential. Currently, some of the TZDs are synthesized to treat human cancers stating high levels of PPARγ because it is expected that activation of PPARγ arbitrates their anticancer activity because PPARγ ligands have recently been established to affect differentiation, cell proliferation and apoptosis of different cell types. In the present review

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23

Viñuelas-Zahínos, E., F. Luna-Giles, P. Torres-García, A. B. Rodríguez, and A. Bernalte-García. "Effects of a derivative thiazoline/thiazolidine azine ligand and its cadmium complexes on phagocytic activity by human neutrophils." Inorganica Chimica Acta 366, no. 1 (2011): 373–79. http://dx.doi.org/10.1016/j.ica.2010.11.037.

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24

Hochscherf, Jennifer, Markus Pietsch, William Tieu, et al. "Crystal structure of highly glycosylated human leukocyte elastase in complex with an S2′ site binding inhibitor." Acta Crystallographica Section F Structural Biology Communications 74, no. 8 (2018): 480–89. http://dx.doi.org/10.1107/s2053230x1800537x.

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Glycosylated human leukocyte elastase (HLE) was crystallized and structurally analysed in complex with a 1,3-thiazolidine-2,4-dione derivative that had been identified as an HLE inhibitor in preliminary studies. In contrast to previously described HLE structures with small-molecule inhibitors, in this structure the inhibitor does not bind to the S1 and S2 substrate-recognition sites; rather, this is the first HLE structure with a synthetic inhibitor in which the S2′ site is blocked that normally binds the second side chain at the C-terminal side of the scissile peptide bond in a substrate prot

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25

Bedair, A. H., Abd El-Wahab, A. M. El-Agrody, F. M. Ali, A. H. Halawa, and G. M. El-Sherbiny. "Binary heterocyclic systems containing the ethylideneamino linkage: synthesis of some new heterocyclic compounds bearing the naphtho-[2,1-b]furan moiety." Journal of the Serbian Chemical Society 71, no. 5 (2006): 459–69. http://dx.doi.org/10.2298/jsc0605459b.

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Ethylidene hydrazine (4a,b) and thiazolidin-4-one (5) derivatives were synthesized by the reaction of ethylidenethiosemicarbazide derivative (3a) with ?-haloketone/ethyl bromoacetate, respectively. Hetrocyclization of ethylideneacetohydrazide derivative (7) with o-phenolic aldehydes gave the corresponding coumarin derivatives (8,9). The interaction of 7 with acetylacetone afforded the corresponding pyridine derivative (10). Treatment of the arylidene derivative 11b with malononitrile afforded the corresponding pyran derivative (12). The new products 3-12 were subjected to IR, 1H NMR and mass s

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Yennawar, Hemant P., Lee J. Silverberg, Kevin Cannon, et al. "Crystal structures of two 1,3-thiazolidin-4-one derivatives featuring sulfide and sulfone functional groups." Acta Crystallographica Section E Crystallographic Communications 74, no. 12 (2018): 1695–99. http://dx.doi.org/10.1107/s2056989018015098.

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The crystal structures of two closely related compounds, 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one, C15H18N2O3S, (1) and 1-cyclohexyl-2-(2-nitrophenyl)-1,3-thiazolidin-4-one 1,1-dioxide, C15H18N2O5S, (2), are presented. These compounds are comprised of three types of rings: thiazolidinone, nitrophenyl and cyclohexyl. In both structures, the rings are close to mutually perpendicular, with interplanar dihedral angles greater than 80° in each case. The thiazolidinone rings in both structures exhibit envelope puckering with the S atom as flap and the cyclohexyl rings are in their expect

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27

Parmar, Kokila A., and Sarju N. Parajapati. "Formation and Biological Evaluation of 4-Thiazolidinone Derivatives for their Pharmacological Activity." International Letters of Chemistry, Physics and Astronomy 61 (November 2015): 84–93. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.61.84.

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Thiazolidin-4-one is a versatile lead molecule for designing potential bioactive agents. An expeditious method for preparation of 4-thiazolidinones 7(a-h) are an important class of heterocycles, having potential biological importance due to their unique features. The process of convert of imine (Schiff’s base) to 4-thiazolidinone through an intermediate of THF mercapto acetic acid with anhydrous zinc chloride is important synthetic method for preparation of 4-thiazolidinone. The structures of the synthesized compounds were confirmed by IR, 1H-NMR, 13C NMR and Mass spectral studies. The compoun

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Walmik, Prabhakar, Basavaraj S. Naraboli, Swathi B, and Somashekhar Ghanti. "DESIGN, SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES CONTAINING INDOL- THIAZOLYL- THIAZOLIDINONE DERIVATIVES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 3 (2018): 113. http://dx.doi.org/10.22159/ajpcr.2018.v11i3.22199.

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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 mas

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Thalamuthu, S., B. Annaraj, Smreti Vasudevan, Suparna Sengupta, and M. A. Neelakantan. "DNA binding, nuclease, and colon cancer cell inhibitory activity of a Cu(II) complex of a thiazolidine-4-carboxylic acid derivative." Journal of Coordination Chemistry 66, no. 10 (2013): 1805–20. http://dx.doi.org/10.1080/00958972.2013.791393.

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30

Araújo, Shyrlene, Amanda Soares e Silva, Fabiana Gomes, et al. "Effects of the new thiazolidine derivative LPSF/GQ-02 on hepatic lipid metabolism pathways in non-alcoholic fatty liver disease (NAFLD)." European Journal of Pharmacology 788 (October 2016): 306–14. http://dx.doi.org/10.1016/j.ejphar.2016.06.043.

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31

Gupta, Amit, Rajendra Singh, Pankaj K. Sonar, and Shailendra K. Saraf. "Novel 4-Thiazolidinone Derivatives as Anti-Infective Agents: Synthesis, Characterization, and Antimicrobial Evaluation." Biochemistry Research International 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/8086762.

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A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100–400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity. Compounds4a[2-(4-fluoro-phenyl)-3-(4-methyl-5,6,7,8-tetrahydro-quinazolin-2-y

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Perepelytsya, O. O., I. M. Yaremiy, K. P. Kupchanko, N. V. Panasenko, M. K. Bratenko, and M. V. Vovk. "Synthesis and hypoglycemic activity of derivatives of 4-((1,3-thiazolydine-5-yliden)methy)pyrazole-3-carbonic acid and its esters." Chernivtsi University Scientific Herald. Chemistry, no. 819 (2019): 37–44. http://dx.doi.org/10.31861/chem-2019-819-06.

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An effective preparative method of synthesis of a series of new (pyrazole-4-il)methylenethiazolidine structures has been elaborated. The structures are functionalized in the 3rd position by the carboxylate or carboxyle group and in the 3rd and 5th positions of the thiazolidine cycle – by the oxo-, thio- or iminogroups. The method involves condensation of 4-formylpyrazole-3-carbonic acids and their ethyl esters with a series of the substituted thiazolidines: 1,3-thiazolidine-2,4-dione, 4-thioxo-1,3-thiazolidine-2-one, 2-thioxo-1,3-thiazolidine-4-one and 2-imino-1,3-thiazolidine-4-one. A group o

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Manojkumar, Parameswaran, Thengungal Ravi, and Gopalakrishnan Subbuchettiar. "Synthesis of coumarin heterocyclic derivatives with antioxidant activity and in vitro cytotoxic activity against tumour cells." Acta Pharmaceutica 59, no. 2 (2009): 159–70. http://dx.doi.org/10.2478/v10007-009-0018-7.

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Synthesis of coumarin heterocyclic derivatives with antioxidant activity andin vitrocytotoxic activity against tumour cellsThe aim of the present work was to synthesise coumarinyl heterocycles and to elucidate the potential role of these compounds as antioxidants and cytotoxic agents against Dalton's lymphoma ascites tumour cells (DLA) and Ehrlich ascites carcinoma cells (EAC). The synthesis of coumarin derivatives containing pyrazole, pyrazolone, thiazolidin-4-one, 5-carboxymethyl-4-thiazolidinone and 3-acetyl-1,3,4-oxadiazole ring is reported. 4-Methylcoumarinyl-7-oxyacetic acid hydrazide (1

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Yoshimoto, T., M. Naruse, M. Nishikawa, et al. "Antihypertensive and vasculo- and renoprotective effects of pioglitazone in genetically obese diabetic rats." American Journal of Physiology-Endocrinology and Metabolism 272, no. 6 (1997): E989—E996. http://dx.doi.org/10.1152/ajpendo.1997.272.6.e989.

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Although an improvement of insulin sensitivity has been shown to be a new therapeutic approach for treating diabetes mellitus, details of effects of this treatment on the cardiovascular system and possible renal complications remain unknown. In the present study, we investigated the effects of a thiazolidine derivative, pioglitazone, and examined the insulin-sensitizing action on blood pressure, nephropathy, and vascular changes in genetically obese diabetic Wistar fatty (WF) rats. Pioglitazone (3 mg.kg-1.day-1) was orally administered for 13 wk starting at the age of 5 wk, and the results wer

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Beise, Frank, Harald Labischinski, and Hans Bradaczek. "On the Relationships between Molecular Conformation, Affinity towards Penicillin-Binding Proteins, and Biological Activity of Penicillin G-Sulfoxide." Zeitschrift für Naturforschung C 43, no. 9-10 (1988): 656–64. http://dx.doi.org/10.1515/znc-1988-9-1006.

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Abstract The binding capacity of penicillin G-sulfoxide towards the penicillin-binding proteins (PBP) of Staphylococcus aureus H was studied. The sulfoxide and its parent compound, penicillin G , differ only in two aspects, the sulfur-bound oxygen and an altered conformation of the five-membered thiazolidine-ring system. These minor alterations of the penicillin structure resulted in a drastical decrease of binding activity (about two orders of magnitude) of the sulfoxide derivative towards its target enzymes. Furthermore, the sulfoxide did not exhibit the selectivity of subinhibitory doses fo

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Ayalew, Hailemichael, Gebremedihin Reda, Tsegaye Gashaw, Neelaiah Babu, and Raj Kumar Upadhyay. "Antimicrobial and Dyeing Properties of Reactive Dyes with Thiazolidinon-4-one Nucleus." ISRN Organic Chemistry 2014 (March 4, 2014): 1–8. http://dx.doi.org/10.1155/2014/894250.

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Four imines, the condensation products of 2,4-dioxo-4-phenylbutanal with four primary amines, were condensed with mercapto acetic acid to obtain thiazolidinon-4-ones which on subsequent condensation with vanillin and isatin separately yielded eight thiazolidin-4-one derivatives. The chemical structures of the synthesized compounds were elucidated by elemental analysis, molecular weight determination, IR and 1H and 13C NMR spectral measurements. Antibacterial and antifungal properties were studied in vitro against two bacteria and two fungi. The dyeing potential of synthesized reactive dyes was

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Dighe, Rajendra Dnyandeo, Vinod A. Bairagi, Parag A. Pathade, and Yogesh T. Sonawane. "Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors." Journal of Drug Delivery and Therapeutics 9, no. 1 (2019): 207–10. http://dx.doi.org/10.22270/jddt.v9i1.2324.

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To determine antimycobacterium and dTDP rhamnose inhibitor activity of the synthesized azetidinone, thiazolidinone derivatives of thiazole, we studied different derivatives for the activity. One pot synthesis of 2-amino-4-methylthiazole-5-carboxylic acid ethyl ester has been carried out and synthesized different derivative compounds. Compounds were tested for antimicrobial activity against different strains of microorganism and antitubercular activity against M. tuberculosis H37Rv. Compounds 7c, 7d, 7i, 8d, 8e, 8g and 8h, were showed antimicrobial activity against Staphylococcus aureus, Escher

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Kumar, Rakesh, and Shailendra Patil. "Synthesis and Antimicrobial Evaluation of 2-(Substituted-phenyl)-3-(4-(4- Nitrophenyl)Thiazol-2-yl)Thiazolidin-4-One Derivatives." Current Bioactive Compounds 15, no. 1 (2019): 114–19. http://dx.doi.org/10.2174/1573407213666171020102638.

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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 Gra

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Kumar, Alleni Suman, Rathod Aravind Kumar, Elala Pravardhan Reddy, et al. "Synthesis of Novel 2-Thioxothiazolidin-4-one and Thiazolidine-2, 4-dione Derivatives as Potential Anticancer Agents." Natural Product Communications 13, no. 5 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300518.

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A variety of novel thiazolidine derivatives (2-thioxothiazolidin-4-one and thiazolidine-2, 4-dione derivatives) have been prepared by using 2,4-diphenyl-2 H-chromene-3-carbaldehyde and its derivatives as starting materials. This is the first example of the preparation of thiazolidine derivatives through this novel method. Structure evolution of the resulting thiazolidine derivatives leads to anticancer agents. Our preliminary data for some model compounds on three cancer cell lines (MCF7, A549 and B-16) suggested reasonable anticancer activity against the A549 and B-16 cell lines, with IC50 va

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Patel, Divyesh, Rahul Patel, Premlata Kumari, and Navin B. Patel. "Synthesis of s-Triazine-Based Thiazolidinones as Antimicrobial Agents." Zeitschrift für Naturforschung C 67, no. 3-4 (2012): 108–22. http://dx.doi.org/10.1515/znc-2012-3-402.

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5A novel series of thiazolidinone derivatives, namely 4-{4-dimethylamino-6-[4-oxo- 2-phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin-3-yl]-[1,3,5]-triazin-2-yloxy}- 1-methyl-1H-quinolin-2-ones, have been synthesized from the key intermediate 4-(4-amino- 6-dimethylamino-[1,3,5]-triazin-2-yloxy)-1-methyl-1H-quinolin-2-one (). Compound 5 was condensed with various aldehydes to give Schiff base derivatives, which after cyclization gave thiazolidinones that were linked with 1-pyridin-2-yl-piperazine to obtain the target compounds. The newly synthesized compounds were evaluated for their

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Youssef El-Sayed, A. "Zero-Crossing Derivative Spectrophotometric Determination of Mercury(II) And Palladium(II) with 5-(3,4-Methoxyhydroxyphenylmethylene)-2-thioxo-1-3-thiazolidine and Cetyltrimethylammonium Bromide." Analytical Letters 31, no. 11 (1998): 1905–16. http://dx.doi.org/10.1080/00032719808005270.

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Kumar, Shiv, Nitin Kumar, Sushma Drabu, et al. "Synthesis of 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)acetamide Based Thiazolidinone Derivatives as Potent Antibacterial and Antifungal Agents." E-Journal of Chemistry 9, no. 4 (2012): 2155–65. http://dx.doi.org/10.1155/2012/857514.

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Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substituted)phenyl-1,3-thiazolidin-3-yl]acetamide (5a-l) were synthesized. These compounds were evaluated for theirin-vitroantibacterial againstE. coli, S. aureus, K. pneumoniae, P. aeruginosa & antifungalactivity againstC. albicans, A. niger & A. flavusby cup-plate method. Structures of all the newly synthesized compounds were confirmed by elemental analysis,1H-NMR & FT-IR spectral data interpretation. Compounds 5d & 5h having p-nitrophenyl &p-trifluoromethylphenyl group respectively on

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Myronenko, Solomija, Oleh Pinyazhko, and Roman Lesyk. "EFFECTS OF 4-THIAZOLIDINONE DERIVATIVES LES-2658 AND LES-1205 ON SLEEP - WAKEFULNESS CYCLE IN KINDLED RATS." EUREKA: Life Sciences 1 (January 31, 2017): 51–56. http://dx.doi.org/10.21303/2504-5695.2017.00289.

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The research is dedicated to in-depth study of neurotrophic and antiepileptic properties of original potential anticonvulsant agents from 4-thiazolidinones – LES-2658 (5-(3-nitro-benzylidene)-2-(thiazol-2-ylimino)-thiazolidin-4-one) and LES-1205 ([2,4-dioxo-5-(thiazol-2-ylcarbamoylmethyl)-thiazolidin-3-yl]-acetic acid ethyl ester), synthesized at the Department of Pharmaceutical, Organic and Bioorganic Chemistry of Danylo Halytsky Lviv National Medical University, Ukraine. Studying of sleep - wakefulness cycle characteristics in animals with chronic epileptic syndrome in conditions of 4-thiazo

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Asgaonkar, Kalyani Dhirendra, Shital Manoj Patil, Trupti Sameer Chitre, et al. "Comparative Docking Studies: A Drug Design Tool for Some Pyrazine- Thiazolidinone Based Derivatives for Anti-HIV Activity." Current Computer-Aided Drug Design 15, no. 3 (2019): 252–58. http://dx.doi.org/10.2174/1573409915666181219125944.

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<P>Background: Acquired immunodeficiency Syndrome (AIDS) is caused by Human immunodeficiency virus type 1 (HIV-1). Pyrazine and Thiazolidinone pharmacophore has diverse biological activities including anti HIV activity. </P><P> Aims and Objectives: To study binding behavior of Pyrazine- thiazolidinone derivatives on four different crystal structures of HIV- 1RT.These molecules which were already reported as anti-TB were investigated for dual activity as Anti-HIV and Anti-TB. </P><P> Materials and Methods: In the present study we describe a comparative docking stud

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RAJALAKSHMI, RAMARAJAN, RAJAVEL SANTHI, and THANGARAJ ELAKKIYA. "Synthesis, Characterization, Biological Evaluation and Molecular Docking Studies of Some Oxazinyl-Thiazolidinone Derivatives." Asian Journal of Chemistry 32, no. 9 (2020): 2125–29. http://dx.doi.org/10.14233/ajchem.2020.22710.

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A series of new 4-thiazolidinone derivatives of 2-(4-chlorophenyl)-3-(6-(thiophen-2-yl)-4-p-tolyl-4H-1,3-oxazin-2-yl)- thiazolidin-4-one (7h-m) are synthesized because of its wide range of biological activities.1H & 13C NMR, IR studies were applied for the elucidation of all the synthesized compounds. All the synthesized compounds have been tested for antidiabetic and antioxidant activity in vitro method against standard. The analogs 7h-m was evaluated for α-amylase and α-glucosidase inhibitory potential. The structures of all the compounds have been screened for antioxidant activity using

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Patel, Navin B., Hetal I. Soni, and Rahul B. Parmar. "Significance of Microwave Irradiation in Synthesis of Thiazolidin-4-one Bearing Pyrimidine Analogues: Their in vitro Antimicrobial, Antituberculosis and Antimalarial Studies." Current Microwave Chemistry 7, no. 3 (2020): 230–37. http://dx.doi.org/10.2174/2213335607999200918155613.

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Aim: To synthesise biologically active thiazolidin-4-one by microwave irradiation method and evaluate against different species of bacteria, fungi and Plasmodium falciparum. Background: Microwave irradiation method is serviceable for rapid and sustainable synthesis. In this present study, Thiazolidin-4-one bearing pyrimidine derivatives have been synthesized by microwave irradiation method. Objective: Thiazolidin-4-one is a valuable motif because of its broad-spectrum biological evaluation. It is famous for many types of biological profiles, mainly antimicrobial, anti-tuberculosis, anti- convu

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Gouda, Moustafa A., and Ameen A. Abu-Hashem. "Synthesis, Characterization, Antioxidant and Antitumor Evaluation of Some New Thiazolidine and Thiazolidinone Derivatives." Archiv der Pharmazie 344, no. 3 (2010): 170–77. http://dx.doi.org/10.1002/ardp.201000165.

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Hara, Takumi, Fumitoshi Hirayama, Hidetoshi Arima, Yoshihiro Yamaguchi та Kaneto Uekama. "Prominent Solubilizing Effect of 2-Hydroxypropyl-β-cyclodextrin on a New Thiazolidine Derivative (FPFS-410) with Antidiabetic and Lipid-lowering Activities through Inclusion Complex Formation". Journal of Inclusion Phenomena and Macrocyclic Chemistry 56, № 1-2 (2006): 135–39. http://dx.doi.org/10.1007/s10847-006-9074-5.

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Hassaneen, Huwaida M. E., and Richard M. Pagni. "Synthesis of New 3-Substituted Indole Derivatives." Zeitschrift für Naturforschung B 65, no. 12 (2010): 1491–97. http://dx.doi.org/10.1515/znb-2010-1213.

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Treatment of 3-cyanoacetyl-2-methylindole (1) with phenyl isothiocyanate gave the corresponding thioacetanilide derivative 3. The thioacetanilide 3 was utilized as the key intermediate for the synthesis of some new 1,3,4-thiadiazole (6a, b and 9a - e), thiophene (11a, b), thiazolidin-4-one (4), thiazole (12 and 13), and benzothiazole (15) derivatives. The structures of the new compounds were elucidated on the basis of elemental analyses and spectral data.

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Balakrishnan, C., M. Theetharappan, Satheesh Natarajan, S. Thalamuthu, and M. A. Neelakantan. "Fluorescence response of a thiazolidine carboxylic acid derivative for the selective and nanomolar detection of Zn(ii) ions: quantum chemical calculations and application in real samples." RSC Advances 5, no. 127 (2015): 105453–63. http://dx.doi.org/10.1039/c5ra21277d.

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A turn-on fluorescent sensor (L) for Zn<sup>2+</sup>detection in nano molar scale was synthesized and characterized. L shows fluorescence withKlebsiella pneumoniaandE. coli. L was utilized to detect Zn<sup>2+</sup>ions and bacteria in environmental water samples.

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