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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 (October 13, 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 [centroid–centroid distance = 3.703 (1) Å]. The chains are linked by further C—H...O hydrogen bonds, forming slabs parallel to theacplane.
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2

Almeida, Marcel L., Douglas C. F. Viana, Valécia C. M. da Costa, Flaviana A. dos Santos, Michelly C. Pereira, Maira G. R. Pitta, Moacyr J. B. de Melo Rêgo, Ivan R. Pitta, and Marina G. R. Pitta. "Synthesis, Antitumor Activity and Molecular Docking Studies on Seven Novel Thiazacridine Derivatives." Combinatorial Chemistry & High Throughput Screening 23, no. 5 (July 9, 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 out if the compounds have therapeutic potential. Materials and Methods: Seven new 3-acridin-9-ylmethyl-thiazolidine-2,4-dione derivatives were synthesized through Michael addition and Knoevenagel condensation strategies. Characterization was performed by NMR and Infrared spectroscopy techniques. Regarding biological activity, thiazacridines were tested against solid and hematopoietic tumoral cell lines, namely Jurkat (acute T-cell leukemia); HL-60 (acute promyelocytic leukemia); DU 145 (prostate cancer); MOLT-4 (acute lymphoblastic leukemia); RAJI (Burkitt's lymphoma); K562 (chronic myelogenous leukemia) and normal cells PBMC (healthy volunteers). Molecular docking analysis was also performed in order to assess major targets of these new compounds. Cell cycle and clonogenic assay were also performed. Results: Compound LPSF/AA-62 (9f) exhibited the most potent anticancer activity against HL-60 (IC50 3,7±1,7 μM), MOLT-4 (IC50 5,7±1,1 μM), Jurkat (IC50 18,6 μM), Du-145 (IC50 20±5 μM) and Raji (IC50 52,3±9,2 μM). While the compound LPSF/AA-57 (9b) exhibited anticancer activity against the K562 cell line (IC50 51,8±7,8 μM). Derivative LPSF/AA-62 (9f) did not interfere in the cell cycle phases of the Molt-4 lineage. However, the LPSF/AA-62 (9f) derivative significantly reduced the formation of prostate cancer cell clones. The compound LPSF/AA-62 (9f) has shown strong anchorage stability with enzymes topoisomerases 1 and 2, in particular due the presence of chlorine favored hydrogen bonds with topoisomerase 1. Conclusion: The 3-(acridin-9-ylmethyl)-5-((10-chloroanthracen-9-yl)methylene)thiazolidine-2,4-dione (LPSF/AA-62) presented the most promising results, showing anti-tumor activity in 5 of the 6 cell types tested, especially inhibiting the formation of colonies of prostate tumor cells (DU-145).
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3

PAYNE, David J., John H. BATESON, David TOLSON, Brian GASSON, Teresa KHUSHI, Philippe LEDENT, and Jean-Marie FRÈRE. "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, no. 2 (March 1, 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 equimolar mixtures of the P99 enzyme with each of the following derivatives, Gly, D-Phe, L-Phe, β-Ala and β-phenyl-β-Ala, effected efficient adduct formation (70–95% of enzyme modified), illustrating the particularly active nature of some of these compounds. All the primary amino acid derivatives gave a similar mass increment, which suggests the displacement of the variable P1´ part of the molecule. This observation provides evidence that the compounds phosphonylate the active-site serine, with the phosphonamidate bond as the scissile bond and the amino acid as the leaving group. The thiazolidine derivative (phosphonamidate methyl ester) also appeared to work by the same mechanism. The comparable proline derivatives caused lower than expected mass shifts of 227–229, and therefore it is proposed that with these compounds both the amino acid and the phosphonamidate ester methoxy group were displaced at the phosphorus atom during the inhibition process. Therefore, electrospray mass spectrometry has provided both a measure of potency and a rationale for the mechanism of inhibition of P99 by these compounds.
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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 (November 5, 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, and PD Woodgate. "vic-Iodo Thiocyanates and Iodo Isothiocyanates. IX. A Synthesis of Penam and Other Polycyclic Β-Lactams." Australian Journal of Chemistry 38, no. 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-( dimethylamino ) propyl ]- 3-ethylcarbodiimide hydrochloride. The structures of the (2α,3aβ,7aβ)- thiazolidine (5) and of the tricyclic β- lactam (41) have been confirmed by X-ray crystallography.
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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 (January 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 (June 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, Gen Inoue, Kiminori Hosoda, Tatsuya Hayashi, Mayumi Watanabe, Shizuko Muraoka, Fumio Yoneda, and Kazuwa Nakao. "Antidiabetic and adipogenic properties in a newly synthesized thiazolidine derivative, FPFS-410." Metabolism 53, no. 12 (December 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 (June 6, 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 -2- yl hydrazone (6) Azomethine (7-10) were prepared through condensation of (1) with aromatic aldehydes or ketones, then compounds (7-9) are converted into a number of tetrazole derivatives (11-13). Treatment of (1) with acetic acid afforded the derivative (14) . The reaction of 2-mercapto pyrimidine with ethyl chloro acetate afforded (15),whereas the reaction of (15) with thiosemicarbazide and 4% sodum hydroxide leads to ring closure giving 1,2,4 triazole derivative (17). Moreover the reaction of 2-mercapto pyrimidine with chloro acetic acid gave (18) followed by refluxing (18) with o- amino aniline to give the benzimidazole derivative (19).the structure of these compounds were characterized by FR-IR, UV spectra and some of them were characterized by element analysis.
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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 (December 2, 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 time and easy workup procedure, avoidance of heavy metal catalyst and harsh reaction conditions make this protocol greener.
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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 (October 15, 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�s complete adjuvant (FCA), unilaterally in the right hind paw. The control non-arthritic rats and the arthritic rats were treated with Que (30 mg/kg/day) or TZD derivative (12 mg/kg/day) for 21 days. The antioxidant effects of 5-chromen-yl- thiazolidinedione were compared to Que. The serum levels of malondialdehyde (MDA) and protein carbonyl (PC) groups, the superoxide dismutase (SOD) and catalase (CAT) activity were assessed. AIA rats showed significatly increased oxidative stress parameter levels in the blood. The results indicated that the TZD derivative decreased the blood oxidative stress parameters in the treated arthritic rats, compared to Que. The antioxidant effects of 5-chromen-yl-thiazolidinedione in AIA suggest its therapeutic properties for the clinical treatment of RA.
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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 (April 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 (February 15, 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 inhibitory as well as hypoglycaemic activity (146.15 and 175.20 mg/dl ) thus emerging as novel dual acting compounds. The bezylidene derivative F3, the most promising of the whole series, showed a well-balanced, consisting of ALR2 inhibitory efficacy (83.00% at 10µg/mL), similarly, F3 have lower blood glucose level in the range of 131.11 mg/dl at 15 mg/kg body weight. This compound show robust in vitro and in vivo efficacy, and could be considered as promising dual target antidiabetic drug candidates. Keywords: Diabetes mellitus, hyperglycemia, Aldose reductase inhibitors
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15

Volkova, Tatyana V., Olga R. Simonova, and German L. Perlovich. "Thiazolidine-2,4-dione derivative in 2-hydroxypropyl-β-cyclodextrin solutions: Complexation/solubilization, distribution and permeability." Journal of Molecular Liquids 333 (July 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, Micalyne Soares do Egito, Carlos André de Souza, Frederico Leite Gouveia, Rafael Matos Ximenes, 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 was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL.
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17

Neda, Ion, Thomas Kaukorat, Peter G. Jones, Reinhard Schmutzler, Harald Grögerh, and 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, no. 10 (October 1, 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 by X-ray analysis; the thiazolidine rings display a twist conformation through the sulfur atom. The molecules are linked via inversion centres by hydrogen bonds of the form N-H···O= C.
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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 (September 28, 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 atoms and the thiazolidinone oxygen atoms result in infinite monochiral chains along the direction of the shortest unit-cell parameter, namelyain1andbin2. C—H...π interactions between the thiazolidinone carbon atom at the 4-position and the phenyl ring of the neighboring enantiomer also help to stabilize the packing in each case, although the crystals are not isostructural.
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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 (August 21, 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 derivatives were used to assess the inhibition of Toxoplasma gondii growth in vitro. All active thiazolidine-4-one derivatives (12 compounds) inhibited T. gondii proliferation in vitro much better than used references drugs both sulfadiazine as well as the synergistic effect of sulfadiazine + trimethoprim (weight ratio 5:1). Most active among them derivatives 94 and 95 showed inhibition of proliferation at about 392-fold better than sulfadiazine and 18-fold better than sulfadiazine with trimethoprim. All active compounds (82–88 and 91–95) against T. gondii represent values from 1.75 to 15.86 (CC30/IC50) lower than no cytotoxic value (CC30).
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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 (October 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 (November 29, 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, the synthesis of various derivatives of thiazolidine-2,4-diones, their mechanism of action and anticancer activity have been highlighted.
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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 (January 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, Kevin Kuan, Andrew D. Abell, Michael Gütschow, and Karsten Niefind. "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 (July 26, 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 protein. The inhibitor also induces the formation of crystalline HLE dimers that block access to the active sites and that are also predicted to be stable in solution. Neither such HLE dimers nor the corresponding crystal packing have been observed in previous HLE crystal structures. This novel crystalline environment contributes to the observation that comparatively large parts of the N-glycan chains of HLE are defined by electron density. The final HLE structure contains the largest structurally defined carbohydrate trees among currently available HLE structures.
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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 spectra studies.
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Yennawar, Hemant P., Lee J. Silverberg, Kevin Cannon, Deepa Gandla, Sandeep K. Kondaveeti, Michael J. Zdilla, and Ahmed Nuriye. "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 (November 6, 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 expected chair conformations. The two structures superpose fairly well, except for the orientation of the nitro groups with respect to their host phenyl ring, with a difference of about 10° between 1 and 2. The extended structure of 1 has two kinds of weak C—H...O interactions, giving rise to a closed ring formation involving three symmetry-related molecules. Structure 2 has four C—H...O interactions, two of which are exclusively between symmetry-related thiazolidinone dioxide moieties and have a parallel `give-and-take-fashion' counterpart. In the other two interactions, the nitrophenyl ring and the cyclohexane ring each offer an H atom to the two O atoms on the sulfone group. Additionally, a C—H...π interaction between a C—H group of the cyclohexane ring and the nitrophenyl ring of an adjacent molecule helps to consolidate the structure.
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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 compounds were screened for their antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Esherichia coli and Pseudomonas aeruginosa was determined by disc diffusion technique. All the synthesized compounds exhibited promising antimicrobial activity against the studied set of microorganisms.
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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 (March 1, 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 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 μg/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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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 (May 1, 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, Edlene Ribeiro, Wilma Oliveira, Amanda Oliveira, Ingrid Lima, Maria do Carmo Lima, Ivan Pitta, and Christina Peixoto. "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-yl)-thiazolidin-4-one] and4e[3-(4,6-dimethyl-pyrimidin-2-yl)-2-(2-methoxy-phenyl)-thiazolidin-4-one] were the most potent compounds of the series, exhibiting marked antimicrobial activity againstPseudomonas fluorescens,Staphylococcus aureus,and the fungal strains. Thus, on the basis of results obtained, it may be concluded that synthesized compounds exhibit a broad spectrum of antimicrobial activity.
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32

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 of 112 white adult nonlinear rats of both genders was used to investigate the hypoglycemic activity of the synthesized compounds. Pioglitazonum (5-{4-[2-(5-ethylpyridine-2-il)etoxy]benzyl}thiazolidine-2,4-dione, M=246) was used as a reference medicine in the standard dosage of 0.0214 mmole/kg. All compounds were administered intragastrically on an empty stomach using a non-traumatic catheter as a 3 % starch suspension while same dosage of the neutral suspension (without any acting medicine) was administered to the animals of the control group. Possible hypoglycemic activity of the compounds was evaluated by the changes in glucose concentration in blood measured before and 2, 4, 6, 8 and 10 hours after the single administration of a compound. An express glucometer “One Touch Select Simple” was employed for the above tests. Then all the data were processed by MS Excel. As seen from the results of the biochemical investigations, a clear hypoglycemic activity has been registered for the compounds mentioned in this work. Five of ten products have ensured a prolonged effect embracing the entire duration of the experiment. 1-methyl-4[(4-oxo-2-thiooxo-1,3-thiazolidine-5-iliden)methyl]-1H-pyrazole-3-carbonic acid caused the deepest decrease in the glucose content (2.0 units or 30.4 %) while in case of the reference medicine it was only 1.35 units (23.9 %). Some dependence between the compound structure and its pharmaceutical activity was also found. The most prolonged and steady hypoglycemic activity was registered for (pyrazole-4-il)methylethiazolidines with methyl group as a substitute in the 1st position and carboxylic group – in the 3rd position. Additional introduction of the methyl and carboxylate groups into pyrazolic scaffold results in a prolonged and deeper hypoglycemic effect leading to the 1.4 times lesser drop in glucose concentration as compared to that after administration of the reference medicine.
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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 (June 1, 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) reacted with arylazopropanes or hydrazono-3-oxobutyrate derivatives to form pyrazole (3a-c) and pyrazolone derivatives (5a-c). Heterocyclisation of Schiff's bases of 1 with thioglycolic acid, thiomalic acid or acetic anhydride afforded novel heterocyclic derivatives 4-thiazolidinones (7a-c), 5-carboxymethyl-4-thiazolidinones (8a-c) and oxadiazoles (9a-c), respectively. Some of the compounds showed promising antioxidant activityin vitroand cytotoxic activity against DLA cells and EAC cells.
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34

Yoshimoto, T., M. Naruse, M. Nishikawa, K. Naruse, A. Tanabe, T. Seki, T. Imaki, R. Demura, E. Aikawa, and H. Demura. "Antihypertensive and vasculo- and renoprotective effects of pioglitazone in genetically obese diabetic rats." American Journal of Physiology-Endocrinology and Metabolism 272, no. 6 (June 1, 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 were compared with those of vehicle-treated WF rats. At the age of 18 wk, vehicle-treated WF rats were associated with mild hypertension, nephropathy with proteinuria histological glomerular injury, and renal arteriolosclerosis in addition to hyperglycemia, hyperinsulinemia, and hyperlipidemia. Treatment with pioglitazone significantly improved glucose and lipid metabolism. In addition, it lowered blood pressure, decreased proteinuria, and prevented glomerular injury, renal arteriolosclerosis, and aortic medial wall thickening, whereas body weight, food intake, sodium balance, and urinary norepinephrine excretion were significantly increased. These results suggest that the insulin-sensitizing agent pioglitazone is effective in correcting not only glucose and lipid metabolism but also cardiovascular and renal complications in non-insulin-dependent diabetes mellitus.
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35

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 (October 1, 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 for PBP 3, as could be observed for penicillin G . The biological consequences of this behaviour were monitored via growth curves, uptake of cell wall label, and analysis of the cell wall. Binding studies revealed that comparable growth inhibition and impairment of cell wall label uptake were achieved by at least a 100-fold higher penicillin G-sulfoxide concentration, compared to its parent compound. In cell wall analysis, the application of high doses of the antibiotics, i.e. nearly saturated PBP , verified the above mentioned observation. Surprisingly, small but significant differences in cell wall composition occurred using subinhibitory doses, probably due to the altered affinity towards PBP 3, supporting the hypothesis of an important role of this PBP in peptidoglycan transpeptidation.
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36

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 investigated with regard to silk, wool, cotton, and polyester fabrics under hot and cold dyeing conditions.
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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 (January 15, 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, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhosa using Gentamycin as standard, while 7b, 7e, 7f, 7i, 8b, 8e, 8f and 8i showed very strong antimycobacterial activity using rifampicine as a standard. Thiazole derivatives especially with carbonyl group scaffold inhibit an enzyme RmlC, which is an essential component for the biosynthesis of dTDP-rhamnose and produce good antimycobacterium and antimicrobial activity. Keywords: Thiazole, thiazolidinone derivatives, azetidinone derivative, well diffusion method, broth microdilution assay, antitubercular activity, antimicrobial activity.
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38

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 (February 6, 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 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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39

Kumar, Alleni Suman, Rathod Aravind Kumar, Elala Pravardhan Reddy, Vavilapalli Satyanarayana, Jajula Kashanna, Boggu Jagan Mohan Reddy, Basireddy Venkata Subba Reddy, and Jhillu Singh Yadav. "Synthesis of Novel 2-Thioxothiazolidin-4-one and Thiazolidine-2, 4-dione Derivatives as Potential Anticancer Agents." Natural Product Communications 13, no. 5 (May 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 values of 20.7 and 20.4 μM, respectively. This method is operationally simple and works with a diverse range of substrates.
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40

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 (April 1, 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 antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri) and four fungi (Aspergillus niger, Candida albicans, Aspergillus fumigatus, Aspergillus clavatus)
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41

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 (August 1998): 1905–16. http://dx.doi.org/10.1080/00032719808005270.

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42

Kumar, Shiv, Nitin Kumar, Sushma Drabu, Suroor Ahmed Khan, Ozair Alam, Manav Malhotra, and Md Akram Minhaj. "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 2-position of thiazolidinone ring attached to N-atom of acetamido group on 1-position of 3-methyl-1H-quinoxaline-2-one, were found to be active against all the bacterial & fungal strains under investigation, while compound 5l having p-chlorophenyl on 2-position of thiazolidinone nucleus was reported as least active compound against all bacterial & fungal strain under investigation.
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43

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-thiazolidinones derivatives LES-2658 and LES-1205 use was performed. The kindling syndrome was induced in Wistar rats via daily pentylenetetrazol (PTZ) (30 mg/kg, i.p.) administrations during three weeks and sleep - wakefulness cycle was studied under conditions of LES-2658 and LES-1205 administrations at doses 25.0and 100.0 mg/kg i.p.. Total wakefulness, non - rapid eye movement sleep, rapid eye movement sleep, falling asleep latency, REM - onset latency and also number of REM sleep episodes have been determined by behavioral characteristics of experimental animals. It was established that 4-thiazolidinone derivatives Les-1205 and Les-2658 reduce REM sleep fragmentation and increase its duration in PTZ-kindled rats. Les-1205 compound at dose 100.0 mg/kg show a clear correcting influence on kindling - induced sleep disturbances.
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Asgaonkar, Kalyani Dhirendra, Shital Manoj Patil, Trupti Sameer Chitre, Vaibhav Nanabhau Ghegade, Saurabh Radhaji Jadhav, Sajid Shaukat Sande, and Atharva Sudhakar Kulkarni. "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 (April 10, 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 study of twentythree derivatives of N-(4-oxo-2 substituted thiazolidin-3-yl) pyrazine-2-carbohydrazide. Binding pattern of these derivatives was gauged by molecular docking studies on four different receptors bearing PDB code 1ZD1, 1RT2, 1FKP and 1FK9 of HIV–RT enzyme using V. Life MDS software Genetic algorithm docking method. </P><P> Result and Discussion: The studies revealed hydrogen bonds, hydrophobic interaction and pi-pi interactions playing significant role in binding of the molecules to the enzyme. Conclusion: Most of the molecules have shown good dock score and binding energy with anti-HIV receptors but Molecules 13 and 14 have potential to act as anti-tubercular and Anti HIV and hence can be further explored for dual activity.</P>
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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 DPPH radical scavenging assay, NO scavenging method. Molecular docking studies were accomplished in addition to understand the binding affinity of those compounds with PDBID 2HR7 which showed that the synthesized derivatives bind in the lively binding site of the target protein
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46

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 (December 30, 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- convulsant, antihypertensive, hypoglycemic agent and antimalarial. This biological response leads our attention towards the change of Thiazolidin-4-one skeleton to enhance potential. Present study aims to carry out a rapid synthesis of Thiazolidin-4-one derivative of pyrimidine by microwave- assisted heating. Methods: 4-(4-substituted phenyl)-6-(substituted aryl) pyrimidin-2-amine was the key intermediate required for the synthesis of 3-(4-(Substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl)-2-(4-hydroxy phenyl) thiozolidin-4-one (5A-J), which was prepared by using microwave irradiation. The structures of all newly synthesized motifs were characterized by spectral analysis (IR, 1H NMR, 13C NMR spectroscopy) and screened for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pyogenes; antifungal activity against Candida albicans, Aspergillus niger, Aspergillus Clavatus; anti-tuberculosis activity against M. tuberculosis H37RV and antimalarial activity against Plasmodium falciparum. Results: Higher yield with less time-consuming method is the main advantage of Thiazolidin- 4-one bearing pyrimidine motifs synthesis. The excellent biological response of compounds 5B, 5C, 5D, 5G, 5H, 5I, and 5J was observed. Conclusion: As compared to conventional method, less time is required for the preparation of Thiazolidin- 4-one analogues by using advantageous microwave irradiation method. Thiazolidin-4-one derivatives showed improved biological activity.
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47

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 (December 27, 2010): 170–77. http://dx.doi.org/10.1002/ardp.201000165.

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48

Hara, Takumi, Fumitoshi Hirayama, Hidetoshi Arima, Yoshihiro Yamaguchi, and 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, no. 1-2 (April 7, 2006): 135–39. http://dx.doi.org/10.1007/s10847-006-9074-5.

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49

Hassaneen, Huwaida M. E., and Richard M. Pagni. "Synthesis of New 3-Substituted Indole Derivatives." Zeitschrift für Naturforschung B 65, no. 12 (December 1, 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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50

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 Zn2+detection in nano molar scale was synthesized and characterized. L shows fluorescence withKlebsiella pneumoniaandE. coli. L was utilized to detect Zn2+ions and bacteria in environmental water samples.
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