• Title/Summary/Keyword: Thiazolidinone

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Discovery of Novel 1,4-Benzodioxane Containing Thiazolidinone Derivatives as Potential Antihepatotoxic Agent

  • Khalilullah, Habibullah;Khan, Shamshir;Ahsan, Mohamed Jawed;Ahmed, Bahar
    • Bulletin of the Korean Chemical Society
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    • v.33 no.2
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    • pp.575-582
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    • 2012
  • In continuance of our search for newer antihepatotoxic agents some novel thiazolidinone derivatives containing 1,4-benzodioxane ring system were synthesized starting from 2,3-dihydro-1,4-benzodioxane-2-carbohydrazide. The synthesized compounds were evaluated for antihepatotoxic activity against $CCl_4$-induced hepatotoxicity in rats. Among them some compounds have shown significant antihepatotoxic activity comparable to standard drug silymarin.

Cycloadditiona reaction of 5-(2-thienyl)methylene derivatives of thiazolidinone-4-thiones and their antimicrobial activities

  • Ead, Hamed A.;Metwalli, Nadia H.;Morsi, Nagwa M.
    • Archives of Pharmacal Research
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    • v.13 no.1
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    • pp.5-8
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    • 1990
  • The cycloaddition of the newely synthesized 5-(2-thienyl)methylene derivatives of thiazolidinone-4-thiones, 2a-c to acrylonitrile (3a), ethylacrylate (3b), N-phenylmaleimide (6) and dimethyl fumarate (8) has been evaluated. Under thermal reaction conditions [4 +2] cycloaddition proceeds with complete site and regioselectivity to yield the cycloadduct, 4, 5, 7 and 9, respectively. The antimicrobial activities of some of the new products were tested.

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Synthesis and In-vitro Activity of Some New Class of Thiazolidinone and Their Arylidene Derivatives

  • Seelam, Nareshvarma;Shrivastava, S.P.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.11
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    • pp.3996-4000
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    • 2011
  • In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, $^1H$ NMR, $^{13}C$ NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

Synthesis of Some Quinoxaline Derivatives Containing Indoline-2,3-dione or Thiazolidinone Residue as Potential Antimicrobial Agents

  • Gendy, Adel-A. El;Meligie, Salwa-El;Afaf-K. El-Ansary;Aly-M. Anmedy
    • Archives of Pharmacal Research
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    • v.18 no.1
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    • pp.44-47
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    • 1995
  • The synthesis of osme quinoxaline derivatives containing indoline-2, 3-dione or thiazolidlinone residue is described. The synthesized derivatives were sureened in vitro for their growth inhibitory activity against six species of bacteria, viz. Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Serratia marcescens and Mycobacterium semegmatils. Most of the compounds exhibited antimicrobial activity especially those having indoline-2, 3-dione moiety.

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Transformations of Aldimines Derived from Pyrrole-2-carbaldehyde. Synthesis of Thiazolidino-Fused Compounds

  • Aydogan, Feray.
    • Bulletin of the Korean Chemical Society
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    • v.22 no.5
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    • pp.476-480
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    • 2001
  • 4-Thiazolidinones which are hetarylsubstituted at the 2-position were prepared by the reaction of mercapto acids with aldimines which were prepared by the condensation of pyrrole-2-carbaldehyde with different aromatic amines. After their benzylide ne derivatives were obtained, we first applied the Wittig reagent on them in the presence of triethylamine, dihydrofurothiazolidines were synthesized. Second, we prepared new pyrazolinothiazolidines by using phenylhydrazine in the presence of sodium acetate. All mentioned compounds have been characterized by their spectral data, and screened for their antimicrobial activities. Some of them exhibit moderate to good antibacterial and tuberculostatic activities.

Synthesis and Preliminary Antimicrobial Screening of New Benzimidazole Heterocycle

  • Fahmy, H.H.;El-masry, A.;Ali Abdelsahed, S.H.
    • Archives of Pharmacal Research
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    • v.24 no.1
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    • pp.27-34
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    • 2001
  • A series of 2-methylbenzimidazole incorporated to different heterocycles through ethyl or carbamoylethyl groups at position 1 of benzimidazole were synthesized. Also 3-(2-methylbenzimidazol-1-yl)propanoic acid hydrazide incorporated with semicarbazides and thiosemicarbazides were prepared. Moreover, the triazole 5e underwent Michael addition and alkylation reaction. Some of the newly synthesized compounds showed considerable antimicrobial activity against gram positive, negative bacteria and yeast.

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Synthesis and Characterization of Some Quinazoline Derivatives as Potential Antimicrobial Agents under Microwave Irradiation

  • Mehta, Sarika;Swarnkar, Neelam;Vyas, Madhuri;Vardia, Jitendra;Punjabi, Pinki B.;Ameta, Suresh C.
    • Bulletin of the Korean Chemical Society
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    • v.28 no.12
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    • pp.2338-2343
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    • 2007
  • Under the framework of green chemistry, an efficient and extremely fast procedure for the synthesis of 5a-h through four-step procedure starting from 2-arylidenetetralin-1-one 1a-d under microwave irradiation is described. A considerable increase in the reaction rate has been observed with better yield. The structures of the synthesized compounds have been characterized on the basis of their elemental analysis and spectral data. Synthesized compounds 5a-h was evaluated for their antimicrobial activity. Some of the compounds exhibited appreciable activity.

A Study of Antibacterial Activity of Some Novel 8-Methoxy-4-methyl-quinoline Derivatives

  • Singh, Sheoraj;Kumar, Vikas;Kumar, Ashok;Sharma, Shalabh;Dua, Piyush
    • Bulletin of the Korean Chemical Society
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    • v.31 no.12
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    • pp.3605-3610
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    • 2010
  • In the present study, some quinoline derivatives have been synthesized like 8-methoxy-4-methyl-2-amino-(3'-chloro-2'-oxo-4'-substituted aryl-1'-azetidinyl)quinolines 8-12 and 8-methoxy-4-methyl-2-amino-(2'-substituted aryl-4'-oxo-1',3'-thiazolidin-3'-yl) quinolines 13-17 from 8-methoxy-4-methyl-2-(substituted arylidenyliminoamino)-quinolines 3-7. The structural assignments of these compounds were based on spectral (IR, $^1H$-NMR, Mass) and elemental (C, H, N) analysis. Further, these compounds were evaluated for antibacterial activity against various bacterial strains. Three compounds 10, 11 and 16 were found to exhibit potent antibacterial activity as compared to the standard drug amphicillin.

Synthesis and Evaluation of the Analgesic and Antiinflammatory Activities of O-Substituted Salicylamides

  • Fahmy, H.H.;El-Eraky, W.
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.171-179
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    • 2001
  • The present investigation deals with the synthesis of some new salicylamidoacetyl sulfonamides 3a,b, salicylamido ethylacetate 4, salicylamido acetic acid hydrazide 5, which is considered as the key intermediate for the synthesis of several series of new compounds such as salicylamido pyrazol 6 and pyrazolone 1. N-imido-derivatives 9, 10, 11, thiadiazole 13, oxadiazole 14, 15, Schiffs bases 16a-f. Cyclocondensation of Schiffs bases with thioglycolic acid gave thiazolidinone 18a-c while with acetylchloride afforded azitidinones 19a-c and with acetic anhydride gave 1,4-benzoxazepine-3,5-dione. Some of the compounds were tested for their analgesic and antiinflammatory activities as well as ulcerogenic effects. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered .

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