• Journal of the Korean Chemical Society
• /
• v.52 no.6
• /
• pp.649-656
• /
• 2008

• Journal of the Korean Chemical Society
• /
• v.56 no.3
• /
• pp.341-347
• /
• 2012

A series of 2-(4-chlorophenylimino)-5-((3-(p-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl) methylene) thiazolidin-4-one ($\mathbf{3a-h}$) compounds were prepared from the 2-(4-chlorophenylimino) thiazolidin-4-one ($\mathbf{1}$) and 1-phenyl-3-(p-substituted phenyl)-1H-pyrazole-4-carbaldehyde ($\mathbf{2a-h}$). All compounds were characterized by elemental (C, H, N) analysis and spectral (FT-IR, $^1H$ NMR and GC-MS) analysis. These newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial activity was observed and evaluated against the bacterial strains like Eschericha coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442) and against the fungal strains like Candida albicans (MTCC 227), Aspergillus niger (MTCC 282) and Aspergillus clavatus (MTCC 1323). All the synthesized compounds were found to possess moderate to excellent antimicrobial activity against above selected strains.

• Journal of the Korean Chemical Society
• /
• v.58 no.1
• /
• pp.33-38
• /
• 2014

In the course of work on new pharmacologically active antimicrobial agents, we have reported the synthesis of a new class of structurally novel derivatives, incorporating two bioactive structures, a benzothiazole and thiazolidin-4-one, to yield a class of compounds having interesting antimicrobial properties. The antimicrobial properties of the synthesized compounds were investigated against bacteria (Staphylococcus aureus and Escherchia coli) and fungi (Candida albicans and Aspergillus niger) using serial plate dilution method. The structure of the synthesized compounds have been established by elemental analysis and spectroscopic data.

• Journal of the Korean Chemical Society
• /
• v.52 no.3
• /
• pp.338-340
• /
• 2008

• Bulletin of the Korean Chemical Society
• /
• v.31 no.5
• /
• pp.1219-1222
• /
• 2010

A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3-yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.8
• /
• pp.2345-2350
• /
• 2010

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives of these moieties were evaluated for antimicrobial activity. Most of the synthesized compounds showed good antimicrobial activity at 200 and $100\;{\mu}g/mL$. Compounds showed most significant antibacterial activity against gram negative test organism Escherichia coli and most significant antifungal activity against test organisms Aspergillus niger and Candida albicans. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] were more potent against microbes as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• Bulletin of the Korean Chemical Society
• /
• v.32 no.3
• /
• pp.1011-1016
• /
• 2011

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• Bulletin of the Korean Chemical Society
• /
• v.26 no.4
• /
• pp.579-584
• /
• 2005

The 3-[(2-furylmethylene)amino]-2-thioxo-1,3-thiazolidin-4-one (FTT) was used as an excellent ionophore in construction of a $Zn^{2+}$ PVC-based membrane sensor. The best performance was obtained with a membrane composition of 30% poly(vinyl chloride), 62% nitrobenzen (NB), 3% FTT and 5% sodium tetraphenyl borate (TBP). This membrane sensor shows very good selectivity and sensitivity towards $Zn^{2+}$ over a wide variety of cations, including alkali, alkaline earth, transition and heavy metal ions. The membrane sensor revealed a great enhancement in selectivity coefficients for $Zn^{2+}$ ions, in comparison to the previously reported $Zn^{2+}$ membrane sensors. Theoretical studies also showed the selective interaction of TFF and $Zn^{2+}$ ions. The proposed membrane sensor exhibits a Nernstian behavior (with slope of 29.3 ${\pm}$ 0.3 mV per decade) over a wide concentration range (1.0 ${\times}$ $10^{-6}$-1.0 ${\times}$ $10^{-2}$) with a detection limit of 8.5 ${\times}$ $10^{-7}$ M (52 ng mL$^{-1}$). It shows relatively fast response time, in the whole concentration range ($\lt$ 20 s), and can be used for at least 10 weeks in a pH range of 3.0-7.0. The proposed membrane sensor was successfully used in direct determination of $Zn^{2+}$ ions in wastewater of industrial zinc electroplating companies, and also as an indicator electrode in titration with EDTA.

• Journal of the Korean Chemical Society
• /
• v.54 no.1
• /
• pp.77-87
• /
• 2010

Hospital-acquired methicillin-resistant Staphylococcus aureus (MRSA) has been an increasing problem worldwide since the initial reports over 40 years ago. To examine new drug leads with potential antibacterial activities, Various N'-[(-3-substituted-4-oxo-1,3-thiazolidin-2-ylidene]-4-hydroxy benzohydrazide (4a-4.i) and N'-[-(3,4-disubstituted)-1,3-thiazolidin-2ylidene)]-4-hydroxybenzohydrazide from (5.a-5.i) to (10.a-10.i) were synthesized using appropriate synthetic route. The entire test compounds (4.a-4.i) and from (5.a-5.i) to (10.a-10.i) were assayed in vitro against s. aureus strain. The minimum inhibitory concentration (MIC) was determined for test compounds and for reference standards. The test compounds showed significant antibacterial activity against the strains used, when tested in vitro. In general, p-hydroxybenzohydrazide ring and substituted thiazoline ring are essential for antimicrobial activity. Among the compounds tested, compounds 6.f, 7.g, 9.f and 10.f, 10 i were found to be most potent. The test compounds were found nontoxic upto the dose level of 2000 ${\mu}g$/mL. The intact compounds were then subjected for 3D-QSAR studies. 3D-QSAR study based on the principal of alignment of pharmacophoric features by Schrodinger PHASE module. The 3D-QSAR study allowed us to confirm the preferential binding mode of p-hydroxybenzohydrazide inside the active site.

• Archives of Pharmacal Research
• /
• v.16 no.3
• /
• pp.186-190
• /
• 1993

Two series of substituted sulforrythiazolidin-4-ones and sulforrylthiazolines have been synthesized and examined for their antidiabetic and biological aticity.