Neat reaction technology for the synthesis of 4-oxo-thiazolidines derived from 2-SH-benzothiazole and antimicrobial screening of some synthesized 4-thiazolidinones (original) (raw)
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2011
A series of novel tetrazoloquinoline schiff’s bases 3a-g,4a-g,5a-g,6a-g,7a-g were prepared from 6/7/8-trisubstituted quinoline carbaldehyde . All tetrazolo quinoline Schiff bases were refluxed with thioacetic acid in presence of anhydrous zinc chloride and solvent N,N-dimethyl formamide to afforded novel series of 4-thiazolidinone 8a-g,9a-g,10a-g,11a-g,12a-g.All synthesized 4- thiazolidinone were screened for their antimicrobial activity.
Synthesis of some bioactive 4-thiazolidinone derivatives incorporating benzothiazole moiety
pelagiaresearchlibrary.com
Some 2-aryl-3-(substituted benzothiazolyl)-1,3-thiazolidine-4-ones have been synthesized by the reaction of substituted-2-aminobenzothiazole with aromatic aldehyde (benzaldehyde, pchlorobenzaldehyde, anisaldehyde, salicylaldehyde) followed by cyclic condensation with mercapto acetic acid. All the synthesized compounds were characterized by elemental analysis, IR spectra, 1 H NMR and Mass spectral studies. These were screened for their entomological (Antifeedant activity, Acaricidal activity, Contact toxicity, Stomach toxicity) and antibacterial activities.
Letters in Drug Design & Discovery, 2011
A novel synthetic method has been developed with palladium-catalyzed Buchwald-Hartwig-type reaction for the synthesis of N-tert-butyl-3-{[2-(arylamino)pyrimidin-4-yl]amino} benzenesulfonamide 5 by the treatment of N-tert-butyl-3-[(2-chloropyrimidin-4-yl)amino] benzenesulfonamide 4 with different aromatic amines in the presence of Cs 2 CO 3 and in DMF under microwave conditions. All the eight compounds 5a-h were evaluated for their antibacterial, antifungal, and cytotoxic activities. Among the title compounds, 5c and 5d showed potent activity towards both gram-positive and gram-negative bacteria. Compounds 5c and 5d displayed good antifungal activity, and the compounds 5c, 5d, and 5f exhibited significant cytotoxicity activity.
Orbital - The Electronic Journal of Chemistry, 2016
Several substituted 4-thiazolidinone derivatives 2a-q have been synthesized from halogenohydroxy substituted Schiff bases 1a-q under microwave irradiation technique. The reactions were carried out using ethanol: 2-methoxyethanol mixture as efficient reaction solvent system to afford high yield of product. The structures of newly synthesized compounds have been established on the basis of elemental analysis, IR, 1 H & 13 C NMR and mass spectral data. Further, all newly synthesized compounds were screened for their in vitro antimicrobial activity. The antifungal and antibacterial effects of the tested compounds are due to their molecular structure and substituent present.
Synthesis and antimicrobial studies of some 4-oxo thiazolidines derivatives
New anils were synthesized in good yield from 4,4'-diaminodiphenyl sulphone and various benzaldehydes. Further these anils were converted into 4-thiazolidines by the action of mercapto acetic acid. All the products have been evaluated for their in vitro antimicrobial activity against various strains of bacteria.
Oriental journal of chemistry, 2017
Synthesis of a series of new substituted benzimidazole derivatives by the condensation of o-phenylenediamine with urea to give 1,3-dihydro-benzimidazol-2-one which reacted with phosphoryl chloride to give 2-chloro-1H-benzimidazole is reported. The product was then alkylated at the benzimidazole NH with different electrophilic reagents leading to functionalized derivatives. Structures of the newly synthesized products have been deduced on the basis of spectral and analytical data. The synthesized compounds were screened for their antimicrobial activity. This exhibited some promising results towards testing organism in-vitro.
Asian Journal of Chemistry, 2017
New 2,3-substituted-1,3-thiazolidin-4-one (6a-f) were prepared by cyclocondensation of 2-[6-(4-chlorobenzyloxy)-2-naphthyliden]-4-(4-substituted phenyl)-5-methyl-1,3-thiazole (5a-f) and mercaptoacetic acid in benzene. The synthesized compounds were characterized on the basis of elemental analysis, 1 H NMR, 13 C NMR and FT-IR. The prepared compounds have been screened in vitro against two Grampositive Staphylococcus aureus, Staphylococcus epidermidis, and two Gram-negative Escherichia coli, Pseudomonas aernuginosa for antibacterial activity and two fungal strains Candida albicans, Candida krusei for antifungal activity using ciprofloxacin, ampicillin and ketoconazole with minimal inhibitory concentration (MIC) value of 10 mcg/L in DMSO. Compounds 6a and 6d showed good antibacterial and antifungal activities compared to reference medications utilized within this study.
Combinatorial chemistry & high throughput screening, 2015
As a part of our ongoing project on design and synthesis of new thiazole derivatives with antimicrobial activity fourteen new ethyl 2-(2-((E)-((Z)-5-(4-benzyliden)-4-oxothiazolidin-2-yliden)amino-4-yl)acetates , carrying halogens, methoxy and other groups were synthesized. Compounds were tested against eight Gram positive and negative bacteria as well as eight yeasts and mold by microdilution assay. All compounds showed good activity against all bacteria tested with MIC ranging between 2.3-39.8 μmol/ml x 10-2 and MBC of 9.2-79.6 μmol/ml x 10-2. As reference drugs Ampicillin (MIC 24.8-74.4 and MBC 37.2-124.0 μmol/ml x 10-2) and Streptomycin (MIC 4,3-17.2 and MBC 8.6-51.6 μmol/ml x 10-2) were used. The best activity was observed for 4-bromo derivative. All tested compounds showed excellent antifungal activity against all fungi tested with MIC in range between 0.3-38.6 μmol/ml x 10-2 and MFC range of 0.6-77.2 μmol/ml x 10-2, better than that of reference drugs, Ketoconazole (MIC 38.0-4...
Microwave Assisted One Pot Synthesis of 2,3-Diaryl-1,3-Thiazolidine-4-Ones
Recently, we have carried out operationally simple, efficient, one pot synthesis of 2,3-diaryl-1,3-thiazolidine-4-ones by condensation of substituted aromatic amines and aldehydes in presence of thioglycolic acid with solid catalyst anhydrous zinc chloride in dioxane by microwave irradiation for 10 min. The yields of the products were excellent. The structure of the synthesized compounds has been established on the basis of IR, NMR, C 13 NMR spectroscopic techniques. The antimicrobial activities of the synthesized compounds were tested in vitro against the sensitive organisms Staphylococcus aureus (Gram positive bacteria) and Escherichia coli (Gram negative bacteria) by using the disc diffusion method.