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Synthesis and pharmacological evaluation of azetidin-2-ones and thiazolidin-4-ones encompassing benzothiazole  [cached]
Gurupadayya B,Gopal M,Padmashali B,Manohara Y
Indian Journal of Pharmaceutical Sciences , 2008,
Abstract: Various 7-chloro-6-fluoro-2-arylidenylaminobenzo(1,3)thiazole (2a-h) have been synthesized by the condensation of 7-chloro-6-fluoro-2-aminobenzo(1,3)thiazole (1) with different aromatic aldehydes. The Schiff′s bases on reaction with acetyl chloride, chloroacetyl chloride and phenyl acetyl chloride yielded 1-(7-chloro-6-fluorobenzothiazol-2-yl)-3,4-substituted-aryl-azetidin-2-ones (3a-x). Similarly, cyclization of Schiff′s base with thioglycolic acid furnished 3-(7-chloro-6-fluoro-benzothiazol-2-yl)-2-substituted-arylthiazolidin-4-ones (4a-h). The structures of the newly synthesized compounds have been established on the basis of their spectral data and elemental analysis. Some selected compounds were evaluated for antiinflammatory, analgesic, CNS depressant and skeletal muscle relaxant activity.
V P Singh,K K Saxena,S K Bhati,Ashok Kumar
Journal of Global Pharma Technology , 2010, DOI: 10.1234/jgpt.v2i7.251
Abstract: Compounds form new Series S-5-bromobenzo[d]thiazol-2-yl 2-chloroethanethioate (1), 5-(5-bromo benzo[d]thiazol-2-ylthio)thiazol-2-amine (2), N-substituted-5(5-bromobenzo[d]thiazol-2-ylthio)thiazol -2-amine (3a-3e), 1-(5-(5-bromobenzo[d]thiazol-2-ylthio)thiazol-2-yl)-3-chloro-4-substituted azetidin-2-one (4a-4e) and 3-(5-(5-bromobenzo[d]thiazol-2-ylthio) thiazol-2-yl)-2-substituted thiazolidin-4-one (5a-5e). These compounds have been evaluated for pesticidal and anti-microbial activities. Compound 3-(5-(5-bromobenzo[d]thiazol-2-ylthio) thiazol-2-yl)-2-(4-hydroxy-3-methoxyphenyl) thiazolidin-4-one 5b has been found to exhibit potential pesticidal and anti-microbial properties. The structure of these compounds has been elucidated by elementa (C, H, N) and spectral (IR, 1H NMR & mass) analysis.
Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: synthesis and their biological evaluation  [PDF]
Journal of the Serbian Chemical Society , 2011,
Abstract: A series of thiazolidin-4-one (2a–h; 3a–h), azetidin-2-one (4a–h) and 1,3,4-oxadiazole (5a–h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflam-matory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new com-pounds, out of 32, showed very good anti-inflammatory activity in the carra-geenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The com-pounds, which showed less ulcerogenic action, also showed reduced malondial-dehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mu-cosal lesions and it can be suggested from the results that their protective ef-fects may be related to inhibition of lipid peroxidation in the gastric mucosa.
Arockia Babu M.,Rakesh Shukla,S.G Kaskhedikar
Journal of Global Pharma Technology , 2009, DOI: 10.1234/jgpt.v1i1.24
Abstract: A series of 3-Chloro-4-(4-Methanesulfonyl-phenyl)-1-phenyl-azetidin-2-one and 5-(4-Methanesulfonyl-phenyl)-3-phenyl-thiazolidin-4-one derivatives were synthesized with a pharmacophoric group of 4-methanesulfonyl group at the para position of one of the aryl rings and characterized by IR,NMR, mass spectral and elemental analyses. All the synthesized compounds were tested at a concentration of 20μM against COX-1 and COX-2 enzymes by Colorimetric COX Inhibitor Screening Assay. From both the derivatives, compd-5, compd- 7 and compd- 10 were found to be active selectively exhibited 65.5%, 72.5% and 66.9% respectively, against COX-2 enzyme.
Synthesis and antibacterial activity of some novel 2-Aroylimino-3-aryl-thiazolidin-4-ones
Saeed, Aamer;Abbas, Naeem;Fl?rke, Ulrich;
Journal of the Brazilian Chemical Society , 2007, DOI: 10.1590/S0103-50532007000300010
Abstract: an efficient, regioselective synthesis of some 2-aroylimino-3-aryl-thiazolidin-4-ones (2a-j) involving base-catalyzed cyclization of 1-aroyl-3-aryl thioureas with chloroacetyl chloride in dioxane is reported. the structures were confirmed by spectroscopic data, elemental analyses and in one case (2j) by single crystal x-ray diffraction data. compounds (2a-j) were assayed in vitro for their antimicrobial activity against gram positive and gram negative bacteria and were found to exhibit promising activity towards the tested microorganisms, comparable to and in some cases better than those of the standard drugs.
Synthesis and Fungicidal Activity of 2-Imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones and Their 5-Arylidene Derivatives  [PDF]
Hui-Ling Liu,Zongcheng Lieberzeit,Thorleif Anthonsen
Molecules , 2000, DOI: 10.3390/50901055
Abstract: Five derivatives of 2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones and a series of their 5-arylidene derivatives have been synthesized and tested for antifungal activity against seven agricultural fungi. 2-Imino-3-(2,4-dichloro-5-fluorophenylthiazol-2-yl)-4-thiazolidi-none and 2-imino-3-(2,4-dichlorophenylthiazol-2-yl)-4-thiazolidione, both of them new compounds, exhibited higher fungicidal effects than the other compounds prepared.
Microwave-assisted Synthesis of New 1,3-thiazolidin-4-ones and Evaluation of Their Anticancer Efficacy  [cached]
Zhengyue Ma,Xinghua Zhang,Ligai Bai,Yajun Zheng
Modern Applied Science , 2011, DOI: 10.5539/mas.v5n3p207
Abstract: An efficient method for the synthesis of thiazolidinones from the microwave-assisted, three-component mixture of an aromatic aldehyde, a 2-amino-4H-benzothiopyrano[4,3-d]thiazole and meraptoacetic acid is described. The transformation of the amino group of 2-amino-4H-[1]benzothiopyrano[4,3-d]thiazo- les into a thiazolidinone ring has not been reported to date. In vitro their anticancer activity was evaluated by MTT method. The results of bioactivities evaluation showed the compound 4 exhibited the best anticancer activity and its IC50 was 5.76 ?M, 6.19 ?M, 6.67 ?M against gastric cancer cells (SGC-7901), cervical cancer cells (Hela) and lung cancer cells (A-549), respectively.
Microwave Assisted and Al2O3/K2CO3 Catalyzed Synthesis of Azetidin-2-One Derivatives Containing Aryl Sulfonate Moiety with Anti-Inflammatory and Anti-Microbial Activity  [PDF]
Babasaheb V. Kendre, Mahadev G. Landge, Sudhakar R. Bhusare
Open Journal of Medicinal Chemistry (OJMC) , 2012, DOI: 10.4236/ojmc.2012.23012
Abstract: We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2). The compound (2) on reaction with p-aminobenzoic acid or 2-aminopyridine gave the corresponding aldimines (3). Furthermore, the aldimines are on reaction with chloroacetyl chloride gives corresponding azetidin-2-ones in good to moderate yield. Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the an-ti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Anti- microbial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities.
The Synthesis and the Biological Evaluation of New Thiazolidin-4-one Derivatives Containing a Xanthine Moiety  [PDF]
Florentina Geanina Lupascu,Oana Maria Dragostin,Liliana Foia,Dan Lupascu,Lenuta Profire
Molecules , 2013, DOI: 10.3390/molecules18089684
Abstract: Starting from theophylline (1,3-dimethylxanthine) new thiazolidin-4-one derivatives 7a1–7, 7b1–7 have been synthesized as potential antidiabetic drugs. The structure of the new derivatives was confirmed using spectral methods (FT-IR, 1H-NMR, 13C-NMR). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the ferric reducing power, the total antioxidant activity and the DPPH and ABTS radical scavenging assays. Reactive oxygen species (ROS) and free radicals are considered to be implicated in a variety of pathological events, such as diabetes mellitus and its micro- and macrovascular complications. The results of chemical modulation of the thiazolidin-4-one intermediaries 6a, 6b through condensation with several aromatic aldehydes is the improvement of the antioxidant effect. All benzylidenethiazolidin-4-one derivatives 7a1–7, 7b1–7 are more active than their parent thiazolidin-4-ones. The most active compounds are the ones obtained by reaction of condensation with 4-hydroxybenzaldehyde (compounds 7a5, 7a6), 4-dimethylaminobenzaldehyde (compounds 7a6, 7b6) and 2-nitrobenzaldehyde (compounds 7a7, 7b7).
Synthesis of Some New Functionalized Bis-thiazolidin-5-one and Bis-thiazolidin-4-one Derivatives
American Journal of Chemistry , 2012, DOI: 10.5923/j.chemistry.20120205.06
Abstract: A series of bis-thiazolidin-5-one and bis-thiazolidin-4-one derivatives 3and5 was prepared by the treatment of highly functional thiocarbamoyl intermediates 2 and 4 with chloroacetyl chloride and chloroacetic acid, respectively. Treatment of the bis-thiocarbamoyl derivative 4a with diazotized sulphanilic acid affected acetyl cleavage to afford the corresponding arylhydrazono-thiocarbamoyl derivative 6.The title compounds bis-thiazolidin-5-one and bis-thiazolidin-4-one derivatives showed high reactivity towards azo coupling reaction with diazotized sulphanilic acid and Knoevenagel reaction with 4-isopropylbenzaldehyde.
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