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The present invention relates to novel 2-thiazolidi­none derivatives of the general formula (I), wherein, A stands for hydrogen, halogen or a C1 4alkyl, C1 4alkoxy or nitro group; and, n is 0 or 1. The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers. The invention includes preparation methods for the above compounds with the general formula (I) and pharmaceutical compositions containing them.

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A series of 2-(p-substituted benzylidene)-3-(5-propyl-1, 3, 4-thiadiazol-2-yl) thiazolidin-4-ones were synthesized by the reaction of Schiff’s bases of N-(p-substituted benzylidene)-5 propyl -1, 3, 4-thiadiazole-2-amines with thioglycolic acid in 1, 4-dioxane as solvent and studied for their in vitro antibacterial activity. Reaction of thiosemicarbazide with butanoic acid in presence of concentrated sulphuric acid led to the formation of 5-propyl-1, 3, 4-thiadiazole-2-amines which on further reaction with different p-substituted benzaldehydes yielded the compounds Schiff’s bases of N-(p-substituted benzylidene)-5-propyl -1,3, 4-thiadiazole-2-amines which is further reaction with thioglycollic acid in presence of small amount of zinc chloride in 1,4 dioxane as solvent gave title compounds. These compounds were characterized by spectral analysis. All the synthesized compounds were evaluated for their in vitro for their antibacterial activity against two Gram positive bacterial strains (Bacillus subtilis and Staphylococcus aureus) and two Gram negative bacterial strains (Escherichia coli and Pseudomonas aeruginosa) and their minimum inhibitory concentration (MIC) were determined.

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Background: Inflammation has been recognized as a key feature of both type 2 diabetes mellitus (T2DM) and atherosclerosis. However, the relationships between circulating levels of novel adipose tissue-derived inflammatory factors, including resistin, vaspin, and visfatin, and the severity of atherosclerosis have not been determined. Moreover, the associations between these inflammatory factors and obesity and insulin resistance in elderly patients remain to be clarified. Methods: A cross-sectional study of 256 elderly patients with T2DM admitted in our center was performed. Baseline circulating levels of resistin, vaspin and visfatin were measured with enzyme-linked immunosorbent assays. Ultrasonic evaluations of the carotid arteries of the patients were performed to reflect the severity of systemic atherosclerosis. Patients were classified as having mild, moderate, or severe atherosclerosis according to the results of carotid ultrasonic examination. Circulating levels of the inflammatory factors listed above also were correlated with body mass index (BMI) and homeostasis model assessment of insulin resistance (HOMA-IR). Results: With more severe carotid atherosclerosis, circulating levels of resistin (mild: 2.01 ± 0.23; moderate: 2.89 ± 1.01; severe: 3.12 ± 1.12; p < 0.05) and visfatin (mild: 11.63 ± 7.48; moderate: 15.24 ± 2.19; severe: 17.54 ± 2.98; p < 0.05) gradually increased, while level of vaspin decreased (mild: 317 ± 23.12; moderate: 269 ± 32.12; severe: 229 ± 14.24; p < 0.05). Subsequent results of Pearson coefficient analyses indicated that all of the tested adipose tissue-derived inflammatory factors were positively correlated with the BMI and HOMA-IR of the patients (all p < 0.05), even after adjustment for hs-CRP. Conclusions: The adipose tissue-derived inflammatory factors resistin, vaspin and visfatin may be involved in the pathogenesis of atherosclerosis in elderly T2DM patients. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 2682-49-7, help many people in the next few years.Related Products of 2682-49-7

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In the modern scenario, thiazolidinone scaffold has emerged as a very potent scaffold as per its clinical significance concerned. It has attracted the keen interest of the researchers due to its great diversity in biological activities. Thiazolidinones are the saturated form of thiazole, called thiazolidine with a carbonyl group. The 1,3-thiazolidin-4-ones possess wide range of pharmacological activities such as anti-cancer, anti-diabetic, anti-microbial, anti-viral, anti-inflammatory and anti-convulsant. In the past few years, various newer synthetic approaches have been designed to synthesize diverse scaffolds to explore the various types of biological activities. In this review, an attempt has been made by the authors to summarize various synthetic strategies for thiazolidinone derivatives as well as their biological significance.

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A new series of spiro 1,2,4-triazoles 5-9a-j were prepared by the reaction of appropriate amidrazones 4 with cyclic ketones in catalytic amount of p-toluene sulfonic acid. The structures of the titled compounds have been elucidated by the elemental analysis and spectroscopic data (IR, 1H NMR, 13C NMR and MS). The biological activities of the prepared compounds were investigated using well-established methods from the literature.

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A series of novel analogues of 2-(5-(1H-indol-3-yl)-1, 3, 4-thiadiazol-2-ylimino)- 5- (substituted benzylidene)thiazolidine-4-one have been synthesized. The structures of newly synthesized compounds were confirmed by FT-IR,1H-NMR,13C-NMR and Mass spectroscopy. The synthesized compounds showed significant antibacterial activity against gram-positive bacteria: Staphylococcus aureus (MTCC 3160), Bacillus subtilis (MTCC 2061), gram-negative Escherichia coli (MTCC 1652), Pseudomonas aeruginosa (MTCC 741) and antifungal activity against fungal strains: Candida albicans (MTCC 183) and Aspergillus Niger (MTCC 2110). Also, their anti-inflammatory activity was evaluated by using carrageenan-induced rat paw edema method. Compounds 7d and 7h with the methoxy substitution on phenyl ring were found as active derivatives of the series, exhibited 49.86% and 49.88% inhibition respectively as compared with Diclofenac sodium. In-silico molecular docking studies of the synthesized compounds was done on crystal structures of proteins of microbes Aspergillus Niger, Bacillus subtilis, Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and cyclooxygenase-2 using GRIP batch docking method of V-life MDS 3.0 software to study their observed activity which revealed a significant correlation between the binding score and biological activity for these compounds.

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Toxoplasma gondii severely threaten the health of immunocompromised patients and pregnant women as this parasite can cause several disease, including brain and eye disease. Current treatment for toxoplasmosis commonly have high cytotoxic side effects on host and require long durations ranging from one week to more than one year. The regiments lack efficacy to eradicate T. gondii tissue cysts to cure chromic infection results in the needs for long treatment and relapsing disease. In addition, there has not been approved drugs for treating the pregnant women infected by T. gondii. Moreover, Toxoplasma vaccine researches face a wide variety of challenges. Developing high efficient and low toxic agents against T. gondii is urgent and important. Over the last decade, tremendous progress have been made in identifying and developing novel compounds for the treatment of toxoplasmosis. This review summarized and discussed recent advances between 2009 and 2019 in exploring effective agents against T. gondii from five aspects of drug discovery.

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Thiazole frame work represents a vital pharmacophore in several areas of chemistry. Consequently, several synthetic protocols to construct and functionalize this core, in an attempt to generate diverse thiazole containing architectures have been developed by various researchers across the globe. These wide range of methodologies developed will allow the access to fully decorated thiazole containing new chemical entities that can find various application in the field of medicinal chemistry, agrochemicals and material science. This review will provide an insight in to the various synthons used in construction and diversification of this core. Diversely functionalized thiazole analogs are considered as a vital azole framework present in many natural products. This prominent heterocycle also constitutes an important pharmacophore in medicinal chemistry, in agrochemicals and in molecules for material science applications. All these above-mentioned features of thiazole necessitates the continuous development of efficient methods to access this heterocycle. Accordingly, various researchers across the globe have come up with efficient synthetic protocols in an attempt functionalize different positions of this important scaffold. This review aims at highlighting some of the latest synthetic approaches to di/tri-substituted thiazole analogs which are known to possess a wide spectrum of biological activities.

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In an attempt to identify potential new agents active against tuberculosis with Shikimate kinase as the target, a novel series of 2-phenyl- 3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one derivatives were synthesized by convenient one-pot three-component reaction of amine, aldehyde and mercaptoacetic acid on montmorillonite KSF clay as a solid acidic catalyst in good yields. The structures of the newly synthesized compounds were confirmed by IR, 1H-NMR and elemental analysis and were subjected for anti-tubercular activity by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv. Docking and ADMET studies were used to better describe the titled compounds as potential anti-tubercular agents. The compound, 2-(3,4-dimethoxyphenyl)-3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one(4j), was found to be the most active against Mycobacterium tuberculosis H37Rv with MIC of 1.6 mug/ml and good drug likeness and dock scores. Molecular docking study revealed that the molecules fit well into the cavity of Shikimate kinase. Also, the molecular properties and bioactivity scores for the synthesized compounds obtained by in-silico studies were found to be within the acceptable range defined for human use revealing their potential as possible drug-like compounds. The anti-tubercular activity of the titled compounds was comparable to that of the standard drug Isoniazid and Ciprofloxacin. The results indicate that the synthesized thiadiazolyl-thiazolidinone derivatives may have an affinity towards Shikimate kinase active site which can be further explored for selective target based studies. Thus these compounds could act as a potential lead for further anti-tubercular studies.

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Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug’s potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, name: Thiazolidin-2-one, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 2682-49-7

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