Synthesis and antimicrobial activity of new 4-thiazolidinone derivatives containing 2-amino-6-methoxybenzothiazole

Patel, Navin B.; Shaikh, Faiyazalam M.

doi:10.1016/j.jsps.2010.05.002

Cited by 39 publications

(22 citation statements)

References 17 publications

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“…23,24 Several researchers have also investigated the antifungal activity of several derivatives of 4-thiazolidinones. 25 In the view of above mentioned findings and as continuation of our efforts to identify new candidates that may be of value in designing new potent, selective, and less toxic and less resistant antimicrobial agents, we report herein in the present work the synthesis and antimicrobial screening of some new 4-thiazolidinone derivatives starting from isonicotinic acid hydrazide.…”

Section: 9mentioning

confidence: 93%

Synthesis and Antimicrobial Activity of N-[2-(aryl/substituted aryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide

Thomas¹,

Nanda²,

Kothapalli³

et al. 2011

Journal of the Korean Chemical Society

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ABSTRACT. A series of isonicotinyl hydrazones and their 4-thiazolidinones have been synthesized by condensation of isonicotinic acid hydrazide with various aromatic aldehydes to yield Schiff's bases, followed by the cyclocondensation of Schiff's bases with 2-mercaptoacetic acid to yield their 4-thiazolidinones. The synthesized compounds have been characterized by their elemental, analytical and spectral studies. All these compounds were evaluated for their invitro antimicrobial activity against a spectrum of non-resistant and resistant microbial organisms. These studies proved that compounds 5e,i against B. subtilis; 5e,f,h against B. anthracis; 5g,i against S. aureus showed good activity at lower concentrations. Compounds 5d-5i displayed significant activity against resistant strain of K. pneumonia with minimum inhibitory potency in the concentration range of 2-16 ug/ml.

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Section: 9mentioning

confidence: 93%

Synthesis and Antimicrobial Activity of N-[2-(aryl/substituted aryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide

Thomas¹,

Nanda²,

Kothapalli³

et al. 2011

Journal of the Korean Chemical Society

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“…[8][9][10] Thiazolidinones are another class of heterocycle that are reported to possess anti-inflammatory, 11) anti-microbial, 12) anti-proliferative, 13,14) anti-viral, 15) anti-convulsant, 16,17) antifungal, 18) and anti-bacterial properties. 19) Recent reports indicate that these compounds possess anticancer properties. 20) Aminoflavones are a class of compounds that do not have any natural occurrence are reported to be highly selective towards breast cancer, and are considered as a new class of anti-cancer agents.…”

Section: )mentioning

confidence: 99%

Synthesis and Anti-cancer Activity of Novel Thiazolidinone Analogs of 6-Aminoflavone

Moorkoth

2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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Novel heterocyclic analogs were synthesized by combining a flavone nucleus and thiazolidinone ring in an effort to potentiate the existing anti-cancer activity of flavone. The syntheses of 6-aminoflavone, 6-amino-3-methoxyflavone, 6-amino-3-methoxy-3′,4′-dimethxyflavone and their corresponding thiazolidinone analogs were performed. Fifteen novel analogs were synthesized and evaluated for their anti-cancer activity using cell-based assay techniques and in vivo testing. As expected, the analogs improved cytotoxicity and were shown to increase the life span of cancer-bearing mice. Cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assays in HeLa, MDA-MB-435, and Vero cell lines. In vivo evaluation of anti-cancer activity performed in albino mice bearing Dalton's ascites carcinoma showed that the new analogs enhanced life span and prevented increases in body weight owing to tumor volumes. Moreover, cell-cycle analysis and Hoechst staining analysis proved the apoptotic potential of these analogs. Preliminary pharmacokinetic evaluation was carried out on the synthesized compounds to determine the lipophilicity and pK a . Lipophilicity was determined using high-performance liquid chromatography and the results showed a direct correlation between the observed anti-cancer activity and log P value, while pK a values indicated the ionizing range which is a prediction tool for solubility and permeability.Key words aminoflavone; thiazolidinone; anticancer; cytotoxicity; lipophilicity; in vivo activity Polyphenols such as flavonoids that contain chromone pharmacophore are known for their wide range of pharmacological activities. It is important to note that these compounds are non-toxic at concentrations that are normally consumed in a normal diet. A flavonoid-rich diet is also considered as a prophylactic treatment for cancer. Various clinical studies performed on flavonoids indicate that these molecules are potent chemotherapeutic agents against cancer. The anticancer activity of flavonoids is mainly by the inactivation of carcinogens, cell-cycle arrest, and by the induction of apoptosis.1) The approach to anticancer drug discovery is to develop cytotoxic agents that can differentiate cancer cells and normal cells. One way of synthesizing molecules with lesser toxicity would be to adopt the molecularly targeted therapeutics, which will provide sufficient selectivity to a receptor.2) The role of flavonoids in chemoprevention of cancer is well established. 3)Major highlight of flavonoids is that they act through multiple mechanisms such as angiogenesis inhibition, inactivation of carcinogen, 4-7) arresting the cell cycle and apoptosis induction. [8][9][10] Thiazolidinones are another class of heterocycle that are reported to possess anti-inflammatory, 11) anti-microbial, 12) anti-proliferative, 13,14) anti-viral, 15) anti-convulsant, 16,17) antifungal, 18) and anti-bacterial properties. 19) Recent reports indicate that these compounds possess anticancer properties. 20)Aminofla...

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“…[1][2][3] Heterocyclic compounds containing the five membared oxadiazole nucleus which shows the diversity against useful biological effects. [4][5][6][7][8] 1,3,4-oxadiazol derivatives were comprehensively studied in recent years for their biological and pharmaceutical applications. 1,3,4-oxadiazol derivatives displayed broad range of biological activities such as anti-tubercular, antimicrobial, anticancer, anti-HIV, anthelmintic activities and anti-inflamatory activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Study of Some New Thiazolidinon Derivatives

Patel¹

2017

WJPPS

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Synthesis and antimicrobial activity of new 4-thiazolidinone derivatives containing 2-amino-6-methoxybenzothiazole

Cited by 39 publications

References 17 publications

Synthesis and Antimicrobial Activity of N-[2-(aryl/substituted aryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide

Synthesis and Antimicrobial Activity of N-[2-(aryl/substituted aryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide

Synthesis and Anti-cancer Activity of Novel Thiazolidinone Analogs of 6-Aminoflavone

Synthesis and Biological Study of Some New Thiazolidinon Derivatives

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