Design, synthesis and biological characterization of thiazolidin-4-one derivatives as promising inhibitors of Toxoplasma gondii

D’Ascenzio, Melissa; Bizzarri, Bruna; Monte, Celeste De; Carradori, Simone; Bolasco, Adriana; Secci, Daniela; Rivanera, Daniela; Faulhaber, Nathan; Bordón, Claudia; Jones‐Brando, Lorraine

doi:10.1016/j.ejmech.2014.08.046

Cited by 47 publications

(41 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The produced compound exhibited amazing growth inhibition at single dosage. D' Ascenzio et al [52] have incorporated innumerable novel thiazolidin-4-one subsidiaries 26 for the assessment of their anti-toxoplasma gondii action. The results showed that thiazole-based compounds were assessed favorably to control parasite growth.…”

Section: Rosy Et Almentioning

confidence: 99%

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

P¹,

M²,

Santhanalakshmi³

et al. 2019

Asian J Pharm Clin Res

View full text Add to dashboard Cite

In the new millennium, we have novel biological targets which are defined at the molecular level, which have incredible success in comprehending human illness. On the other hand, the drug design processes are largely including pharmaceutical research study, scientific intuition, reaction and expertise to drive. Final thoughts attracted from this analysis can perform crucial function shaping the way our team believe concerning existing as well as future projects. With its origins rooted in natural synthesis as well as medicinal chemistry, heterocyclic compounds are existed themselves as a fundamental department of organic chemistry. IUPAC defined “cyclic compounds possessing ring members with atoms of at least two distinct elements" 1. Heterocyclic ring structures are core substances made up of components aside from carbon, where one of the most usual substituents is oxygen, nitrogen as well as sulphur 2, 3. According to the heteroatom(s) existing in the ring structure, heterocyclic could be recorded as oxygen, nitrogen or sulfur based and within each and every class of compound is based on the size of the ring structure, determined by the total number of atoms 4. The type and size of the ring structures, as one with the substituent groups of the core scaffold, impact is strongly on the physico-chemical properties 5. Heating responses with conventional devices, such as oil bath and also home heating mantles, are not only slow, yet additionally it produces a hot surface area on the reaction vessel where reagents, items and substrates are frequently disintegrate after at some time. Microwave power alternatively, is brought right into the chemical reactor from another location and travels through the walls of the response vessel, warming the catalysts and solvents directly. Microwave dielectric heating drives chain reactions by manipulating the benefit of the potential of some solids and liquids to change electromagnetic radiation into warm. Recently, a new technique has actually concerned the leading edge of chemical investigation, that is, microwave dielectric heating. In a similar method to the introduction of the isomantle, this technical advancement will no question need an adjustment in the drug store's mind set. In the future, the drug store will make use of fast blasts of microwave power to heat and also increase chemical reactions, as opposed to an alternate application in the very first circumstances for the mantle or hot plate. High-speed synthesis with microwaves has actually attracted a significant quantity of rate of interest in most recent years 6. Considering that, the very first reports on the usage of microwave home heating by Gedye and also Giguere / Majetich groups in speeding up organic chemical conversion in 1986, far more than 2,000 write-ups have been released in the area of Microwave Assisted Organic Synthesis 7, 8.

show abstract

Section: Rosy Et Almentioning

confidence: 99%

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

P¹,

M²,

Santhanalakshmi³

et al. 2019

Asian J Pharm Clin Res

View full text Add to dashboard Cite

show abstract

“…A data set comprising of 68 inhibitors of T. gondii based on thiazolidin-4-one was obtained from the work of Bizzarri et al (D'Ascenzio et al, 2014). The experimental therapeutic indexes together with thiazolidin-4-one analogs are given in Table 1.…”

Section: Data Set Molecular Optimization and Descriptors Calculationmentioning

confidence: 99%

“…Novel thiazolidin-4-one analogs are reported recently as effective inhibitors with minor cell toxicity (D'Ascenzio et al, 2014), measured by therapeutic index [TI = median cytotoxic dose (TD 50 )/median inhibitory concentration (IC 50 )]. However, more surveys are required to find more selective and potent inhibitors with less toxicity.…”

Section: Introductionmentioning

confidence: 99%

Therapeutic index modeling and predictive QSAR of novel thiazolidin-4-one analogs against Toxoplasma gondii

Asadollahi-Baboli

Mani-Varnosfaderani

2015

European Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…On the other hand, thiazoles have diverse biological activities . Recently, several articles reported about the pharmacological properties of thiazole derivatives as histone acetyltransferase inhibitors , anti‐toxoplasma gondii , and antimicrobial activity . Based on the above advantage of those heterocycles and continuation of our previous studies , we reported herein the synthesis of new pyridines, pyrido‐coumarins, and pyrido‐thiazoles to investigate their antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Antimicrobial Evaluation of some Novel Pyridine, Coumarin, and Thiazole Derivatives

Khidre

El‐Gogary

Mostafa

2017

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

in Wiley Online Library (wileyonlinelibrary.com).Treatment of 2-cyano-N 0 -(1-(pyridin-2-yl)ethylidene)acetohydrazide 1 with aromatic/heterocyclic aldehydes 2a-f gave arylidene derivatives 3a-f. Polysubstituted pyridine derivatives 4a,b were prepared either from reaction of arylidene 3a,b with malononitrile or from reaction of acetohydrazide 1 with arylidenemalononitrile 5a,b. Cyclocondensation of acetohydrazide 1 with salicylaldehyde derivatives and acetylacetone furnished pyrido-coumarins 6,7 and 2-pyridone-3-carbonitrile 8, respectively. In addition, pyrido-thiazoles 13 and 15 were obtained through reaction of 2-(1-(pyridin-2-yl)ethylidene) hydrazinecarbothioamide 11 with hydrazonyl chlorides and α-haloketones, respectively. The structures of synthesized compounds were elucidated with spectral and elemental data. The antimicrobial activity of the synthesized compounds was studied. J. Heterocyclic Chem., 54, 2511 (2017). Scheme 1. Synthesis of compounds 3a-f and 4a,b. Scheme 2. Synthesis of compounds 6a,b and 7a,b.

show abstract

Design, synthesis and biological characterization of thiazolidin-4-one derivatives as promising inhibitors of Toxoplasma gondii

Cited by 47 publications

References 28 publications

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

Therapeutic index modeling and predictive QSAR of novel thiazolidin-4-one analogs against Toxoplasma gondii

Design, Synthesis, and Antimicrobial Evaluation of some Novel Pyridine, Coumarin, and Thiazole Derivatives

Contact Info

Product

Resources

About