Synthesis and antibacterial activity of 5-ylidenethiazolidin-4-ones and 5-benzylidene-4,6-pyrimidinediones

Tomašič, Tihomir; Zidar, Nace; Mueller‐Premru, Manica; Kikelj, D.; Mašič, Lucija Peterlin

doi:10.1016/j.ejmech.2009.12.030

Cited by 58 publications

(18 citation statements)

References 16 publications

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“…Furthermore, compound 3 exhibited an MIC value of >128 µg/mL towards two strains of Gram-negative bacteria (i.e., E. coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853). Compound 4, which was prepared to provide improved LogP properties over compound 3, gave the same results with MIC values >128 µg/mL against all of the bacterial strains tested in the study (Figure 4) [43].…”

Section: Naohmentioning

confidence: 60%

The Synthesis and Anti-Bacterial Activities of N-carboxymethyl Rhodanines

Piao¹

2014

Med chem

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A large number of reports have been published in recent years regarding the use of N-carboxymethyl rhodanines as antimicrobial agents. Molecules belonging to this structural class have been reported to exhibit good inhibitory activities towards various Gram-positive bacteria, including several multidrug-resistant strains such as methicillinresistant Staphylococcus aureus and quinolone-resistant Staphylococcus aureus. In this mini-review, we have provided a summary of recent research directed towards the synthesis of N-carboxymethyl rhodanines, and their pharmacological evaluation as antimicrobial agents.

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Section: Naohmentioning

confidence: 60%

The Synthesis and Anti-Bacterial Activities of N-carboxymethyl Rhodanines

Piao¹

2014

Med chem

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“…According to references [27][28][29][30][31], syntheses of these compounds result in (Z)-izomers. The same has recently been proved for 3-aminorhodanine derivatives [25].…”

Section: Resultsmentioning

confidence: 99%

(Z)-3-Amino-5-(pyridin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one

Hirsova

Dolezel²,

Kučerová-Chlupáčová

et al. 2015

Molbank

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“…Thus, later designs and screens focused on diphosphate analogs likely to be permeant, as with the MurB inhibitors discussed above. Several series of multiple‐ligase inhibitors contained rhodanines, 66–69 some of which showed antibacterial activity. Rhodanines are among those compounds known to have Pan‐Assay‐INterfering (PAIN) activity, 70 in some cases due to aggregation or alkylation and whose activity is often abrogated by serum proteins.…”

Section: Targets In the Cytoplasmic Portion Of The Main Pathway: Stage Imentioning

confidence: 99%

Viable screening targets related to the bacterial cell wall

Silver¹

2012

Annals of the New York Academy of Sciences

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The synthesis of the bacterial peptidoglycan has been recognized for over 50 years as fertile ground for antibacterial discovery. Initially, empirical screening of natural products for inhibition of bacterial growth detected many chemical classes of antibiotics whose specific mechanisms of action were eventually dissected and defined. Of the nontoxic antibiotics discovered, most were found to be inhibitors of either protein synthesis or cell wall synthesis, which led to more directed screening for inhibitors of these pathways. Directed screening and design programs for cell wall inhibitors have been undertaken since the 1960s. In that time it has become clear that, while certain steps and intermediates have yielded selective inhibitors and are established targets, other potential targets have not yielded inhibitors whose antibacterial activity is proven to be solely due to that inhibition. Why has this search been so problematic? Are the established targets still worth pursuing? This review will attempt to answer these and other questions and evaluate the viability of targets related to peptidoglycan synthesis.

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Synthesis and antibacterial activity of 5-ylidenethiazolidin-4-ones and 5-benzylidene-4,6-pyrimidinediones

Cited by 58 publications

References 16 publications

The Synthesis and Anti-Bacterial Activities of N-carboxymethyl Rhodanines

The Synthesis and Anti-Bacterial Activities of N-carboxymethyl Rhodanines

(Z)-3-Amino-5-(pyridin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one

Viable screening targets related to the bacterial cell wall

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