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Stana A.,University of Medicine and Pharmacy, Cluj-Napoca | Tiperciuc B.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Pirnau A.,Romanian Institute of Isotopic And Molecular Technology | And 2 more authors.
Journal of the Serbian Chemical Society | Year: 2014

A series of new 5-(2,6-dichlorobenzylidene)thiazolidine-2,4-dione and 5-(4-methoxybenzylidene)thiazolidine-2,4-dione derivatives (3a-h and 5a-h, respectively) were synthesized starting from 5-arylidenethiazolidine- -2,4-dione and α-halo-ketones. The structural elucidation of the newly synthesized compounds was based on elemental analysis and spectroscopic data (MS, 1H-NMR and 13C-NMR). The synthesized compounds were screened in vitro for their antimicrobial activities against several pathogenic strains of Gram-positive and Gram-negative bacteria and one fungal strain (Candida albicans), as growth inhibition diameters. Some of the compounds displayed better inhibitory activities than that of the reference drug against the Gram- -positive Staphylococcus aureus, Bacillus cereus and Listeria monocytogenes bacterial strains, and showed good antifungal activity against C. albicans, while the antibacterial activity against the Gram-negative Escherichia coli and Salmonella typhimurium bacterial strains was moderate. © 2014 (CC) SCS.


Tiperciuc B.,University of Medicine and Pharmacy, Cluj-Napoca | Zaharia V.,University of Medicine and Pharmacy, Cluj-Napoca | Colosi I.,University of Medicine and Pharmacy, Cluj-Napoca | Moldovan C.,University of Medicine and Pharmacy, Cluj-Napoca | And 5 more authors.
Journal of Heterocyclic Chemistry | Year: 2012

A series of new 1,3,4-oxadiazole/thiadiazole and 1,2,4-triazole derivatives have been synthesized starting from 2-aryl-4-methylthiazol-5-carbohydrazides and isonicotinic acid hydrazide. All the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectrometry. The synthesized compounds were screened for their antibacterial and antifungal activity, assessed as growth inhibition diameter. Some of them showed good antibacterial activity against gram positive Staphylococcus aureus, while the antibacterial activity against Listeria monocytogenes, Escherichia coli, and Salmonella typhymurium and antifungal activity against Candida albicans was modest. None of the tested compounds showed inhibitory activity against gram positive bacteria Enterococcus faecalis and Bacillus cereus and against gram negative bacteria Pseudomonas aeruginosa. © 2012 HeteroCorporation.


Nastasa C.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Marie C.,French Institute of Health and Medical Research | Scherman D.,French Institute of Health and Medical Research | And 2 more authors.
Digest Journal of Nanomaterials and Biostructures | Year: 2013

The continuous need for discovering new antimicrobial agents, resulted from the alarming development process of bacterial resistance, and for new antiproliferative compounds, derived from the alarming increase of cancers all over the world, determined us to obtain new N-substituted 5-chromenyl thiazolidinediones and evaluate them as antimicrobial and antiproliferative agents. The synthetic route started with the condensation of 2,4-thiazolidinedione with 3-formyl-chromones. The new derivatives were treated after with various alkyl halides or 2-iodoacetamide, in order to obtain N-substituted compounds. The purity was confirmed by TLC, and all new molecules were characterized by elemental analysis and spectroscopic data (NMR, MS). The antimicrobial activity was assessed on Gram-positive and Gram-negative bacteria and one fungal strain. The compounds showed a promising potential. The antiproliferative effect was evaluated on both murine and human cancer lines and demonstrated a moderate active of the tested new derivatives.


Rozsa T.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Vlase L.,University of Medicine and Pharmacy, Cluj-Napoca | Ionut I.,University of Medicine and Pharmacy, Cluj-Napoca | And 3 more authors.
Journal of Heterocyclic Chemistry | Year: 2015

Thiazole and bisthiazole derivatives represent a prevalent scaffold in the antimicrobial drug discovery. Therefore, we have decided to synthesize some new series of 4,5′-bisthiazoles. A total of 17 compounds were synthesized, their structural elucidation being based on elemental analysis (C,H,N,S) and spectroscopic data (MS and 1H NMR). Their in vitro antimicrobial activities were assessed against several Gram-positive and Gram-negative bacteria strains and also against one fungal strain (Candida albicans) using the difusimetric method. Some of the compounds showed modest to good antibacterial activity against Gram-negative Escherichia coli and Salmonella typhimurium and Gram-positive Staphylococcus aureus and Bacillus cereus bacterial strains. All of the synthesized compounds showed moderate to very good antifungal activity against C. albicans. © 2014 HeteroCorporation.


Stana A.,University of Medicine and Pharmacy, Cluj-Napoca | Tiperciuc B.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Vlase L.,University of Medicine and Pharmacy, Cluj-Napoca | And 3 more authors.
Journal of Heterocyclic Chemistry | Year: 2014

A total of 17 new N-substituted derivatives (2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i, 2j, 2k and 3b, 3c, 3d, 3e, 3f, 3g, 3h) of 5-((2-phenylthiazol-4-yl) methylene) thiazolidine-2,4-dione (2a) and 5-(2,6-dichloro- benzylidene) thiazolidine-2,4-dione (3a) were synthesized. The structural elucidation of the newly synthesized compounds was based on elemental analysis and spectroscopic data (MS, 1H NMR, 13C NMR), and their antimicrobial activities were assessed in vitro against several strains of Gram-positive and Gram-negative bacteria and one fungal strain (Candida albicans) as growth inhibition diameter. Some of them showed modest to good antibacterial activity against Gram-negative Escherichia coli and Salmonella typhimurium and Gram-positive Staphylococcus aureus, Bacillus cereus, and Enterococcus fecalis bacterial strains, whereas almost all the compounds were inactive against Listeria monocytogenes. All of the synthesized compounds showed moderate to very good activity against C. albicans. © 2013 HeteroCorporation.


Rad O.,University of Medicine and Pharmacy, Cluj-Napoca | Tibor R.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Vlase L.,University of Medicine and Pharmacy, Cluj-Napoca | And 4 more authors.
Studia Universitatis Babes-Bolyai Chemia | Year: 2016

Starting from 5-amino-2-mercapto-1,3,4-thiadiazole, 23 compounds, Schiff bases and S-mercapto-substituted derivatives, were synthesized. Their structural elucidation was based on elemental analysis, mass spectrometry and proton nuclear magnetic resonance spectroscopy (1H NMR). The screening of the antimicrobial activity of the title compounds was realized using the diffusimetric method against several strains of Gram-positive and Gramnegative bacteria and one fungal strain (Candida albicans). Some of the molecules showed moderate to good antibacterial activity against Gramnegative (S. typhimurium, E. coli) and better activity against Gram-positive (B. cereus, L. monocytogenes, S. aureus) bacterial strains. All compounds exhibited moderate to very good activity against C. albicans. Qualitative relationships (SAR) were also established between the chemical structures and the antimicrobial activity of these compounds. © 2016, Universitatea Babes-Bolyai, Catedra de Filosofie Sistematica. All Rights Reserved.


Nastasa C.M.,University of Medicine and Pharmacy, Cluj-Napoca | Duma M.,State Veterinary Laboratory for Animal Health and Food Safety | Pirnau A.,Romanian Institute of Isotopic And Molecular Technology | Vlase L.,University of Medicine and Pharmacy, Cluj-Napoca | And 2 more authors.
Clujul Medical | Year: 2016

Background and aims. In the context of the increasing phenomenon of microbial resistance to usual drugs, the development of new treatment strategies and new therapeutic protocols is a constant need. Thiazolidinedione and chromone represent two important scaffolds in medicinal chemistry due to their large pharmacological applicability. Methods. We synthesized a new 5-(chromene-3-yl)methylene-2,4-thiazolidinedione starting from 6,8-dichloro-4-oxo-4H-chromene-3-carbaldehyde. Then, by treating with different α-bromoalkylarylketones, we obtained N-substituted derivatives. All new compounds were investigated for their antimicrobial potential, using the diffusion method, against Listeria monocytogenes ATCC 13932, Staphylococcus aureus ATCC 49444, Escherichia coli ATCC 25922, Salmonella typhimurium ATCC 14028 and Candida albicans ATCC 10231. Three concentrations, 10 mg/ml, 5 mg/ml and 1 mg/ml of compounds were used. The results were evaluated by the measurement of the inhibition zone diameters and compared to those of gentamicin and fluconazole respectively, as reference drugs. Results. All new synthesized compounds were characterized using physicochemical and spectrometric methods. They displayed modest to good antimicrobial activity. New molecules 8, 9 and 10 may represent promising candidates, showing zone inhibition diameters superior to those of reference drugs. Conclusions. This work presents chemical synthesis, characterization and investigation of the antibacterial and antifungal potential of 5-(chromene-3-yl) methylene-2,4-thiazolidinedione derivatives, which may be worthy of future research for designing new chemical entities.


PubMed | State Veterinary Laboratory for Animal Health and Food Safety, University of Medicine and Pharmacy, Cluj-Napoca and Romanian Institute of Isotopic And Molecular Technology
Type: Journal Article | Journal: Clujul medical (1957) | Year: 2016

In the context of the increasing phenomenon of microbial resistance to usual drugs, the development of new treatment strategies and new therapeutic protocols is a constant need. Thiazolidinedione and chromone represent two important scaffolds in medicinal chemistry due to their large pharmacological applicability.We synthesized a new 5-(chromene-3-yl)methylene-2,4-thiazolidinedione starting from 6,8-dichloro-4-oxo-4H-chromene-3-carbaldehyde. Then, by treating with different -bromoalkylarylketones, we obtained N-substituted derivatives. All new compounds were investigated for their antimicrobial potential, using the diffusion method, against Listeria monocytogenes ATCC 13932, Staphylococcus aureus ATCC 49444, Escherichia coli ATCC 25922, Salmonella typhimurium ATCC 14028 and Candida albicans ATCC 10231. Three concentrations, 10 mg/ml, 5 mg/ml and 1 mg/ml of compounds were used. The results were evaluated by the measurement of the inhibition zone diameters and compared to those of gentamicin and fluconazole respectively, as reference drugs.All new synthesized compounds were characterized using physico-chemical and spectrometric methods. They displayed modest to good antimicrobial activity. New molecules 8, 9 and 10 may represent promising candidates, showing zone inhibition diameters superior to those of reference drugs.This work presents chemical synthesis, characterization and investigation of the antibacterial and antifungal potential of 5-(chromene-3-yl)methylene-2,4-thiazolidinedione derivatives, which may be worthy of future research for designing new chemical entities.

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