Journal ArticleDOI
Synthesis and antimicrobial activity of some new hydrazone-bridged thiazole-pyrrole derivatives.
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In this work, fourteen different compounds which contain hydrazone bridged thiazole and pyrrole rings were synthesized and screened for their antibacterial and antifungal activities against twelve different microorganisms by using microbroth dilution method.Abstract:
In this work, we synthesized fourteen different compounds which contain hydrazone bridged thiazole and pyrrole rings. For this purpose, pyrrole-2-carboxaldehydes were reacted directly with thiosemicarbazide in ethanol and then obtained thiosemicarbazones were condensed with α-bromoacetophenone derivatives (Hantzsch reaction) to give 1-substituted pyrrole-2-carboxaldehyde [4-(4-substituted phenyl)-1,3-thiazol-2-yl] hydrazones. The structures of the obtained compounds were elucidated by using IR, (1)H-NMR and FAB(+)-MS spectral data and elemental analyses results. All of the compounds were screened for their antibacterial and antifungal activities against twelve different microorganisms by using microbroth dilution method. Ketoconazole and chloramphenicol were used as standard drugs. All of the compounds showed good activity against Staphylococcus aureus and Enterococcus faecalis.read more
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Journal ArticleDOI
Synthesis of a Sugar-Based Thiosemicarbazone Series and Structure-Activity Relationship versus the Parasite Cysteine Proteases Rhodesain, Cruzain, and Schistosoma mansoni Cathepsin B1
Nayara Cristina Fonseca,Luana Faria da Cruz,Filipe Silva Villela,Glaécia Aparecida do Nascimento Pereira,Glaécia Aparecida do Nascimento Pereira,Jair L. Siqueira-Neto,Danielle Kellar,Brian M. Suzuki,Debalina Ray,Thiago Belarmino de Souza,Ricardo José Alves,Policarpo Ademar Sales Junior,Alvaro J. Romanha,Alvaro J. Romanha,Silvane M. F. Murta,James H. McKerrow,Conor R. Caffrey,Renata Barbosa de Oliveira,Rafaela Salgado Ferreira +18 more
TL;DR: The thiosemicarbazones and heterocyclic analogues have been shown to be both antitrypanocidal and inhibitory against parasite cysteine proteases and a series of compounds synthesized and evaluated against cruzain, rhodesain, and SmCB1 through biochemical assays revealed active compounds among this series.
Journal ArticleDOI
An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives.
TL;DR: An overview of different methods for the synthesis of thiazole and bisthiazole derivatives can be found in this article, which describes various compounds bearing a thiazoleside and bistshiazoles moiety possessing antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects.
Journal ArticleDOI
Inhibition activity of new thiazole hydrazones towards mild steel corrosion in acid media by thermodynamic, electrochemical and quantum chemical methods
TL;DR: In this article, the mild steel anti-corrosion potential by newly synthesized thiazole hydrazones, 4-(4methoxy-phenyl)-thiazole-2-carboxylic acid benzylidene-hydrazide (TH-1), 4-(methoxphenyl)thiazoles, 2.5 M hydrochloric acid was studied by gravimetric and electrochemical techniques, and the results showed that addition of inhibitors simultaneously decreased corrosion current density and double layer capacitance but increased charge transfer resistance.
Journal ArticleDOI
Synthesis, biological evaluation and molecular docking studies of thiazole-based pyrrolidinones and isoindolinediones as anticonvulsant agents
Hazem A. Ghabbour,Hazem A. Ghabbour,Adnan A. Kadi,Kamal E.H. ElTahir,Rihab F. Angawi,Hussein I. El-Subbagh +5 more
TL;DR: In this paper, a series of new 1-(thiazol-2-yl)pyrrolidinones 5a-m and isoindolinediones 6a-l were synthesized and tested as anticonvulsant.
Journal ArticleDOI
Microwave assisted synthesis of five membered nitrogen heterocycles
TL;DR: In this article, a review of the developments in microwave assisted synthesis of pyrroles and other five-membered nitrogen heterocycles is presented, focusing on the developments of microwave assisted organic synthesis.
References
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TL;DR: 3 case histories-one involving Escherichia coli resistance to third-generation cephalosporins, another focusing on the emergence of vancomycin-resistant Staphylococcus aureus, and a third detailing multidrug resistance in Pseudomonas aeruginosa--are reviewed to illustrate the varied ways in which resistant bacteria develop.
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Biological activities of hydrazone derivatives.
Sevim Rollas,Ş. Güniz Küçükgüzel +1 more
TL;DR: There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities.
Journal ArticleDOI
Trends in Antimicrobial Drug Development: Implications for the Future
TL;DR: The need for new antimicrobial agents is greater than ever because of the emergence of multidrug resistance in common pathogens, the rapid emergence of new infections, and the potential for use of multi-drug-resistant agents in bioweapons.
Journal ArticleDOI
The future challenges facing the development of new antimicrobial drugs
TL;DR: This work focuses primarily on an alternative novel strategy for antibacterial drug development that could potentially alleviate the current situation of drug resistance — targeting non-multiplying latent bacteria, which prolong the duration of antimicrobial chemotherapy and so might increase the rate of development of resistance.