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1.
Bioorg Med Chem Lett ; 24(15): 3569-73, 2014 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-24951333

RESUMO

A one-pot, three-component, microwave assisted and conventional synthesis of new 3-(4-chloro-2-hydroxyphenyl)-2-(substituted) thiazolidin-4-one (4a-n) was carried out by using N,N-dimethylformamide as a solvent with high product yield. Among these synthesized compounds (4f, 4g, 4l and 4m) were found to be a broad spectrum molecule active against all bacterial and fungus strains tested, except fungus Aspergillus niger. Amongst the compounds (4g, 4l and 4m) were found to be more potent than respective standard drugs used in the experiment against Candida albicans, Staphylococcus aureus and Aspergillus flavus, respectively. All synthesized compounds were also tested for their cytotoxic activity against HeLa and MCF-7 cell lines by the sulforhodamine B (SRB) assay. This study shows that all compounds were non-cytotoxic in nature, and confirmed their antimicrobial specificity apart from any general cytotoxicity.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Micro-Ondas , Tiazolidinas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Aspergillus flavus/efeitos dos fármacos , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Relação Dose-Resposta a Droga , Células HeLa , Humanos , Células MCF-7 , Testes de Sensibilidade Microbiana , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Tiazolidinas/síntese química , Tiazolidinas/química
2.
Singapore Med J ; 53(5): e106-9, 2012 May.
Artigo em Inglês | MEDLINE | ID: mdl-22584986

RESUMO

Peritonitis is a common problem in patients undergoing peritoneal dialysis. However, peritonitis due to Cunninghamella (C.) bertholletiae, a fungus of the class Zygomycetes, is rare. We present a case of fungal peritonitis in a patient on continuous ambulatory peritoneal dialysis due to kidney rejection. Direct examination of the patient's peritoneal fluid showed fungal hyphae, and the culture was identified as C. bertholletiae. A cumulative dose of 1,600 mg fluconazole was given to the patient intraperitoneally over a one-week period. When his condition had stabilised, oral antifungal treatment was administered for two weeks. After removal of the Tenckhoff catheter, the patient was discharged with arteriovenous fistulation for haemodialysis. Zygomycosis due to C. bertholletiae is often fatal and non-responsive to systemic antifungal therapy. This case is the first from India with a successful outcome, and highlights the importance of early detection and intervention for successful outcome of peritonitis caused by C. bertholletiae.


Assuntos
Cunninghamella/isolamento & purificação , Fluconazol/administração & dosagem , Rejeição de Enxerto/complicações , Falência Renal Crônica/terapia , Mucormicose/tratamento farmacológico , Diálise Peritoneal Ambulatorial Contínua/efeitos adversos , Peritonite/tratamento farmacológico , Antifúngicos/administração & dosagem , Vias de Administração de Medicamentos , Seguimentos , Humanos , Falência Renal Crônica/complicações , Transplante de Rim , Masculino , Pessoa de Meia-Idade , Mucormicose/etiologia , Mucormicose/microbiologia , Peritonite/etiologia , Peritonite/microbiologia
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