4-Substituted anilino imidazo[1,2-a] and triazolo[4,3-a]quinoxalines. Synthesis and evaluation of in vitro biological activity
| Autor: | Giuseppe Paglietti, Paolo La Colla, Giuseppina Sanna, Gabriella Vitale, Gabriella Collu, Paola Corona, Mario Loriga, Roberta Loddo |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Chemical synthesis Cell Line Structure-Activity Relationship Quinoxalines Drug Discovery Humans Cytotoxicity Cell Proliferation Antibacterial agent Pharmacology Molecular Structure biology Cell growth Chemistry Organic Chemistry Imidazoles Biological activity General Medicine Triazoles biology.organism_classification Antimicrobial Corpus albicans In vitro Yeast Biochemistry Bacteria |
| Zdroj: | European Journal of Medicinal Chemistry. 41:1102-1107 |
| ISSN: | 0223-5234 |
| Popis: | Fifteen imidazo[1,2-a] and [1,2,4]triazolo[4,3-a]quinoxalines were prepared. These compounds bear at position 4 various substituents related to the moieties present in classical and non-classical antifolic agents. And we evaluated in vitro antimicrobial, antiviral and antiproliferative activities. In particular, title compounds were evaluated in vitro against representative strains of Gram-positive and Gram-negative bacteria (S. aureus, Salmonella spp.), mycobacteria (M. fortuitum, M. smegmatis ATCC 19420 and M. tuberculosis ATCC 27294), yeast and moulds (C. albicans ATCC 10231 and A. fumigatus). Furthermore, their antiretroviral activity against HIV-1 was determined in MT-4 cells together with cytotoxicity. In these assays title compounds were tested for their capability to prevent MT-4 cell growth. Among the examined series, the compounds 5, 7 and 10 showed cytotoxicity against mock-infected MT-4 cells. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect