Antimicrobial Activity and Mechanism of Action of New N-heteroaryl-1H-(benz)Imidazoles

• Tipo: Outra Publicação em Revista Científica Internacional
• Data: 2014

Autores

Eugenia Pinto (Autor) FFUP; Helena Neves (Autor) Outra; Karnjana Hrimpeng (Autor) Outra; Ana Filipa Silva (Autor) Outra; Agathe Begouin (Autor) Outra; Graciliana Lopes (Autor) Outra; Maria Joao R P Queiroz (Autor) Outra

Revista

Título: Mini-Reviews in Medicinal Chemistry

Vol. 14

Páginas: 941-952

ISSN: 1389-5575

Editora: Bentham Science

Indexação

ISI Web of Knowledge - 2 Citações

Scopus - 3 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

Outras Informações

ID Authenticus: P-009-YWZ

DOI: 10.2174/1389557514666141029225524

Abstract (EN): The antimicrobial activity of sixteen new N-heteroarylated 1H-(benz)imidazoles was evaluated against clinically relevant bacteria (Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa) and fungi (Candida, Aspergillus and dermatophyte) species according to the Clinical and Laboratory Standards Institute guidelines. None of the tested compounds were active against Gram negative bacteria, but only against S. aureus, that was particularly susceptible to N-thianthrenyl- and N-dibenzothienyl imidazole derivatives. Most of the imidazole derivatives showed a broad spectrum of antifungal activity in all tested fungal strains, including fluconazole-resistant species, with a particularly low minimum inhibitory concentration (MIC) for dermatophytes. N-(dibenzofuran-4-yl)-1H-imidazole (1) and N-(dibenzothien-4-yl)-1H-imidazole (3) showed the highest antifungal potential, being most active against Candida albicans. Some N-heteroarylated benzimidazoles showed low activity for fungi with the exception of 3-(1H-benzo [d]imidazol-1-yl)quinoline (14) which was selective against dermatophytes (MIC-4-16 mu g/mL). The effect of the active compounds in the inhibition of the dimorphic transition, ergosterol biosynthesis and mitochondrial activity was evaluated in C. albicans. Compounds 1 and 3 showed the capacity to inhibit the germ tube formation in C. albicans, reduced the ergosterol production and impaired the mitochondrial function. Compounds 1 and 3 showed antimicrobial activity and low cytotoxicity, being of interest for further investigation concerning specially the development of new antifungal agents.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 12