7-Aza-des-A-steroids with Antimicrobial and Cytotoxic Activity

This paper describes a convenient approach to the 7-aza-des-A-steroid (6,6a,7,8,9,9a-hexahydro-5H-cyclopenta[h]quinoline) scaffold starting from Grundmann’s ketone using two different pyridine annulation protocols. The biological evaluation of the pyridine and pyridinium products revealed that these...

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Detalles Bibliográficos
Autores principales: Krojer, Melanie, Keller, Marco, Bracher, Franz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Österreichische Apotheker-Verlagsgesellschaft 2013
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3700069/
https://www.ncbi.nlm.nih.gov/pubmed/23833707
http://dx.doi.org/10.3797/scipharm.1303-03
Descripción
Sumario:This paper describes a convenient approach to the 7-aza-des-A-steroid (6,6a,7,8,9,9a-hexahydro-5H-cyclopenta[h]quinoline) scaffold starting from Grundmann’s ketone using two different pyridine annulation protocols. The biological evaluation of the pyridine and pyridinium products revealed that these compounds unexpectedly do not interfere with ergosterol and cholesterol biosynthesis. The pyridinium compound 6 showed significant antimicrobial and cytotoxic activities which are most likely due to its detergent-like structure.

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