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Efforts To Access the Potent Antitrypanosomal Marine Natural Product Janadolide: Synthesis of Des-tert-butyl Janadolide and Its Biological Evaluation

[Image: see text] To identify novel antitrypanosomal agents based on Janadolide, a potent macrocyclic polyketide–peptide hybrid, a macrolactonization strategy was explored. We prepared des-tert-butyl Janadolide and evaluated its antitrypanosomal activity. Our findings suggest that the tert-butyl gro...

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Detalles Bibliográficos
Autores principales: Athawale, Paresh R., Jachak, Gorakhnath R., Shukla, Anurag, Shanmugam, Dhanasekaran, Reddy, D. Srinivasa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6044843/
https://www.ncbi.nlm.nih.gov/pubmed/30023831
http://dx.doi.org/10.1021/acsomega.7b01920
Descripción
Sumario:[Image: see text] To identify novel antitrypanosomal agents based on Janadolide, a potent macrocyclic polyketide–peptide hybrid, a macrolactonization strategy was explored. We prepared des-tert-butyl Janadolide and evaluated its antitrypanosomal activity. Our findings suggest that the tert-butyl group is necessary for the desired bioactivity.