Design and De Novo Synthesis of 6-Aza-artemisinins
2018; American Chemical Society; Volume: 20; Issue: 15 Linguagem: Inglês
10.1021/acs.orglett.8b01987
ISSN1523-7060
AutoresKarunakar Reddy Bonepally, Takahisa Hiruma, Haruki Mizoguchi, Kyohei Ochiai, Shun Suzuki, Hideaki Oikawa, Aki Ishiyama, Rei Hokari, Masato Iwatsuki, Kazuhiko Otoguro, Satoshi Ōmura, Hiroki Oguri,
Tópico(s)Malaria Research and Control
ResumoDevelopment of designer natural product variants, 6-aza-artemisinins, enabled us to achieve structural modification of the hitherto unexplored cyclohexane moiety of artemisinin and concise de novo synthesis of the tetracyclic scaffold in just four steps from the modular assembly of three simple building blocks. This expeditious catalytic asymmetric synthetic approach generated lead candidates exhibiting superior in vivo antimalarial activities to artemisinin.
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