New semisynthetic quassinoids with in vivo antimalarial activity

Nobutoshi Murakami; Masanori Sugimoto; Motoyuki Kawanishi; Satoru Tamura; Hye Sook Kim; Khurshida Begum; Yusuke Wataya; Motomasa Kobayashi

doi:10.1021/jm0201971

New semisynthetic quassinoids with in vivo antimalarial activity

Nobutoshi Murakami, Masanori Sugimoto, Motoyuki Kawanishi, Satoru Tamura, Hye Sook Kim, Khurshida Begum, Yusuke Wataya, Motomasa Kobayashi

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25 Citations (Scopus)

Abstract

On the basis of a comparative analysis for stability in mouse serum between 15-O-acetylbruceolide and bruceolide 15-methyl carbonate, several 3,15-dialkyl carbonates of bruceolide were synthesized and their in vitro antimalarial activity was assessed. Methyl, ethyl, and isopropyl carbonates with pronounced in vitro activity were further evaluated for in vivo antimalarial potency. Both the methyl and ethyl carbonates significantly increased the life span of mice as compared with 3,15-di-O-accetylbruceolide and chloroquine.

Original language	English
Pages (from-to)	638-641
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	46
Issue number	4
DOIs	https://doi.org/10.1021/jm0201971
Publication status	Published - Feb 13 2003

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ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Cite this

Murakami, N., Sugimoto, M., Kawanishi, M., Tamura, S., Kim, H. S., Begum, K., Wataya, Y., & Kobayashi, M. (2003). New semisynthetic quassinoids with in vivo antimalarial activity. Journal of medicinal chemistry, 46(4), 638-641. https://doi.org/10.1021/jm0201971

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abstract = "On the basis of a comparative analysis for stability in mouse serum between 15-O-acetylbruceolide and bruceolide 15-methyl carbonate, several 3,15-dialkyl carbonates of bruceolide were synthesized and their in vitro antimalarial activity was assessed. Methyl, ethyl, and isopropyl carbonates with pronounced in vitro activity were further evaluated for in vivo antimalarial potency. Both the methyl and ethyl carbonates significantly increased the life span of mice as compared with 3,15-di-O-accetylbruceolide and chloroquine.",

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AU - Murakami, Nobutoshi

AU - Sugimoto, Masanori

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AU - Kim, Hye Sook

AU - Begum, Khurshida

AU - Wataya, Yusuke

AU - Kobayashi, Motomasa

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10.1021/jm0201971