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

Research output: Contribution to journal › Article › peer-review

26 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

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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title = "New semisynthetic quassinoids with in vivo antimalarial activity",

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.",

author = "Nobutoshi Murakami and Masanori Sugimoto and Motoyuki Kawanishi and Satoru Tamura and Kim, {Hye Sook} and Khurshida Begum and Yusuke Wataya and Motomasa Kobayashi",

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doi = "10.1021/jm0201971",

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T1 - New semisynthetic quassinoids with in vivo antimalarial activity

AU - Murakami, Nobutoshi

AU - Sugimoto, Masanori

AU - Kawanishi, Motoyuki

AU - Tamura, Satoru

AU - Kim, Hye Sook

AU - Begum, Khurshida

AU - Wataya, Yusuke

AU - Kobayashi, Motomasa

PY - 2003/2/13

Y1 - 2003/2/13

N2 - 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.

AB - 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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New semisynthetic quassinoids with in vivo antimalarial activity

Abstract

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