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 | |
| Publication status | Published - Feb 13 2003 |
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ASJC Scopus subject areas
- Organic Chemistry
Cite this
New semisynthetic quassinoids with in vivo antimalarial activity. / Murakami, Nobutoshi; Sugimoto, Masanori; Kawanishi, Motoyuki; Tamura, Satoru; Kim, Hye-Sook; Begum, Khurshida; Wataya, Yusuke; Kobayashi, Motomasa.
In: Journal of Medicinal Chemistry, Vol. 46, No. 4, 13.02.2003, p. 638-641.Research output: Contribution to journal › Article
}
TY - JOUR
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.
UR - http://www.scopus.com/inward/record.url?scp=0037434546&partnerID=8YFLogxK
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U2 - 10.1021/jm0201971
DO - 10.1021/jm0201971
M3 - Article
VL - 46
SP - 638
EP - 641
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 4
ER -