ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
基本信息
- 批准号:3839828
- 负责人:
- 金额:--
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:
- 资助国家:美国
- 起止时间:至
- 项目状态:未结题
- 来源:
- 关键词:Moniliales Plasmodium berghei Plasmodium falciparum antimalarial agents chemical structure function chemical substitution chemical synthesis drug design /synthesis /production folk medicine hydroxyl group laboratory mouse malaria malaria vaccines medicinal plants microorganism culture microorganism disease chemotherapy microorganism metabolism molecular asymmetry molecular polarity nonhuman therapy evaluation nuclear magnetic resonance spectroscopy sesquiterpenes stereochemistry
项目摘要
Some 270 million people worldwide are infected with malaria which causes
between 1 and 2 million deaths per year. The formidable problems
encountered in developing a malaria vaccine, and the ability of Plasmodium
falciparum to become resistant to new drugs, has stimulated the World
Health Organization and others to search for new drigs to treat this
disease. Artemisinin has served as a lead compound to develop new drugs
to treat the resistant strains of P. falciparum that have spread ouver
southeast Asia and threaten India and Aftica. Since no strains P.
falciparum resistant to artemisinin derivatives have appeared, many
derivatives (esters and ethers of dihydtoartemisinin) have been prepared
in China and the United States. Metabolic studies of arteether, a
dihydroartemisinin derivative scheduled for clinical tests, found that it
is rapidly dealkylated to dihydroartemisinin. It is very likely that
esters of dihydroartemisinin are rapidly hydrolyzed to the same compound.
In order to prepare compounds that can not be degraded to
dihydroartemisinin, we introduced additional functional groups into
artemisinin by a microbially mediated oxidation using Beauveria
sulfurescens. Derivatives of these hydroxylated materials hiave been
prepared and tested. IN a second approach we replaced by hydroxy group of
dihydroartemisinin with an allyl group. The double bond of the allyl
substitutent enabled us to introduce polar groups into the molecule so as
to adjust its lipo- or hydro-philicity. The polarity is important in
deciding the mode of administration. Most of the compounds were found to
be as or more effective than artemisinin and arteether against P.
falciparum in vitro. The best compound, the n-propyl derivative, is
undergoing in vivo testing in mice infected with P. berghei.
全世界约有2.7亿人感染疟疾
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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{{ truncateString('H ZIFFER', 18)}}的其他基金
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
5201943 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3776276 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
4689595 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3754167 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3964446 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3875833 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3917716 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3854783 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
6161927 - 财政年份:
- 资助金额:
-- - 项目类别:
ASYMMETRIC SYNTHESIS--STRUCTURE, STEREOCHEMISTRY AND NMR
不对称合成——结构、立体化学和核磁共振
- 批准号:
3940611 - 财政年份:
- 资助金额:
-- - 项目类别:
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