Synthesis and antimalarial activities of several fluorinated artemisinin derivatives.
نویسندگان
چکیده
The carbonyl groups in several artemisinin derivatives were converted into geminal difluorinated compounds on treatment with diethylaminosulfur trifluoride. A number of other mono- and polyfluorinated artemisinin derivatives were prepared. Their in vitro antimalarial activities were all equal to or greater than the nonfluorinated analogs or precursors.
منابع مشابه
Cryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملCryptolepine and development of new antimalarial agents
Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...
متن کاملAntimalarial Activity of C-10 Substituted Triazolyl Artemisinin
We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial ac...
متن کاملStereoselective Synthesis Diastereoselective Synthesis of b-Ether Derivatives of Artemisinin, an Antimalarial Drug: The Effect of Nitrile on Stereoselectivity
Malaria is a life-threatening disease affecting a major portion of the world’s population with considerable loss of human life. Artemisinin, isolated from Artemisia annua, its oiland water-soluble derivatives, and other known antimalarials are recommended for artemisinin combination therapy by the World Health Organization. We have established a method for the stereoselective synthesis of bethe...
متن کاملC-16 artemisinin derivatives and their antimalarial and cytotoxic activities: syntheses of artemisinin monomers, dimers, trimers, and tetramers by nucleophilic additions to artemisitene.
Nucleophilic additions of lithium keto and ester enolates and mono- and bifunctional Grignard reagents to artemisitene provided C-16-derived artemisinin monomers, dimers, trimers, and tetramers whose antimalarial and cytotoxic activities have been evaluated.
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Journal of medicinal chemistry
دوره 38 20 شماره
صفحات -
تاریخ انتشار 1995