Orthosteric–allosteric dual inhibitors of PfHT1 as selective antimalarial agents
نویسندگان
چکیده
منابع مشابه
Identification of selective tubulin inhibitors as potential anti-trypanosomal agents.
The potency of a series of sulfonamide tubulin inhibitors against the growth of Trypanosoma brucei (T. brucei), as well as human cancer and primary fibroblast cells were evaluated with the aim of determining whether compounds that selectively inhibit parasite proliferation could be identified. Several compounds showed excellent selectivity against T. brucei growth, and have the potential to be ...
متن کاملOrally Active and Selective Tubulin Inhibitors as Anti-Trypanosome Agents
OBJECTIVES There is an urgent need to develop a safe, effective, orally active, and inexpensive therapy for African trypanosomiasis due to the drawbacks of current drugs. Selective tubulin inhibitors have the potential to be promising drug candidates for the treatment of this disease, which is based on the tubulin protein structural difference between mammalian and trypanosome cells. We propose...
متن کاملSynthesis of Plasmepsin II Inhibitors – Potential Antimalarial Agents
Abstract: A new series of plasmepsin II (PM II) inhibitors has been prepared based on 4-aminopiperidine-tert-butyl-carbamate (1). These compounds might be useful as antimalarial drugs acting via a new mechanism, and therefore be less susceptible to parasite resistance now often observed with current antimalarial therapies. Some of the final compounds prepared exhibited encouraging inhibitory ac...
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 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...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 2021
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.2017749118