Design, synthesis of 4-aminoquinoline-derived thiazolidines and their antimalarial activity and heme polymerization inhibition studies
نویسندگان
چکیده
منابع مشابه
Inhibition of Heme Polymerization, the Mechanism of Antimalarial Activity in Phlomis caucasica Rech.f. (Lamiaceae)
Background: Malaria is one of the most important parasitic diseases in the world caused by Plasmodium species. The malaria parasite digests hemoglobin in vacuole to amino acids and heme. Plasmodium has got several detoxification mechanisms to protect itself from toxic heme. The most important mechanism is heme polymerization. Identifying compounds that inhibit heme polymerization is an approach...
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In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn(2+) complex]. The bisquino...
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Due to growing problems with drug resistance, there is an outstanding need for new, cost-effective drugs for the treatment of malaria. The 4-aminoquinolines have provided a number of useful antimalarials, and Plasmodium falciparum, the causative organism for the most deadly form of human malaria, is generally slow to develop resistance to these drugs. Therefore, diverse screening libraries of q...
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Background and objectives: Viola odorata L. is a grassy plant that grows in the humid regions and has been used to treat liver diseases and complicated and tropical fevers in Iranian traditional medicine (ITM). V. odorata has cold and humid temperament while the temperament of fever which is the most important symptom of malaria is the opposite. Antimalarial a...
متن کاملRelationship between antimalarial drug activity, accumulation, and inhibition of heme polymerization in Plasmodium falciparum in vitro.
We have investigated the contribution of drug accumulation and inhibition of heme polymerization to the in vitro activities of a series of antimalarial drugs. Only those compounds exhibiting structural relatedness to the quinolines inhibited heme polymerization. We could find no direct correlation between in vitro activity against chloroquine-susceptible or chloroquine-resistant isolates and ei...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2012
ISSN: 1475-6366,1475-6374
DOI: 10.3109/14756366.2012.666537