نتایج جستجو برای: antimalarial compounds
تعداد نتایج: 232060 فیلتر نتایج به سال:
the formation of hemozoin (malaria pigment) has been proposed as an ideal drug target for antimalarial screening programs. in this study, we used an improved, cost-effective and high-throughput spectrophotometric assay to screen plant extracts for finding novel antimalarial plant sources. fifteen extracts with different polarity from three iranian artemisia species, a. ciniformis, a. biennis an...
Plasmodium falciparum, the most deadly agent of malaria, displays a wide variety of resistance mechanisms in the field. The ability of antimalarial compounds in development to overcome these must therefore be carefully evaluated to ensure uncompromised activity against real-life parasites. We report here on the selection and phenotypic as well as genotypic characterization of a panel of sensiti...
The emergence and spread of drug resistant malaria represents a considerable challenge to controlling malaria. To date, malaria control has relied heavily on a comparatively small number of chemically related drugs, belonging to either the quinoline or the antifolate groups. Only recently have the artemisinin derivatives been used but mostly in south east Asia. Experience has shown that resista...
There is an urgent need to discover new antimalarials, due to the spread of chloroquine resistance and the limited number of available drugs. In the last few years, artemisinin, the endoperoxide sesquiterpene lactone derived from Artemisia annua, and its derivatives proved to be very active against Plasmodium falciparum. These compounds are characterized by an endoperoxide pharmacophore that is...
Quinazolinedione is one of the most notable pharmacophores in drug discovery due to its broad spectrum biological activities including antimalarial, anticancer, anti-inflammatory, and others. TCMDC-125133, whose structure features a quinazolinedione core, exhibits promising antimalarial activity low toxicity as described GlaxoSmithKline (GSK) report. Herein, concise four-step synthesis towards ...
This article reports the regioselective and chemoselective synthesis of 4,5-dialkoxy-2-nitroanilines substituted with two alkoxys at C-4 C-5. Here we show optimization protocol transetherification reaction used to synthesize 20 new compounds good excellent yields (50–92%). We describe a simple efficient one-step procedure that can be applied obtain significant number pharmacologically active co...
The activities of total extracts and lupane triterpenes, isolated from the stem bark of Acacia mellifera, were evaluated against Plasmodium berghei strain ANKA in a female Swiss mouse model. Five isolated compounds and the crude extracts were evaluated for antimalarial activity and Quinine hydrochloride was used as a positive control. Only betulin and the methanolic extract produced considerabl...
A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more active against non-replicating than replicating cultures of Mycobacterium tuberc...
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