An approach to the synthesis of novel 11-hydroxyartemisinin derivatives

1991 ◽  
Vol 56 (5) ◽  
pp. 1037-1041 ◽  
Author(s):  
Orlin Petrov ◽  
Iliya Ognyanov
Keyword(s):  
Antimalarial Drugs ◽  
Artemisinin Derivatives

The conversion of artemisinin (I) to the epoxide V and its use for the preparation of novel artemisinin derivatives as potential antimalarial drugs is described.

scholarly journals Rapid quantification of artemisinin derivatives in antimalarial drugs with dipstick immunoassays

2020 ◽  
Vol 191 ◽  
pp. 113605
Author(s):  
Jingqi Qian ◽  
Qingqing He ◽  
Lulu Liu ◽  
Mian Wang ◽  
Baomin Wang ◽  
...  
Keyword(s):  
Antimalarial Drugs ◽  
Artemisinin Derivatives ◽  
Rapid Quantification

scholarly journals Availability of Antimalarial Drugs and Evaluation of the Attitude and Practices for the Treatment of Uncomplicated Malaria in Bangui, Central African Republic

2010 ◽  
Vol 2010 ◽  
pp. 1-5 ◽  
Author(s):  
Alexandre Manirakiza ◽  
Siméon Pierre Njuimo ◽  
Alain Le Faou ◽  
Denis Malvy ◽  
Pascal Millet
Keyword(s):  
Uncomplicated Malaria ◽  
Health Workers ◽  
Combined Treatment ◽  
Multidrug Resistant ◽  
Antimalarial Drugs ◽  
Health Care Facilities ◽  
Management Policy ◽  
National Guidelines ◽  
Cross Sectional ◽  
Artemisinin Derivatives

National malaria management policy is based upon the availability of effective and affordable antimalarial drugs. This study was undertaken to evaluate the quality of the treatment of uncomplicated malaria cases in Bangui, an area with multidrug-resistant parasites, at a time preceding implementation of a new therapeutic policy relying on the artemisinin derivative combined treatment artemether-lumefantrine. A cross-sectional study was carried out in Bangui city to assess availability of antimalarial drugs and the performances of health workers in the management of uncomplicated malaria. Availability of drugs was recorded in all drugs wholesalers (n=3), all pharmacies in health facilities (n=14), private drugstores (n=15), and in 60 non-official drug shops randomly chosen in the city. Despite a limited efficacy at the time of the survey, chloroquine remained widely available in the official and nonofficial markets. Artemisinin derivatives used in monotherapy or in combination were commonly sold. In health care facilities, 93% of the uncomplicated malaria cases were treated in the absence of any laboratory confirmation and the officially recommended treatment, amodiaquine-sulfadoxine/pyrimethamine, was seldom prescribed. Thus, the national guidelines for the treatment of uncomplicated malaria are not followed by health professionals in Bangui. Its use should be implemented while a control of importation of drug has to be reinforced.

scholarly journals The Use of Antimalarial Drugs against Viral Infection

2020 ◽  
Vol 8 (1) ◽  
pp. 85 ◽  
Author(s):  
Sarah D’Alessandro ◽  
Diletta Scaccabarozzi ◽  
Lucia Signorini ◽  
Federica Perego ◽  
Denise P. Ilboudo ◽  
...  
Keyword(s):  
Ebola Virus ◽  
Viral Infections ◽  
Antimalarial Drugs ◽  
Drug Resistant ◽  
Emerging Viruses ◽  
Antimicrobial Drugs ◽  
Artemisinin Derivatives ◽  
Antiviral Activities

In recent decades, drugs used to treat malaria infection have been shown to be beneficial for many other diseases, including viral infections. In particular, they have received special attention due to the lack of effective antiviral drugs against new emerging viruses (i.e., HIV, dengue virus, chikungunya virus, Ebola virus, etc.) or against classic infections due to drug-resistant viral strains (i.e., human cytomegalovirus). Here, we reviewed the in vitro/in vivo and clinical studies conducted to evaluate the antiviral activities of four classes of antimalarial drugs: Artemisinin derivatives, aryl-aminoalcohols, aminoquinolines, and antimicrobial drugs.

From studies on artemisinin derivatives to trioxaquines

2002 ◽  
Vol 06 (04) ◽  
pp. 271-273 ◽  
Author(s):  
Bernard Meunier
Keyword(s):  
Malaria Parasite ◽  
Alkylating Agent ◽  
Antimalarial Drugs ◽  
Reduced Form ◽  
Artemisinin Derivatives ◽  
Main Target ◽  
Covalently Linked

Heme, resulting from hemoglobin digestion by the malaria parasite is one of the main target of antimalarial drugs like chloroquine and artemisinin. This later molecule contains a trioxane which is activated by the reduced form of heme to generate a strong alkylating agent able to react with heme itself. Taking advantage of these studies, we prepared new antimalarial drugs, trioxaquines, containing a trioxane motif covalently linked to an aminoquinoline.

scholarly journals THE TRAGEDY CAUSED BY FAKE ANTIMALARIAL DRUGS

2012 ◽  
Vol 4 (1) ◽  
pp. e2012027 ◽  
Author(s):  
Pierre Ambroise-Thomas
Keyword(s):  
Developing Countries ◽  
Health Problem ◽  
Artemisinin Resistance ◽  
Antimalarial Drugs ◽  
Pharmaceutical Market ◽  
African Countries ◽  
Artemisinin Derivatives ◽  
International Programme

Counterfeit antimalarials (mainly artemisinin derivatives) is a crucial health problem in developing countries, particularly in Africa. The illegal production, sale and distribution of fake drugs is a huge market evaluated to several billion of dollars and represents more than 50% of the pharmaceutical market in several African countries. Fake drugs have led to a very great number of deaths from untreated malaria or fatality provoked by toxic ingredients. These fake medicines increase the risk of artemisinin resistance developed by the use of sub therapeutic dosages of antimalarials. Tackling this criminal traffic is the objective of an international  programme created by WHO  and involves the international police and custom organizations like INTERPOL. Several very important and encouraging results have been obtained, but the problem will be completely solved if genuine antimalarials, free-of-charge, are handed-over to populations in sub Sahara African countries.  

scholarly journals Treatment of Murine Cerebral Malaria by Artemisone in Combination with Conventional Antimalarial Drugs: Antiplasmodial Effects and Immune Responses

2014 ◽  
Vol 58 (8) ◽  
pp. 4745-4754 ◽  
Author(s):  
W. Armand Guiguemde ◽  
Nicholas H. Hunt ◽  
Jintao Guo ◽  
Annael Marciano ◽  
Richard K. Haynes ◽  
...  
Keyword(s):  
Cerebral Malaria ◽  
Antimalarial Activity ◽  
Interleukin 10 ◽  
Antimalarial Drugs ◽  
New Drugs ◽  
Artemisinin Derivative ◽  
Content Type ◽  
Artemisinin Derivatives ◽  
Dual Action

ABSTRACTThe decreasing effectiveness of antimalarial therapy due to drug resistance necessitates constant efforts to develop new drugs. Artemisinin derivatives are the most recent drugs that have been introduced and are considered the first line of treatment, but there are already indications ofPlasmodium falciparumresistance to artemisinins. Consequently, drug combinations are recommended for prevention of the induction of resistance. The research here demonstrates the effects of novel combinations of the new artemisinin derivative, artemisone, a recently described 10-alkylamino artemisinin derivative with improved antimalarial activity and reduced neurotoxicity. We here investigate its ability to killP. falciparumin a high-throughputin vitroassay and to protect mice against lethal cerebral malaria caused byPlasmodium bergheiANKA when used alone or in combination with established antimalarial drugs. Artemisone effects againstP. falciparumin vitrowere synergistic with halofantrine and mefloquine, and additive with 25 other drugs, including chloroquine and doxycycline. The concentrations of artemisone combinations that were toxic against THP-1 cellsin vitrowere much higher than their effective antimalarial concentration. Artemisone, mefloquine, chloroquine, or piperaquine given individually mostly protected mice against cerebral malaria caused byP. bergheiANKA but did not prevent parasite recrudescence. Combinations of artemisone with any of the other three drugs did completely cure most mice of malaria. The combination of artemisone and chloroquine decreased the ratio of proinflammatory (gamma interferon, tumor necrosis factor) to anti-inflammatory (interleukin 10 [IL-10], IL-4) cytokines in the plasma ofP. berghei-infected mice. Thus, artemisone in combinations with other antimalarial drugs might have a dual action, both killing parasites and limiting the potentially deleterious host inflammatory response.

scholarly journals The Ototoxicity of Antimalarial Drugs—A State of the Art Review

2021 ◽  
Vol 12 ◽  
Author(s):  
Magdalena Jozefowicz-Korczynska ◽  
Anna Pajor ◽  
Weronika Lucas Grzelczyk
Keyword(s):  
Hearing Loss ◽  
State Of The Art ◽  
Current Knowledge ◽  
Antimalarial Drugs ◽  
Clinical Applications ◽  
Monitoring Systems ◽  
Auditory Function ◽  
Artemisinin Derivatives ◽  
Antimalarial Agents ◽  
Vestibular Symptoms

This review summarizes current knowledge about the occurrence of hearing and balance disorders after antimalarial drugs treatment. It also examines the clinical applications of antimalarials, their mechanisms behind this ototoxicity and how it can be monitored. It includes studies with larger numbers of patients and those in which auditory function was assessed using audiological tests. Some antimalarials have been repurposed for other conditions like autoimmune disorders, rheumatic diseases, some viral diseases and cancers. While old antimalarial drugs, such as quinoline derivatives, are known to demonstrate ototoxicity, a number of new synthetic antimalarial agents particularly artemisinin derivatives, demonstrate unknown ototoxicity. Adverse audiovestibular effects vary depending on the medication itself, its dose and route of administration, as well as the drug combination, treated disease and individual predispositions of the patient. Dizziness was commonly reported, while vestibular symptoms, hearing loss and tinnitus were observed much less frequently, and most of these symptoms were reversible. As early identification of ototoxic hearing loss is critical to introducing possible alternative treatments with less ototoxic medications, therefore monitoring systems of those drugs ototoxic side effects are much needed.

From Mechanistic Studies on Artemisinin Derivatives to New Modular Antimalarial Drugs

2002 ◽  
Vol 35 (3) ◽  
pp. 167-174 ◽  
Author(s):  
Anne Robert ◽  
Odile Dechy-Cabaret ◽  
Jérôme Cazelles ◽  
Bernard Meunier
Keyword(s):  
Antimalarial Drugs ◽  
Mechanistic Studies ◽  
Artemisinin Derivatives

scholarly journals Susceptibility of Plasmodium falciparum isolates to antimalarial drugs in a highly seasonal malaria endemic village in Mali

2019 ◽  
Author(s):  
Karim Traoré ◽  
Seidina AS Diakité ◽  
Sekou Bah ◽  
Drissa S Konaté ◽  
Djeneba Dabitao ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Ex Vivo ◽  
Control Program ◽  
Antimalarial Drugs ◽  
Sensitivity Testing ◽  
Artemisinin Derivatives ◽  
Malaria Control Program ◽  
National Malaria Control Program ◽  
Antimalarial Resistance ◽  
Ic50 Values

Abstract Background: In 2006, the National Malaria Control Program (NMCP) in Mali recommended artemisinin-based combination therapy (ACT) as the first-line treatment for uncomplicated malaria. Since the introduction of ACT, few reports are available on the level of resistance of Plasmodium falciparum (P. falciparum) to antimalarial drugs in Mali. Dihydroartermisinin is the active metabolite of artemisinin derivatives. Here, we conducted an ex-vivo drug sensitivity testing in a rural area of southern Mali, namely the Kéniéroba village from 2016 to 2017. Methods: Seventy-five (75) isolates of P. falciparum were successfully evaluated for ex-vivo sensitivity to key anti-malarial drugs, namely chloroquine (CQ), quinine (QN), amodiaquine (AQ), mefloquine (MQ), lumefantrine (LUM), dihydroartermisinin (DHA) , and piperaquine (PPQ). P. falciparum sensitivity to these drugs was assessed using the World Wide Antimalarial Resistance Network (WWARN) SYBR-GREEN method of inhibitory concentration of 50% (IC50) determination. Reduced sensitivity to antimalarial drugs was defined as IC50 less than the WWARN standard IC50. Results: The proportion of resistant P. falciparum isolates was 20.2% for CQ, 40.5% for QN, 6.8% for AQ, and 1.3% for MQ. All tested P. falciparum isolates were sensitive to LUM, DHA, and PPQ. A statistically significant correlation was found between QN and AQ IC50 values (r = 0.80; r2 = 0.64, P<0.0001). Conclusions: P. falciparum isolates were sensitive to all ACT derivates tested in Kenieroba in Mali. In contrast, P. falciparum isolates were resistant to, CQ, QN, and AQ as evidenced by high IC50 to these drugs.

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