&lt;p&gt;Antimalarial Drug Resistance and Novel Targets for Antimalarial Drug Discovery&lt;/p&gt;

Shibeshi, Melkamu Adigo; Kifle, Zemene Demelash; Atnafie, Seyfe Asrade

doi:10.2147/idr.s279433

Cited by 118 publications

(83 citation statements)

References 116 publications

(130 reference statements)

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“…Furthermore, mutations in PfKelch13 have been identified which confer partial resistance to artemisinin, first-line treatment for P. falciparum infections [ 4 ]. Resistance to other drugs (antifolates, naphthoquinones, antibiotics like clindamycin and doxycycline and 4-aminoquinolines) has also emerged in malarial parasites and few novel targets have recently been identified for the development of new antimalarial drugs [ 13 ].…”

Section: Global Epidemiology Of Malariamentioning

confidence: 99%

Current Status and the Epidemiology of Malaria in the Middle East Region and Beyond

2021

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Vector-borne parasitic infectious diseases are important causes of morbidity and mortality globally. Malaria is one of the most common vector-borne parasitic infection and is caused by five Plasmodium species, namely P. falciparum, P. vivax, P. ovale, P. malariae, and P. knowlesi. Epidemiologically, differences in the patterns of malaria cases, causative agent, disease severity, antimicrobial resistance, and mortality exist across diverse geographical regions. The world witnessed 229 million malaria cases which resulted in 409,000 deaths in 2019 alone. Although malaria cases are reported from 87 countries globally, Africa bears the brunt of these infections and deaths as nearly 94% of total malaria cases and deaths occur in this continent, particularly in sub-Saharan Africa. Most of the Middle East Region countries are malaria-free as no indigenous cases of infection have been described in recent years. However, imported cases of malaria continue to occur as some of these countries. Indeed, the six Gulf Cooperation Council (GCC) countries have large expatriate population originating from malaria endemic countries. In this review, the current status and epidemiology of malaria in the Middle East Region countries and other malaria-endemic countries that are home to a large migrant workforce being employed in Middle East Region countries are discussed.

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Section: Global Epidemiology Of Malariamentioning

confidence: 99%

Current Status and the Epidemiology of Malaria in the Middle East Region and Beyond

2021

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“…In Ethiopia, chloroquine treatment failure against falciparum and vivax malaria was reported for the fist time from Debre Zeit in 1995. Then after, chloroquine resistance has abeen detected in Ethiopia [25,62]. However, drug resistance to chloroquine can be reversed by certain agents, including verapamil, desipramine, and chlorpheniramine, but the clinical value of resistance-reversing drugs is not established [59].…”

Section: Conventional Medicinesmentioning

confidence: 99%

“…Chills, high fever, malaise, headache, muscle aches and sweating are the most frequently reported symptoms of malaria infection. The current diagnostic methods used for identification of Plasmodium species from blood samples are light/ fluorescence microscopy (gold standard method), immuno-chromatographic lateral flow assays (RDTs-rapid diagnostic tests), serology tests, and nucleic acid amplification techniques including PCR (polymerase chain reaction) and isothermal amplification [25]. Rolling circle enhanced enzyme activity detection (REEAD) and micromagnetic resonance reflaxometric (MMR) tests are recently developed parasitological methods appropraite for utilization in field detection of malaria infected individuals for population screenings [26].…”

Section: Introductionmentioning

confidence: 99%

“…About 30,485,416 Ethiopians are living at high risk places for malaria infection. In 2019, 213 deaths and 904,496 confirmed cases due to malaria were reported by Ethiopian Federal Ministry of Health (FMoH) [25,28]. Despite decreased malaria occurrence rate and death rate in Ethiopia since 2010 [28], high prevalence was observed in some areas in contrast to high household coverage of control interventions [36,37].…”

Section: Introductionmentioning

confidence: 99%

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Malaria: Introductory Concepts, Resistance Issues and Current Medicines

Nureye¹

2021

Plasmodium Species and Drug Resistance

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Malaria continues to be the main community health problem in numerous nations. Six species of Plasmodium are documented as the cause of human malaria infection. Among others, Plasmodium falciparum and Plasmodium vivax parasites produce an immense challenge in the public health. Anopheles funestus and Anopheles gambiae are the major transimmiter of the disease (malaria) from one person to another. The disease parasite has a complicated cycle of life that occurs in human and mosquitoes. In general, malaria diagnosis is divided into parasitological and clinical diagnosis. Internationally, the death rate of malaria becomes reduced although few records from Ethiopia describe the presence of raised prevalence of malaria in certain areas. Apart from reduction in incidence and prevalence, transmission of malaria is continued throughout the globe. Hence, its control needs a combined approach comprising treatment with effective antimalarial agents. A lot of novel compounds are under pre-clinical and clinical studies that are triggered by the occurrence of resistance among commonly used antimalarial drugs. In addition to the already known new compounds and targets for drug discovery, scientists from all corner of the world are in search of novel targets and chemical entities.

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“…Increasing resistance to all classes of antimalarial agents, including artemisinin derivatives, poses a threat to endemic regions. A reason for the emerging resistance is the improper use of antimalarial drugs, which exerts selection pressure on the parasites [ 4 , 7 , 8 , 9 , 10 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antiplasmodial Activity of Bisindolylcyclobutenediones

Lande

Nasereddin²,

Alder

et al. 2021

Molecules

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Malaria is one of the most dangerous infectious diseases. Because the causative Plasmodium parasites have developed resistances against virtually all established antimalarial drugs, novel antiplasmodial agents are required. In order to target plasmodial kinases, novel N-unsubstituted bisindolylcyclobutenediones were designed as analogs to the kinase inhibitory bisindolylmaleimides. Molecular docking experiments produced favorable poses of the unsubstituted bisindolylcyclobutenedione in the ATP binding pocket of various plasmodial protein kinases. The synthesis of the title compounds was accomplished by sequential Friedel-Crafts acylation procedures. In vitro screening of the new compounds against transgenic NF54-luc P. falciparum parasites revealed a set of derivatives with submicromolar activity, of which some displayed a reasonable selectivity profile against a human cell line. Although the molecular docking studies suggested the plasmodial protein kinase PfGSK-3 as the putative biological target, the title compounds failed to inhibit the isolated enzyme in vitro. As selective submicromolar antiplasmodial agents, the N-unsubstituted bisindolylcyclobutenediones are promising starting structures in the search for antimalarial drugs, albeit for a rational development, the biological target addressed by these compounds has yet to be identified.

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<p>Antimalarial Drug Resistance and Novel Targets for Antimalarial Drug Discovery</p>

Cited by 118 publications

References 116 publications

Current Status and the Epidemiology of Malaria in the Middle East Region and Beyond

Current Status and the Epidemiology of Malaria in the Middle East Region and Beyond

Malaria: Introductory Concepts, Resistance Issues and Current Medicines

Synthesis and Antiplasmodial Activity of Bisindolylcyclobutenediones

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