An Overview of Currently Available Antimalarials

Gorobets, Nikolay Yu.; Sedash, Yuriy V.; Singh, Brajendra K.; Poonam, .; Rathi, Brijesh

doi:10.2174/1568026617666170130123520

Cited by 19 publications

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“…Additionally, in the same year, ∼212 million cases of malaria were noted worldwide, particularly in African regions. Advanced prevention and treatment techniques and malaria eradication initiatives, including insecticide‐treated bed nets, insecticide sprays, and artemisinin‐based combination therapies (ACTs), have collectively decreased the lethality of malaria (∼4% per year), with a 40% decrease in the number of clinical malaria cases between 2000 and 2015 . However, certain factors, including increased resistance of the parasite to drugs, extended period of infection in the human host, high cost of drugs and lack of new potent drugs, are still obstacles to controlling the disease .…”

Section: Introductionmentioning

confidence: 99%

“…Since the 1990s, the global market has been waiting for new drug molecules with novel modes of action. In the early 2000s, a new efficient drug, arterolane, was presented as an effective treatment in the form of a fixed‐dose combination with piperaquine and was marketed in India and several African countries . However, this combination therapy still requires approval from the World Health Organization (WHO) for general usage.…”

Section: Introductionmentioning

confidence: 99%

“…Advanced prevention and treatment techniques and malaria eradication initiatives, including insecticide-treated bed nets, insecticide sprays, and artemisinin-based combination therapies (ACTs), have collectively decreased the lethality of malaria (∼4% per year), with a 40% decrease in the number of clinical malaria cases between 2000 and 2015. [3][4][5][6] However, certain factors, including increased resistance of the parasite to drugs, extended period of infection in the human host, 7 high cost of drugs and lack of new potent drugs, are still obstacles to controlling the disease. 8 The frontline treatments for P. falciparum infection are based on artemisinin (ART) in combination with effective companion drugs such as mefloquine, lumefantrine, and piperaquine.…”

Section: Introductionmentioning

confidence: 99%

“…In the early 2000s, a new efficient drug, arterolane, was presented as an effective treatment in the form of a fixed-dose combination with piperaquine and was marketed in India and several African countries. 6 However, this combination therapy still requires approval from the World Health Organization (WHO) for general usage. In addition, the currently available vaccine does not provide absolute protection from the disease.…”

Section: Introductionmentioning

confidence: 99%

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Multistage inhibitors of the malaria parasite: Emerging hope for chemoprotection and malaria eradication

Poonam

Gupta

et al. 2018

Medicinal Research Reviews

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Over time, several exciting advances have been made in the treatment and prevention of malaria; however, this devastating disease continues to be a major global health problem and affects millions of people every year. Notably, the paucity of new efficient drug molecules and the inevitable drug resistance of the malaria parasite, Plasmodium falciparum, against frontline therapeutics are the foremost struggles facing malaria eradication initiatives. According to the malaria eradication agenda, the discovery of new chemical entities that can destroy the parasite at the liver stage, the asexual blood stage, the gametocyte stage, and the insect ookinete stage of the parasite life cycle (i.e., compounds exhibiting multistage activity) are in high demand, preferably with novel and multiple modes of action. Phenotypic screening of chemical libraries against the malaria parasite is certainly a crucial step toward overcoming these crises. In the last few years, various research groups, including industrial research laboratories, have performed large-scale phenotypic screenings that have identified a wealth of chemical entities active against multiple life stages of the malaria parasite. Vital scientific and technological developments have led to the discovery of multistage inhibitors of the malaria parasite; these compounds, considered highly valuable starting points for subsequent drug discovery and eradication of malaria, are reviewed.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Multistage inhibitors of the malaria parasite: Emerging hope for chemoprotection and malaria eradication

Poonam

Gupta

et al. 2018

Medicinal Research Reviews

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“…According to World Health Organization (WHO), about 216 million cases and 445,000 deaths from malaria were reported in 2016 ( WHO, 2018c ). Furthermore, the resistance to antimalarial drugs is a common and growing issue and constitutes a substantial threat for populations in endemic regions ( Gorobets et al, 2017 ; Menard and Dondorp, 2017 ). In a study reported by Zhang et al (2013) , a data set of 3,133 compounds reported as active or inactive against P. falciparum chloroquine susceptible strain (3D7) was used to develop QSAR models.…”

Section: Practical Applications Of Qsar-based Virtual Screeningmentioning

confidence: 99%

QSAR-Based Virtual Screening: Advances and Applications in Drug Discovery

et al. 2018

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Virtual screening (VS) has emerged in drug discovery as a powerful computational approach to screen large libraries of small molecules for new hits with desired properties that can then be tested experimentally. Similar to other computational approaches, VS intention is not to replace in vitro or in vivo assays, but to speed up the discovery process, to reduce the number of candidates to be tested experimentally, and to rationalize their choice. Moreover, VS has become very popular in pharmaceutical companies and academic organizations due to its time-, cost-, resources-, and labor-saving. Among the VS approaches, quantitative structure–activity relationship (QSAR) analysis is the most powerful method due to its high and fast throughput and good hit rate. As the first preliminary step of a QSAR model development, relevant chemogenomics data are collected from databases and the literature. Then, chemical descriptors are calculated on different levels of representation of molecular structure, ranging from 1D to nD, and then correlated with the biological property using machine learning techniques. Once developed and validated, QSAR models are applied to predict the biological property of novel compounds. Although the experimental testing of computational hits is not an inherent part of QSAR methodology, it is highly desired and should be performed as an ultimate validation of developed models. In this mini-review, we summarize and critically analyze the recent trends of QSAR-based VS in drug discovery and demonstrate successful applications in identifying perspective compounds with desired properties. Moreover, we provide some recommendations about the best practices for QSAR-based VS along with the future perspectives of this approach.

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Plants as Sources of Natural and Recombinant Antimalaria Agents

et al. 2022

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Malaria is one of the severe infectious diseases that has victimized about half a civilization billion people each year worldwide. The application of long-lasting insecticides is the main strategy to control malaria; however, a surge in antimalarial drug development is also taking a leading role to break off the infections. Although, recurring drug resistance can compromise the efficiency of both conventional and novel antimalarial medicines. The eradication of malaria is significantly contingent on discovering novel potent agents that are low cost and easy to administer. In this context, plant metabolites inhibit malaria infection progression and might potentially be utilized as an alternative treatment for malaria, such as artemisinin. Advances in genetic engineering technology, especially the advent of molecular farming, have made plants more versatile in producing protein drugs (PDs) to treat infectious diseases, including malaria. These recent developments in genetic modifications have enabled the production of native pharmaceutically active compounds and the accumulation of diverse heterologous proteins such as human antibodies, booster vaccines, and many PDs to treat infectious diseases and genetic disorders. This review will discuss the pivotal role of a plant-based production system that expresses natural antimalarial agents or host protein drugs to cure malaria infections. The potential of these natural and induced compounds will support modern healthcare systems in treating malaria infections, especially in developing countries to mitigate human fatalities.

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An Overview of Currently Available Antimalarials

Abstract: Despite the seemingly large number of the drugs currently available for malaria treatment, this arsenal is limited due to the narrow variation of their mechanism of action.

Cited by 19 publications

References 0 publications

Multistage inhibitors of the malaria parasite: Emerging hope for chemoprotection and malaria eradication

Multistage inhibitors of the malaria parasite: Emerging hope for chemoprotection and malaria eradication

QSAR-Based Virtual Screening: Advances and Applications in Drug Discovery

Plants as Sources of Natural and Recombinant Antimalaria Agents

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