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

文献类型： 外文期刊

作者： Poonam 1 ; Gupta, Yash 2 ; Gupta, Nikesh 3 ; Singh, Snigdha 4 ; Wu, Lidong 5 ; Chhikara, Bhupender Singh 7 ; Rawat, Ma 1 ;

作者机构： 1.Univ Delhi, Dept Chem, Miranda House, Delhi, India

2.Natl Inst Malaria Res ICMR, New Delhi, India

3.Jawaharlal Nehru Univ, Special Ctr Nanosci, New Delhi, India

4.Univ Delhi, Hansraj Coll Univ Enclave, Dept Chem, Lab Translat Chem & Drug Discovery, Delhi 110007, India

5.MIT, Dept Chem, Cambridge, MA 02139 USA

6.Chinese Acad Fishery Sci, Minist Agr, Key Lab Control Qual & Safety Aquat Prod, Beijing, Peoples R China

7.Univ Delhi, Dept Chem, Aditi Mahavidyalaya, Delhi, India

8.Univ New Mexico, Dept Internal Med, Albuquerque, NM 87131 USA

关键词： antimalarials; malaria eradication; multistage activity

期刊名称：MEDICINAL RESEARCH REVIEWS （ 影响因子：12.944； 五年影响因子：12.341 ）

ISSN： 0198-6325

年卷期： 2018 年 38 卷 5 期

页码：

收录情况： SCI

摘要： 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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