Perspective in Antimalarial Chemotherapy

Abstract

Antimalarial chemotherapy has become more complex and challenging because of multidrug resistant strains of Plasmodium falciparum. Due to resistance of malarial parasite against well known drugs, the chemotherapy of malaria has become complicated. In this review we have discussed brief introduction followed by life cycle of malaria parasite. The list of commercially available antimalarial drugs along with there action on different stages of parasite have been discussed. A brief description of their mechanism of action and advantages and disadvantages were reported. The natural products as antimalarial have been discussed in the review. On the basis of chemical classes the natural products were divided in the following categories; Quinoline alkaloids, Iso-quinoline alkaloids, Indoloquinoline alkaloids, Carbolines, Bis-isoquinoline, 4-Quinazole derivatives, Trioxanes, Terpenes, Naphthoquinone, Anthraquinones, Chalcones, Hydroxy flavanones, Coumarins and phenolic glycoside. The combination chemotherapy has been highlighted in the review. The Biochemical and Immunological changes in malarial infection are discussed along with complications of malarial chemotherapy due to resistance. In the conclusion section, the future strategies for the chemotherapy of malaria have been discussed.

Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores

“…Quinoline containing compounds, such as the potent and inexpensive chloroquine (CQ) [2,3,4] have a long tradition in the treatment of malaria, and systematic modification has led to a variety of antimalarial drugs with diverse substitutions around the quinoline ring [5,6]. However, the spread of chloroquine-resistant Plasmodium falciparum strains has dashed hopes of global malaria eradication and has complicated the clinical management of malaria in endemic areas.…”

Malaria Chemotherapeutics Part I: History of Antimalarial Drug Development, Currently Used Therapeutics, and Drugs in Clinical Development

“…P. ovale is mainly confined to tropical West Africa, while the occurrence of P. malariae is worldwide, although its distribution is patchy. [1,2] "If as standard of importance is taken the greatest harm to the greatest number", [3] malaria is the most important infectious disease. It has been estimated that there were up to 660 million clinical cases of P. falciparum malaria in 2002.…”

“…These gametocytes undergo sexual reproduction within the mosquito mid-gut producing thousands of infective sporozoites, which migrate to the salivary gland where they are ready for a new infection (Figure 2). [1,2] With the rupture of the erythrocyte, the parasite's waste and cell debris is released into the blood stream, causing some of the clinical symptoms of malaria. The main symptom is fever, but rarely in the classical tertian (every 48 h) or quartan (every 72 h) patterns.…”

“…In cases of P. vivax and P. ovale, a combination of blood schizonticides and tissue schizonticides is required. [2] 2. 4-Aminoquinolines and Arylamino alcohols…”

Antimalarial Drugs – What is in Use and What is in the Pipeline

“…These gametocytes undergo sexual reproduction within the mosquito midgut producing thousands of infective sporozoites, which migrate to the salivary gland ready for a new infection cycle ( Fig. 1) [1,4].…”