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Antimalarial drugs

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Antimalarials are able to kill or inhibit the malaria parasite and the process of plasmodium propagation, being drugs for the prevention and treatment of malaria. On as early as the 1st, 2nd century (AD), there had been already records about the antimalarial effect of antifebrile dichroa in "Shen Nong's Herbal Classic."

The earliest applied natural antimalarial drug, quinine, was the antimalarial component in the cinchona bark used by Indian for the treatment of fever. In 1907, Rabe had clarified its chemical structure. Subsequently, people had been actively engaged in the research of synthesizing antimalarial drugs. In 1926, Schulemann had for the first time synthesized the artificial antimalarial-plasmochin, also known as pamaquine. Atebrine and chloroquine have also successively come out. In 1944, Woodward had successfully performed de novo synthesis of quinine and confirmed its structure. During the World War II, people had successfully synthesized primaquine and pentaquine to replace the pamaquine; starting from the antagonism of biochemical metabolism, people had successfully synthesized proguanil and pyrimethamine.

In early 1960, the emergence of the resistance of plasmodium to chloroquine had set off a new climax to identify the novel antimalarial drugs. Because of the foreign-depth study of the structure-activity relationship of quinine, people had developed novel antimalarial drugs, quinoline-methanols with the representative being the meqloquine. Starting from the study of the structure-activity relationship of the 4-amino-quinoline drugs, people had synthesized amodiaquine-type or hydroxypiperaquine-type drugs such as bis-pyroquilon (M6407), pyracrine and pyronaridine which have bilateral side chain of pyrrolidine and methyl aminophenol. They not only have lower cardiac toxicity than chloroquine and also have varying degrees of anti-arrhythmia effects.

Chinese scientists have discovered Radix dichroa), Hydrangea umbellate and Brucea javanicaL.Merr from Chinese herbs. Through analysis, people have clarified the chemical structure of the Febrifugine. At early 1970s, people have further isolated artemisinin from Artemisia annua. Animal experiments and clinical observations had confirmed that its antimalarial effects are more excellent than chloroquine and it can be used to rescue dangerous type of malaria. The analysis results of chemical structure have demonstrated that it is a kind of sesquiterpene containing the peroxide bridge, being a totally new type in the anti-malarial drugs. People have realized the de novo total synthesis of this kind of peroxide bridges sesquiterpene lactones in 1982. Chinese scholars have also found another kind of sesquiterpene containing the peroxide bridge, yingzhaosu A, from the Artabotrys hexapetalus. Artemisinin and its derivatives also have significant anti-schistosome effect.

In addition, the antibiotic clindamycin and tetracyclines also have antimalarial effect. However, due to the slow effect, they are generally not used alone. There are also clindamycin which can be used in combination with quinine to treat falciparum malaria and so on.

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Structure:
Chemical Name:
Cinchonine
CAS:
118-10-5
MF:
C19H22N2O
Structure:
Chemical Name:
Artemisinin
CAS:
63968-64-9
MF:
C15H22O5
Structure:
Chemical Name:
Artemether
CAS:
71963-77-4
MF:
C16H26O5
Structure:
Chemical Name:
Lumefantrine
CAS:
82186-77-4
MF:
C30H32Cl3NO
Structure:
Chemical Name:
8-Hydroxyquinoline
CAS:
148-24-3
MF:
C9H7NO
Structure:
Chemical Name:
Quinine
CAS:
130-95-0
MF:
C20H24N2O2
Structure:
Chemical Name:
Pyrimethamine
CAS:
58-14-0
MF:
C12H13ClN4
Structure:
Chemical Name:
Hydroxychloroquine sulfate
CAS:
747-36-4
MF:
C18H28ClN3O5S
Structure:
Chemical Name:
DHQHS 2
CAS:
71939-50-9
MF:
C15H24O5
Structure:
Chemical Name:
Artesunate
CAS:
88495-63-0
MF:
C19H28O8
Structure:
Chemical Name:
Quinine sulfate dihydrate
CAS:
6119-70-6
MF:
C20H26N2O6S
Structure:
Chemical Name:
HYDROQUININE (ANTHRAQUINONE-1 4-DIYL)
CAS:
176097-24-8
MF:
C54H56N4O6
Chemical Name:
artesunate
CAS:
83507-69-1
Structure:
Chemical Name:
4-[2-[(1S,2R,4aS,7S,8aR)-4a-[(Acetyloxy)methyl]-1,2,3,4,4a,7,8,8a-octahydro-7-hydroxy-5-(hydroxymethyl)-1,2-dimethyl-1-naphthalenyl]ethyl]-2(5H)-furanone
CAS:
125675-09-4
MF:
C22H32O6
Structure:
Chemical Name:
Tesmilifene
CAS:
98774-23-3
MF:
C19H25NO
Structure:
Chemical Name:
QUINACRINE DIHYDROCHLORIDE
CAS:
69-05-6
MF:
C23H32Cl3N3O
Structure:
Chemical Name:
Chloroquine diphosphate
CAS:
50-63-5
MF:
C18H32ClN3O8P2
Structure:
Chemical Name:
CINCHONINE HYDROCHLORIDE
CAS:
5949-11-1
MF:
C19H23ClN2O
Structure:
Chemical Name:
4,4'-(1,3-Propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline) phosphate
CAS:
85547-56-4
MF:
C29H32Cl2N6.H3PO4
Structure:
Chemical Name:
MEFLOQUINE
CAS:
53230-10-7
MF:
C17H16F6N2O
Structure:
Chemical Name:
Hsdb 7458
CAS:
91487-94-4
MF:
C19H28O8
Structure:
Chemical Name:
Primaquine
CAS:
90-34-6
MF:
C15H21N3O
Chemical Name:
Naphthoquine Phosphate
Structure:
Chemical Name:
Primaquine diphosphate
CAS:
63-45-6
MF:
C15H27N3O9P2
Structure:
Chemical Name:
3-Aminocarbonyl-1-Boc-pyrrolidine
CAS:
122684-34-8
MF:
C10H18N2O3
Structure:
Chemical Name:
Quinine hydrochloride
CAS:
130-89-2
MF:
C20H25ClN2O2
Structure:
Chemical Name:
NAPHTHOQUINE PHOSPHATE
CAS:
173531-58-3
MF:
C24H31ClN3O5P
Structure:
Chemical Name:
Mepacrine hydrochloride
CAS:
6151-30-0
MF:
C23H36Cl3N3O3
Structure:
Chemical Name:
Malaridine
CAS:
121836-29-1
MF:
C16H23N3O3
Structure:
Chemical Name:
alpha-Dihydroartemisinin
CAS:
81496-81-3
MF:
C15H24O5
Structure:
Chemical Name:
Dihydroartemisinin
CAS:
81496-82-4
MF:
C15H24O5
Structure:
Chemical Name:
Chlorguanide Hydrochloride
CAS:
637-32-1
MF:
C11H17Cl2N5
Structure:
Chemical Name:
HALOFANTRINE
CAS:
69756-53-2
MF:
C26H30Cl2F3NO
Structure:
Chemical Name:
2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol
CAS:
118-42-3
MF:
C18H26ClN3O
Structure:
Chemical Name:
pamaquine
CAS:
635-05-2
MF:
C42H45N3O7
Structure:
Chemical Name:
Piperaquine
CAS:
83764-65-2
MF:
C29H32Cl2N6
Structure:
Chemical Name:
CHLOROQUINE
CAS:
54-05-7
MF:
C18H26ClN3
Structure:
Chemical Name:
N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
CAS:
500-92-5
MF:
C11H16ClN5
Structure:
Chemical Name:
CINCHONINE MONOHYDROCHLORIDE HYDRATE 9&
CAS:
312695-48-0
MF:
C19H27ClN2O3
Structure:
Chemical Name:
Halofantrine hydrochloride
CAS:
36167-63-2
MF:
C26H30Cl2F3NO.ClH
Chemical Name:
Lumefrantrine
Structure:
Chemical Name:
Amodiaquine
CAS:
86-42-0
MF:
C20H22ClN3O
Structure:
Chemical Name:
Quinine dihydrochloride
CAS:
60-93-5
MF:
C20H26Cl2N2O2
Structure:
Chemical Name:
Piperaquinoline
CAS:
4085-31-8
MF:
C29H32Cl2N6