Antimalaria drugs

Nursing alcohol lamps and charcoal fires in his tiny home laboratory during the Easter vacation of 1856, a teenager slowly teased out the constituents of a black and tarry goo. Working nights, weekends, and holidays on chemistry, he was searching for a test-tube substitute for quinine, the antimalaria drug derived from plants. The black precipitate he had made was obviously not quinine, but the youth was well trained in chemistry, so he did not throw it out. Instead, he treated it with alcohol, and a fabulously intense purple appeared. Then he tested the purple on a piece of silk. 

At the time, little was known about the internal structure of compounds or about how one compound was transformed into another. Chemists concentrated instead on the proportions of various chemicals in a substance. Hofmann realized that the proportions of ingredients in the antimalaria drug quinine— 20 equivalents of carbon, 11 equivalents of hydrogen, 1 equivalent of nitrogen, and 2 equivalents of oxygen —were almost identical to those in aniline. The difference was only two equivalents of water. Hofmann speculated that he might be able to turn aniline into quinine. With European colonization headed toward the tropics, the drug was desperately needed. 

With good reason, Allied military leaders regarded malaria as a dangerous enemy. Quinine was unavailable because the Japanese controlled production areas, and other antimalaria drugs had to be developed. The disease was still endemic to parts of the United States, northern and southern Europe, the Mediterranean, and a broad swath of the Earth from Africa through the Pacific islands. It was—and remains today—the world s most widespread contagious disease. 

Warfarin Antimalaria drugs 8 oz of freshly prepared GFJ from concentrate t.i.d. for 1 wk N/A Prothrombin time <->, international normalized ratio (120)... 

JM Wooden, LH Hartwell, B Vasquez, CH Sibley. Analysis in yeast of antimalaria drugs that target the dihydrofolate reductase of Plasmodium falciparum. Mol Biochem Parasitol 85 25 10, 1997. 

Overall, hair analysis provides convincing evidence of past exposure to a drug. Viala et al. identified by GC/MS chloroquine and its major metabolite in hair samples of patients who received the antimalaria drug for several months. 

Kumar, N. and Zheng, H. (1990) Stage-specific gametocytocidal effect in vitro of the antimalaria drug qinghaosu on Plasmodium falciparum. Parasitol. Res., 76, 214-218. 

QUINIDINE Quinidine is one of the quinoline alkaloids in Cinchona bark. (See POl, Antimalaria-drugs). Thus, quinidine is an antiarrythmic drug, whereas its stereoisomer, quinine, is an antimalarial. In antiarryth-mically effective doses quinidine reduces the contraction capacity of the heart. The minute volume of the heart diminishes through its negative inotropic effect. Quinidine is used clinically for treatment of relapse into auricle fibrillation, and at extrasystohcs and paroxysmal tachycardia and ventricular tachycardia. 

Madinaveitia, J. Antagonism of some antimalaria] drugs by riboflavin. 

Croft AM, Herxheimer A. Hypoftiesis Adverse effects of the antimalaria drug, mefloquine due to primary liver damage with secondary thyroid involvement BMCPubUcHealth (2002)... 

The important antimalaria drug rac-eryt/zro-mefloquine HCl, 2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol, has been widely applied under the name Lariam in spite of the fact that its (—) enantiomer is believed to cause adverse side elfects in malaria treatment resulting from binding to the adenosine receptor in the human brain. The absolute configuration of this enantiomer has been established by Schmidt et al by the use of a combination of /hh couplings, chemical shifts, rotational Overhauser elfects, and residual dipolar couplings. 

During World War II, the United States accelerated a wartime program to investigate antimalaria drugs, thereby providing a boost to pharmacology research. 

A variety of microorganisms produce hydrocarbons or their precursors. For example, bacteria, primarily Bacillus, produce isoprene (Kuzma et al. 1995). Iso-prenoid compounds are common in nature, mostly in plants, and find application in human life in the production of pharmaceuticals, flavours, fragrances and pigments (Walsh 2007). Due to interest in these applications, strains of E. coli and S. cerevisiae have been established for the overproduction of certain isoprenoids. One instance is artemisinic acid, a precursor to artemisinin and an antimalaria drug... 

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