Abstract

Publisher Summary This chapter discusses studies that focus on antiparasitic agents. A model in vitro system for testing susceptibility of human parasites to antimalarial drugs was proposed. Structure–activity correlations for 2-phenylquinoline-4-carbinol antimalarials were obtained by the Free-Wilson method. An extensive study of tissue distribution and urine excretion of chloroquine was reported. Observations on the mode of action of chloroquine and quinine in blood stages of P. berghei were reported. Development of resistance and cross-resistance to antifolic antimalarials was studied in a variety of bacteria. The antimalarial primaquin caused a total inhibition of protein synthesis in B. megaterium. Parallelism in reversible coenzyme Q 10 -inhibition and antimalarial properties was demonstrated in substituted quinolinequinones and napthoquinones. Extensive structure–activity relationships in phenanthrene-9-amino alcohols and in 2,6-diaryl pyridyl-4-methanols were reported. Parallelism in reversible coenzyme Q 10 -inhibition and antimalarial properties was demonstrated in substituted quinol inequinones and napthoquinones. Chlorinated lincomycin analogs were evaluated against chloroquine resistant falciparium malaria. The antibiotic clindamycin phosphate, a lincomycin analog, showed antimalarial activity. Vermicillin, a novel antibiotic from Penicillium vermiculatum , was also found active against Tryp. cruzi and Leishm. brasiliensis .

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