Antimalarial activities of new guanidylimidazole and guanidylimidazoline derivatives

…, B Pybus, MT O'Neil, MP Kozar, AJ Lin

Index: Zhang, Liang; Sathunuru, Ramadas; Caridha, Diana; Pybus, Brandon; O'Neil, Michael T.; Kozar, Michael P.; Lin, Ai J. Journal of Medicinal Chemistry, 2011 , vol. 54, # 19 p. 6634 - 6646

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Citation Number: 4

Abstract

A series of new guanidylimidazole derivatives was prepared and evaluated in mice and Rhesus monkeys infected with malarial sporozoites. The majority of the new compounds showed poor metabolic stability and weak in vitro activities in three clones of Plasmodium falciparum. Compounds 8a, 8h, 9a, 16a, and 16e cured the mice infected with sporozoites of P. berghei at 160 and 320 mg/kg/day× 3 po. Compounds 8a showed better causal ...