Antimalarial activity of 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) and its carboxylic acid derivatives

作者：Sato Akira; Kawai Satoru; Hiramoto Akiko; Morita Masayuki; Tanigawa Natsuki; Nakase Yukari; Komichi Yuka; Matsumoto Masahiro; Hiraoka Osamu; Hiramoto Kazuyuki; Tokuhara Hidekazu; Masuyama Araki; Nojima Masatomo; Higaki Kazutaka; Hayatsu Hikoya; Wataya Yusuke; Kim Hye Sook^*

来源：Parasitology International, 2011, 60(4): 488-492.

DOI：10.1016/j.parint.2011.08.017

• 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl) hexan-1-ol
• N-251
• Antimalarial activity
• Carbon radical
• Plasmodium falciparum
• Plasmodium berghei

Malaria is one of the world's deadliest diseases and is becoming an increasingly serious problem as malaria parasites develop resistance to most of the antimalarial drugs used today. We previously reported the in vitro and in vivo antimalarial potencies of 1,2,6,7-tetraoxaspiro[7.11]nonadecane (N-89) and 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-l-ol (N-251) against Plasmodium falciparum and Plasmodium berghei parasites. To improve water-solubility for synthetic peroxides, a variety of cyclic peroxides having carboxyl functionality was prepared based on the antimalarial candidate, N-251, and their antimalarial activities were determined. The reactions of N-89 and its derivatives with Fe(II) demonstrated a highly efficient formation of the corresponding carbon radical which may be suspected as a key for the antiparasitic activity. Published by Elsevier Ireland Ltd.

• 出版日期2011-12