[2025371-99-5]    

Synonyms : (3-Hydroxy-3-methylazetidin-1-yl)(5-((1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)pyrazin-2-yl)methanone

Applications : AN-13762 is a novel benzoxaborole antimalarial agent. AN-13762 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mice, rats, and dogs. It was highly active against the other 11 P. falciparum strains, which are mostly resistant to chloroquine and pyrimethamine. It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg. The combined properties of this novel benzoxaborole support its progression to preclinical development.

References : Yong-Kang Zhang et al.: J. Med. Chem., 60(13), 5889-5908, 2017.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.