An efficient synthesis for a new class antimalarial agent, 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole

Efficient synthesis is essential for antimalarial therapeutics. A four-step route has been established for the synthesis of 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole 1 that is a potent new class boron-containing antimalarial agent in preclinical development with IC50=26nM against th...

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Bibliographic Details
Published inTetrahedron letters Vol. 52; no. 30; pp. 3909 - 3911
Main Authors Zhang, Yong-Kang, Plattner, Jacob J., Easom, Eric E., Waterson, David, Ge, Min, Li, Zhiya, Li, Lingchao, Jian, Yong
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 27.07.2011
Elsevier
Subjects
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarial therapeutics
Antiparasitic agents
Benzoxaborole
Biological and medical sciences
Chemistry
Chemistry, Organic
Exact sciences and technology
Heterocyclic compounds
Malaria
Medical sciences
Miscellaneous
Organic chemistry
Parasites
Pharmacology. Drug treatments
Physical Sciences
Plasmodium falciparum
Preparations and properties
Science & Technology
Synthesis
Synthesis (chemistry)
Tetrahedrons
Benzoxaborole
Plasmodium falciparum
Antimalarial therapeutics
Synthesis
Malaria
Protozoa
Antimalarial
Apicomplexa
Organic boron compounds
Oxygen boron heterocycle
Chemical synthesis
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Summary:Efficient synthesis is essential for antimalarial therapeutics. A four-step route has been established for the synthesis of 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole 1 that is a potent new class boron-containing antimalarial agent in preclinical development with IC50=26nM against the malaria parasite Plasmodium falciparum.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2011.05.088