- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: AN13762 is a preclinical antimalarial candidate optimized from the benzoxaboroles, a novel class of boron-containing compound .
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Sonoiki E, Ng CL, Lee MC, Guo D, Zhang YK, Zhou Y, Alley MR, Ahyong V, Sanz LM, Lafuente-Monasterio MJ et al.. (2017)
A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue.
Nat Commun, 8: 14574. [PMID:28262680]
2. Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Freund YR, Berry P, Ciaravino V, Erve JCL, Rosenthal PJ et al.. (2017)
Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate.
J Med Chem, 60 (13): 5889-5908. [PMID:28635296]
3. Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Gut J, Rosenthal PJ, Waterson D, Gamo FJ, Angulo-Barturen I et al.. (2011)
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents.
Bioorg Med Chem Lett, 21 (2): 644-51. [PMID:21195617]
4. Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Ye L, Zhou H, Waterson D, Gamo FJ, Sanz LM et al.. (2012)
Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.
Bioorg Med Chem Lett, 22 (3): 1299-307. [PMID:22243961]