Akama T Zhang YK Freund YR Berry P Lee J Easom EE Jacobs RT Plattner JJ Witty MJ Peter R Rowan TG Gillingwater K Brun R Nare B Mercer L Xu M Wang J Liang H 2018 Novel l-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T. vivax) parasites. The study identified 4-fluorobenzyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborole-6-carbonyl)-l-valinate (5, AN11736), which showed IC50 values of 0.15 nM against T. congolense and 1.3 nM against T. vivax, and demonstrated 100% efficacy with a single dose of 10 mg/kg against both T. congolense and T. vivax in mouse models of infection (IP dosing) and in the target animal, cattle, dosed intramuscularly. AN11736 has been advanced to early development studies. https://sonar.ch/global/documents/232568 eng info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2017.11.028 info:eu-repo/semantics/altIdentifier/pmid/29169674 Bioorganic & medicinal chemistry letters. - 2018 Benzoxaborole Cattle Lead optimisation Protozoan SAR Trypanosomiasis Animals Antiprotozoal Agents Boron Compounds Cattle Mice Structure-Activity Relationship Trypanosoma congolense Trypanosoma vivax Trypanosomiasis, African Valine Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT). http://purl.org/coar/resource_type/c_6501