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.

设计并合成了新型L-缬氨酸酰胺苯并氧硼杂硼化合物和类似物，用于结构-活性关系 (SAR) 研究，以优化对刚果锥虫( T. congolense ) 和间日锥虫( T. vivax ) 寄生虫的生长抑制活性。该研究鉴定出 4-氟苄基 (1-羟基-7-甲基-1,3-二氢苯并[ c ][1,2]氧杂硼杂环戊二烯-6-羰基)-l-缬氨酸( 5 , AN11736 )，其 IC ₅₀值为针对刚果锥虫为 0.15 nM，针对间日锥虫为 1.3 nM，在小鼠感染模型（IP 给药）和目标中，单剂量 10 mg/kg 对刚果锥虫和间日锥虫均具有 100% 功效动物、牛，肌肉注射。 AN11736已进入早期开发研究。