A series of new fluoro-substituted benzimidazole derivatives were designed, synthesized and pharmacologically evaluated. All the target compounds were characterized by ¹HNMR, ¹³CNMR, mass spectra and elemental analysis. The biological evaluation showed that most of the synthesized compounds displayed nanomolar affinity to the angiotensin II type 1 (AT₁) receptor and could decrease blood pressure efficiently in spontaneously hypertensive rats. The maximal response of mean blood pressure (MBP) lowered 74.5 ± 3.5 mmHg (1g) and 69.2 ± 0.9 mmHg (2a) at 10 g/kg after oral administration, and the antihypertensive effect lasted beyond 24 h, which performed better than both losartan and telmisartan. So, compounds 1g and 2a may be considered as potential antihypertension drug candidates.

设计，合成和药理学评估了一系列新的氟取代的苯并咪唑衍生物。所有目标化合物均通过¹ HNMR，¹³ CNMR，质谱和元素分析进行表征。生物学评估表明，大多数合成化合物对自发性高血压大鼠的血管紧张素II 1型（AT ₁）受体均具有纳摩尔浓度的亲和力，并且可以有效降低血压。口服后10 g / kg的平均血压（MBP）的最大响应降低了74.5±3.5 mmHg（1g）和69.2±0.9 mmHg（2a），并且降压作用持续超过24 h，其效果均优于氯沙坦和替米沙坦。所以，化合物1g和2a可能被视为潜在的抗高血压药物候选者。