Acute asthma is still a major medical issue in the modern world. Despite its prevalence, asthma remains a challenging condition to manage effectively, so continuous research efforts are necessary. Firstly, it is necessary to understand the underlying causes and mechanisms of asthma to develop effective prevention strategies and treatments. Exacerbations are a key factor in determining the severity of asthma in people of all ages. Additionally, research is needed to explore new therapeutic options and interventions that can improve the management of asthma, reduce symptom severity, and enhance the overall quality of life for individuals with asthma. Therefore, in this present work, we designed some novel Benzimidazole derivatives 1-(1H-benzimidazol-1-yl)-2-(substituted) ethanone (III-a to III-i) and synthesized by simple synthesis of Benzimidazol-1-yl-2-chloroethanone (II). Benzimidazol-1-yl-2- chloroethanone (II) is treated with different aromatic and aliphatic amines in ethanol, refluxed for 4-6 hrs to obtain final Benzimidazole derivatives 1-(1H-benzimidazol-1- yl)-2-(substituted) ethanone (III). The designed and synthesized novel derivatives were screened for invitro anti-asthmatic and anti-inflammatory activities. In-vitro anti-asthmatic activity was performed by using the Isolated Goat Tracheal chain method. In-vitro anti-inflammatory activity was performed by the Gelatin Zymography method. Experimental results revealed that some of the derivatives showed good anti-asthmatic & anti-inflammatory activities along with the standard drug fexofenadine