Antagonists of adenosine receptor are under exploration as potential drug candidates for treatment of neurological disorders, depression, certain cancers and potentially used as a cancer immunotherapy. Herein, we describe design and synthesis of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine (6) derivatives. All the compounds were evaluated for A_2A AR antagonist activity and displayed encouraging results (IC₅₀ 9–300 nM) of A_2A AR antagonist binding affinity in biochemical assay. Compound 27 exhibits good activity in A_2A AR antagonist cAMP functional assay (IC₅₀ 31 nM) and further this compound shows T-cell activation at the IL-2 production assay (EC₅₀ 165 nM). Molecular docking studies were carried out to rationalize the observed binding affinity of compound 27.

腺苷受体的拮抗剂正在探索作为治疗神经系统疾病，抑郁症，某些癌症的潜在候选药物，并有可能用作癌症免疫疗法。在这里，我们描述了新型支架苯并[4,5]咪唑并[1,2 - a ]吡嗪-1-胺（6）衍生物的设计和合成。对所有化合物的A _2A AR拮抗剂活性进行了评估，并在生化分析中显示出令人鼓舞的A _2A AR拮抗剂结合亲和力结果（IC ₅₀ 9–300 nM）。化合物27在A _2A AR拮抗剂cAMP功能测定（IC ₅₀31 nM），并且该化合物在IL-2产生试验（EC ₅₀ 165 nM）时显示T细胞活化。进行了分子对接研究以合理化所观察到的化合物27的结合亲和力。