Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH-58, Near Baghpat Crossing, Bypass Road, Meerut-250005, India.
Mini Rev Med Chem. 2019;19(9):727-736. doi: 10.2174/1389557518666180928154004.
Azaindoles have been accepted as important structures having various biological activities in medicinal chemistry in novel drug discovery. Various azaindole derivatives have been used commercially and newer analogues are synthesized continuously. As in literature, azaindole is a very potent moiety, its derivatives displayed a number of biological activities such as kinase inhibitors, cytotoxic agents, anti-angiogenic activity, CRTh2 receptor antagonists, melanin agonists, nicotine agonists, effectiveness in alzheimer disease, cytokinin analogs, Orai inhibitors in asthma and chemokine receptor- 2 (CCR2) antagonists. This review consists of biological activities of various azaindole analogs, reported so far, and their structure activity relations, along with future perspectives in this field.
在新药发现中，氮茚类化合物已被接受为具有各种生物活性的重要结构，在医学化学中具有重要地位。各种氮茚类衍生物已被商业化应用，并且新型类似物也在不断被合成。正如文献中所指出的，氮茚是一种非常有效的部分，其衍生物表现出许多生物活性，如激酶抑制剂、细胞毒性剂、抗血管生成活性、CRTh2 受体拮抗剂、黑色素激动剂、尼古丁激动剂、阿尔茨海默病的疗效、细胞分裂素类似物、哮喘中的 Orai 抑制剂和趋化因子受体-2 (CCR2) 拮抗剂。这篇综述包括迄今为止报道的各种氮茚类类似物的生物活性及其构效关系，并展望了该领域的未来前景。
