An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4,3-d]pyrimidine scaffold

作者：Cherukupalli Srinivasulu; Hampannavar Girish A; Chinnam Sampath; Chandrasekaran Balakumar; Sayyad Nisar; Kayamba Francis; Aleti Rajeshwar Reddy; Karpoormath Rajshekhar^*

来源：Bioorganic & Medicinal Chemistry, 2018, 26(2): 309-339.

DOI：10.1016/j.bmc.2017.10.012

• Pyrazolo[4,3-d]pyrimidine
• Synthetic strategies
• Anti-cancer agents
• Anti-infectious agents
• PDE-5 inhibitors
• Cytokinin antagonists

Pyrazolo[4,3-d]pyrimidine, a fused heterocycle bearing pyrazole and pyrimidine portions has gained a significant attention in the field of bioorganic and medicinal chemistry. Pyrazolo[4,3-d]pyrimidine derivatives have demonstrated numerous pharmacological activities particularly, anti-cancer, anti-infectious, phosphodiesterase inhibitors, adenosine antagonists and cytokinin antagonists etc. This review extensively unveils the synthetic and pharmacological diversity with special emphasis on structural variations around pyrazolo[4,3-d]pyrimidine scaffold. This endeavour has thus uncovered the medicinal worthiness of pyrazolo[4,3-d]pyrimidine framework. To the best of our knowledge this review is the first compilation on synthetic, medicinal and structure activity relationship (SAR) aspects of pyrazolo[4,3-d]pyrimidines since 1956.

• 出版日期2018-1-15