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

  • Bioorg Med Chem. 2018 Jan 15;26(2):309-339. doi: 10.1016/j.bmc.2017.10.012.
Srinivasulu Cherukupalli  1 ,  Girish A Hampannavar  1 ,  Sampath Chinnam  1 ,  Balakumar Chandrasekaran  1 ,  Nisar Sayyad  1 ,  Francis Kayamba  1 ,  Rajeshwar Reddy Aleti  1 ,  Rajshekhar Karpoormath  2
Affiliations
  • 1. Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
  • 2. Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa. Electronic address: [email protected].
PMID: 29273417 DOI: 10.1016/j.bmc.2017.10.012
Abstract

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.

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