2. Academic Validation
  3. An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold

An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold

  • Eur J Med Chem. 2017 Jan 27:126:298-352. doi: 10.1016/j.ejmech.2016.11.019.
Srinivasulu Cherukupalli 1,  Rajshekhar Karpoormath 2,  Balakumar Chandrasekaran 1,  Girish A Hampannavar 1,  Neeta Thapliyal 1,  Venkata Narayana Palakollu 1
Affiliations

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: karpoormath@ukzn.ac.za.
PMID: 27894044 DOI: 10.1016/j.ejmech.2016.11.019
Abstract

Pyrazolo[1,5-a]pyrimidine scaffold is one of the privileged hetrocycles in drug discovery. Its application as a buliding block for developing drug-like candidates has displayed broad range of medicinal properties such as Anticancer, CNS agents, anti-infectious, anti-inflammatory, CRF1 antagonists and radio diagnostics. The structure-activity relationship (SAR) studies have acquired greater attention amid medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is plenty of room for the medicinal chemists to further exploit this privileged scaffold in developing potential drug candidates. The present review briefly outlines relevant synthetic strategies employed for pyrazolo[1,5-a]pyrimidine derivatives. It also extensively reveals significant biological properties along with SAR studies. To the best of our understanding current review is the first attempt made towards the compilation of significant advances made on pyrazolo[1,5-a]pyrimidines reported since 1980s.

Keywords

Anti-cancer agents; Anti-infectious agents; Anti-inflammatory agents; CNS agents; Pyrazolo[1,5-a]pyrimidine; Radiopharmaceuticals.

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