title: An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
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, CRF1antagonists 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.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
authors.forename: Srinivasulu
authors.initials: S
authors.lastname: Cherukupalli
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa. Electronic address: karpoormath@ukzn.ac.za.
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
authors.forename: Balakumar
authors.initials: B
authors.lastname: Chandrasekaran
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
authors.forename: Girish A
authors.initials: GA
authors.lastname: Hampannavar
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
authors.forename: Neeta
authors.initials: N
authors.lastname: Thapliyal
authors.affiliation: Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
authors.forename: Venkata Narayana
authors.initials: VN
authors.lastname: Palakollu
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry*
chemical_list: D011720:Pyrazoles; D011743:Pyrimidines
keywords: Anti-cancer agents; Anti-infectious agents; Anti-inflammatory agents; CNS agents; Pyrazolo[1,5-a]pyrimidine; Radiopharmaceuticals