Cherukupalli Srinivasulu, Karpoormath Rajshekhar, Chandrasekaran Balakumar, Hampannavar Girish A, Thapliyal Neeta, Palakollu Venkata Narayana
Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
Eur J Med Chem. 2017 Jan 27;126:298-352. doi: 10.1016/j.ejmech.2016.11.019. Epub 2016 Nov 10.
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, CRF 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.
吡唑并[1,5 - a]嘧啶骨架是药物研发中一类重要的杂环结构。它作为开发类药物候选物的构建模块，展现出广泛的药用特性，如抗癌、中枢神经系统药物、抗感染、抗炎、促肾上腺皮质激素释放因子拮抗剂以及放射性诊断等。构效关系（SAR）研究在药物化学家中受到了更多关注，并且许多先导化合物已针对各种疾病靶点得以衍生。然而，药物化学家在开发潜在药物候选物时，进一步利用这种重要骨架仍有很大空间。本综述简要概述了用于吡唑并[1,5 - a]嘧啶衍生物的相关合成策略。它还广泛揭示了其重要的生物学特性以及构效关系研究。据我们所知，当前的综述是首次尝试汇编自20世纪80年代以来报道的关于吡唑并[1,5 - a]嘧啶的重大进展。
