An appraisal on synthetic and pharmaceutical perspectives of pyrazolo[4, 3-d]pyrimidine scaffold. Issue 2 (15th January 2018)

• Record Type: Journal Article
• Authors: Cherukupalli, Srinivasulu; Hampannavar, Girish A.; Chinnam, Sampath; Chandrasekaran, Balakumar; Sayyad, Nisar; Kayamba, Francis; Reddy Aleti, Rajeshwar; Karpoormath, Rajshekhar
• Is Part Of: Bioorganic & medicinal chemistry. Volume 26:Issue 2(2018)
• Page Start: 309
• Page End: 339
• Publication Date: 2018-01-15
• Subjects: A. flavus Aspergillus flavus -- C. albicans Candida albicans -- cAMP cyclic adenosine monophosphate -- CDK cyclin-dependent kinase -- CNS central nervous system -- COX cyclooxygenase -- CRF corticotropin-releasing hormone -- CRK cdc2-related kinase -- CYC6 cyclin 6 -- DNA deoxyribonucleic acid -- E. coli Escherichia coli -- EAC Ehrlich ascites carcinoma -- EC50 half maximal effective concentration -- ED50 median effective dose -- ER estrogen receptor -- G. candidum Geotrichum candidum -- GI50 half maximal growth inhibitory -- hA human adenosine -- HCV hepatitis C virus -- HDACs histone deacetylases -- HIV human immunodeficiency virus -- HLM human liver microsome -- HSV-1 herpes simplex virus type-1 -- IC50 half maximal inhibitory concentration -- Ki inhibition constant -- kNN-MFA k-nearest neighbor molecular field analysis -- MIC minimum inhibitory concentration -- MLR multiple linear regression -- P. aeruginosa Pseudomonas aeruginosa -- PAH pulmonary arterial hypertension -- PDE phosphodiesterase -- PET positron emission tomography -- RNA ribonucleic acid -- RSV human respiratory syncytial virus -- S. lactis Streptococcus lactis -- S. aureus Staphylococcus aureus -- SI selectivity index; Pyrazolo[4, 3-d]pyrimidine -- Synthetic strategies -- Anti-cancer agents -- Anti-infectious agents -- PDE-5 inhibitors -- Cytokinin antagonists; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2017.10.012
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Highlights: Pyrazolo[4, 3- d ]pyrimidine: Nitrogen containing bicyclic heterocyclic ring with diverse biological activities. Synthetic strategies for variously substituted pyrazolo[4, 3- d ]pyrimidine. The numerous pharmacological activities of pyrazolo[4, 3- d ]pyrimidine has been discussed. SAR of pyrazolo[4, 3- d ]pyrimidine scaffold for miscellaneous activities has been explained. This review will be helpful for medicinal chemists in designing future drugs. 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.