A review of recent progress (2002-2012) on the biological activities of pyrazoles

Abstract

Dedicated to Professor Rosa M. Claramunt on the occasion of her 65 th anniversary AbstractIn this review, we report the structures of 243 pyrazoles with their corresponding biological activities. All of them are represented around the common structure of the pyrazole ring even in those cases where the heterocycle is only a minor part of the molecule. The classification we have used is based on chemical structure considerations and not in terms of the therapeutic area which is the more common approach. Some general conclusions have been drawn linking structures with activities.

Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET)

“…Abdel-Maksoud et al have demonstrated antitumoral activity of several compounds with a pyrazole and sulfonamide moieties [19]; antibacterial and antifungal activity of pyrazole was demonstrated by Chowdary et al [20]. Pyrazoles also showed good activity as monoamine oxidase inhibitors, antidepressant and anticonvulsant agents [21], as BRAF inhibitors [22] and DNA gyrase inhibitors [23] and present antileishmanial, anti-inflammatory, analgesic, antidiabetic and cannabinoid activity; cyclin-dependent kinase and tissue-nonspecific alkaline phosphatase inhibitory activity and moderate antihepatotoxic activity, among others [9,11,[24][25][26][27][28][29]. In 2013, Prabhu et.…”

Possible interactions between fused pyrazole derivative and magnesium ions - NMR experiments and theoretical calculations

“…Pyrazole derivatives are also useful in the treatment of obesity and CNS disorders including Alzheimer's and Parkinson's disease. [1][2][3][4] Among the anticancer drugs, pyrazole or indazole derivatives like Celecoxib, anthrapyrazoles (piroxantrone, losoxantrone), and Axitinib Magnesium ions, Mg 2+ , participate in many biochemical processes including these involved in cancerogenesis like proliferation, angiogenesis and apoptosis. 7,8 The role of magnesium in cancerogenesis is, however, not clearly understood.…”

Novel directed synthesis of functionalized pyrazole derivatives via regioselective solvent-free thiylation of 3-alkenylpyrazoles with arenethiols

“…Pyrazole and its derivatives attract the attention of the chemical community mainly on account of the wide spectrum of their pharmacological activities, [1][2][3][4][5][6] including antibacterial, 7 antidepressant, 8 antiinflammatory, 9 antitumor, 10 etc. They are widely used as agrochemicals.…”

“…24,25 They are also applied in the design of complexes with unusual magnetic properties. 26,27 In the search for novel pyazoles as building blocks for the synthesis of biologically active and technologically useful substances, [1][2][3][4][5][6] the development of new methods for the preparation of functionalized pyrazoles and the synthesis of new pyrazole derivatives present an urgent challenge.…”

“…[1][2][3][4][5][6][28][29][30][31][32][33][34][35][36][37][38][39] The chemical transformations of alkenylpyrazoles are still poorly understood. It is known that N-alkenyl-and some 4-alkenylpyrazoles can participate in polymerization, 21,29 complex formation, 30,31 thiylation, 32 and cycloaddition.…”