Evaluation of Novel 7-(hetero)aryl-substituted Pyrazolo[1, 5-a]pyrimidines as Phosphodiesterase-4 Inhibitors

Construction of a six-membered fused N-heterocyclic ring via a new 3-component reaction: synthesis of (pyrazolo)pyrimidines/pyridines

“…1) derived from Ibudilast A as a potential scaffold for the development of novel PDE4 inhibitors. 5 In further continuation of this research and our long standing interest in PDE4/TNF-a inhibitors, 4,6 we planned to generate a library of compounds based on C (Fig. 1).…”

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

“…SAR analysis indicated that the existence of a heteroaryl moiety (possessing acidic hydrogen) or bi-cyclic aryl at the carbon-7 of the pyrazolopyrimidine skeleton was key for the inhibitory potential of this group of derivatives. 156 Based on the structure of 2-[(4,6-diphenethoxypyrimidin-2yl)thio]hexanoic acid (183), Hieke et al discovered a new family of strong 5-LOX inhibitors. All the target compounds were characterized for their inuence on the activity of human 5-LOX.…”

“…SAR analysis indicated that the existence of a heteroaryl moiety (possessing acidic hydrogen) or bi-cyclic aryl at the carbon-7 of the pyrazolopyrimidine skeleton was key for the inhibitory potential of this group of derivatives. 156 …”