Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists

A Greener and Efficient Method for Nucleophilic Aromatic Substitution of Nitrogen-Containing Fused Heterocycles

“…Some [1,2,4]-triazolo[1,5- a ]pyrimidines possess herbicidal activity [ 46 , 47 ], while others can act as antifungal [ 48 , 49 ], antitubercular [ 50 , 51 ] and antibacterial [ 52 ] agents. Polycyclic systems containing a [1,2,4]triazolo[1,5- a ]-pyrimidine moiety are reported as antitumor agents [ 53 , 54 ], as corticotropin releasing factor 1 receptor antagonists [ 55 ] or calcium channel modulators [ 56 ] and they can also be used for the treatment of Alzheimer’s disease [ 57 ] and insomnia [ 58 ].…”

Aminoazole-Based Diversity-Oriented Synthesis of Heterocycles

“…Acetoacetic esters may be easily replaced by malonic ester or sodium nitromalonaldehyde monohydrate (Ren et al, 2012 ). The malonic esters 248 were used as efficient starting materials for the synthesis of the azoloazines 249 substituted in the position 5 (Saito et al, 2011 ; Figure 20 ).…”

Synthesis of New [1,2,4]Triazolo[1,5‐a]pyrimidine Derivatives: Reactivity of 3‐Amino[1,2,4]triazole towards Enaminonitriles and Enaminones

“…Over the years, various substituted derivatives of these scaffolds have shown to act as antifungal , antitubercular , and antibacterial agents. They have proven as well to be excellent herbicidal and plant growth regulators ; polycyclic systems containing [1,2,4]triazolo[1,5‐ a ]‐pyrimidine moiety are reported as corticotropin‐releasing factor 1 receptor antagonists or calcium channel modulators . They were also reported to possess promising anticancer activities, particularly those with C‐5, C‐6, or C‐7 substituents .…”