A Sonochemical Access to 5-Aryl Substituted Pyrazolo[1,5-a]Pyrimidines as Potential Inhibitors of TNF-α

Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo[1,5-a]pyrimidine scaffold

“…The mechanism involved the furan-2,5dione ring-opening and cyclocondensation steps. Treatment of pyrazoloij1,5-a]pyrimidine 122 with 3-acetyldihydrofuran-2IJ3H)one (123) in phosphorus oxychloride yielded the tricyclic 124 as a major product with the formation of the tetracyclic product Scheme 11 Synthesis of pyrazolopyrimidinyl-N,N-alkyl-acetamides.…”

“…The potency of the compounds against 15-LOX presented a good potential inhibition for compound 186c (IC 50 = 5.6 μM) even though it was more potent than nordihydroguaiaretic acid (IC 50 = 8.5 μM). More recently, Prasada Rao et al 123 have prepared a series of pyrazolo[1,5- a ]pyrimidine derivatives and assessed their potency against inhibition of TNF-α with remarkable results.…”