Recent Progress in 1,2,4-Triazolo[1,5-a]pyrimidine Chemistry

Metal-Based Therapeutics for Leishmaniasis

“…The most widely known derivative is the simple molecule Trapidil or Rocornal, a clinically used antiischemic and cardiatonic agent which acts as a platelet-derived growth factor (PDGF) antagonist and as a phosphodiesterase inhibitor. [39] This family of compounds have also found interesting applications as antipyretic, analgesic and antiinflammatory, herbicidal, fungicidal agents with about 200 relevant patents. For example, 2arenesulfonamido triazolopyrimidines were tested as leishmanicides showing some of them similar in vitro activity than pentamidine against L. donovani (Figure 7).…”

“…Structures of triazolopyrimidine drugs: a) the anticoagulant drug Trapidil; b) a series of leishmanicidal derivatives [39]. …”

Synthesis and biological evaluation of novel steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines

“…On the other hand, 1,2,4-triazolo[1,5-a]pyrimidines (TPs), a subtype of purine analogs, have been widely investigated and identified to possess multifaceted pharmacological properties, including antihypertensive, cardiac stimulant, antimalarial, antifungal, anti-HBV, antimicrobial and anticancer activities [14][15][16][17][18][19][20][21]. In addition, triazolopyrimidines are versatile ligands and their coordination compounds can be considered as model systems for metal-ligand interactions observed in biological systems [20a,22].…”

An Efficient Three Component One-Pot Synthesis of 5-Amino-7-aryl-7,8-dihydro-[1,2,4] triazolo[4,3-a]-pyrimidine-6-carbonitriles

“…It is well known that the condensation of aminoheterocycles and pyrimidine gives rise to the formation of bicyclic heterocycles known as triazolopyrimidines [ 5 ]. The 1,2,4-triazolopyrimidines have attracted growing interest due to their important pharmaceutical properties [ 6 , 7 , 8 ], and they appear in a variety of synthetic pharmacophores which possess anti-parasitic, antimicrobial, anticancer and antibiotic activities [ 9 , 10 , 11 ].…”