An Overview on Synthetic and Medicinal Perspectives of [1,2,4]Triazolo[1,5‐a]pyrimidine Scaffold

Abstract

Triazolo[1,pyrimidine is an important heterocyclic scaffold known to have a wide range of pharmacological activities such as anticancer, antimicrobial, anti-tubercular, CB 2 cannabinoid agonists, feticide, and adenosine antagonists. Several clinical trials and marketed drugs such as Trapidil, Essramycin, Pyroxsulam, DSM-265, Flumetsulam, GNF-6702, and Cevipabulin indicate the potential of [1,2,4]triazolo[1,5-a]pyrimidine moiety with various functional groups in medicinal chemistry. Herein, we represent a concise report focusing on the synthetic strategies used for diversely substituted [1,2,4]triazolo [1,5-a]pyrimidine analogs and their pharmacological applications. To the best of our knowledge, since 1980, we are the first to write a review on this emerging scaffold, which reveals the synthetic strategies, and pharmacological activities of differently substituted [1,2,4]triazolo[1,5-a]pyrimidine with special emphasis on structure-activity relationship studies.

Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives

“…Various antimicrobial triazole derivatives have Molecules 2023, 28, 7876 2 of 16 been developed and most of them show potent antimicrobial activity [8]. It is particularly noteworthy that more effective antibacterial candidates might be obtained from the various triazole fused heterocyclic derivatives, extensively existing in chemistry, such as triazolo[1,5-a]pyrimidine [9], triazolo [4,5-c]pyridine [10], triazolo [4,3-a]pyrazine [11], triazolo [4,5-d]pyrimidine [12], triazolo [4,3-a]quinoxaline [13], triazolo[1,5-a]quinolines [14], and triazolo[1,5-a]pyridine [15,16]. Some triazole fused heterocyclic derivatives have been found to have high antibacterial activity against both drug-sensitive and drug-resistant pathogens and are not inferior to the first-line antimicrobial agents [17,18].…”