Design, Synthesis, and Structure–Activity Relationship of 2‑(Piperazin-1-yl)quinazolin-4(3H)‑one Derivatives as Active Agents against Toxoplasma gondii

• Published in: Journal of agricultural and food chemistry Vol. 73; no. 10; pp. 6215 - 6230
• Main Authors: Deng, Yu, Yu, Yuan-Di, Song, Chao, Xu, Guo-Yang, Xu, Yue, Ye, Chang-Ju
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 12.03.2025; Amer Chemical Soc
• Subjects: Agriculture; Agriculture, Multidisciplinary; animal models; Animals; Antiprotozoal Agents - chemical synthesis; Antiprotozoal Agents - chemistry; Antiprotozoal Agents - pharmacology; Chemistry; Chemistry, Applied; cytotoxicity; Drug Design; Female; food chemistry; Food Science & Technology; Functional Structure/Activity Relationships; Humans; hybridization; Life Sciences & Biomedicine; Mice; Mice, Inbred BALB C; moieties; Molecular Structure; parasite load; parasites; Physical Sciences; piperazine; Piperazines; Quinazolinones - chemical synthesis; Quinazolinones - chemistry; Quinazolinones - pharmacology; Science & Technology; Structure-Activity Relationship; structure-activity relationships; Toxoplasma - drug effects; Toxoplasma - growth & development; Toxoplasma gondii; Toxoplasmosis - drug therapy; Toxoplasmosis - parasitology; quinazolinone; diarylether; antiparasitic; Toxoplasma gondii; ACID; RECEPTOR; MALARIA; HIGHLY POTENT; POTENT INHIBITORS; DISCOVERY; HYBRID

A novel series of quinazolin-4­(3H)-one derivatives were synthesized using a hybridization strategy that combined the quinazolin-4­(3H)-one scaffold, the diarylether fragment, and the piperazine ring. The in vitro activity evaluation of these compounds against Toxoplasma gondii demonstrated that mos...