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Pelizaro, Bruno I.; Batista, Jaqueline C. Z.; Portapilla, Gisele B.; das Neves, Amarith R.; Silva, Fernanda; Carvalho, Diego B.; Shiguemoto, Cristiane Y. K.; Pessatto, Lucas R.; Paredes-Gamero, Edgar J.; Cardoso, Iara A.; Luccas, Pedro H.; Nonato, M. Cristina; Lopes, Norberto P.; Galvão, Fernanda; Oliveira, Kelly M. P.; Cassemiro, Nadla S.; Silva, Denise B.; Piranda, Eliane M.; Arruda, Carla C. P.; de Albuquerque, Sergio; Baroni, Adriano C. M.
Journal of medicinal chemistry, 02/2024, Letnik: 67, Številka: 4Journal Article
A series of 28 compounds, 3-nitro-1H-1,2,4-triazole, were synthesized by click-chemistry with diverse substitution patterns using medicinal chemistry approaches, such as bioisosterism, Craig-plot, and the Topliss set with excellent yields. Overall, the analogs demonstrated relevant in vitro antitrypanosomatid activity. Analog 15g (R1 = 4-OCF3–Ph, IC50 = 0.09 μM, SI = >555.5) exhibited an outstanding antichagasic activity (Trypanosoma cruzi, Tulahuen LacZ strain) 68-fold more active than benznidazole (BZN, IC50 = 6.15 μM, SI = >8.13) with relevant selectivity index, and suitable LipE = 5.31. 15g was considered an appropriate substrate for the type I nitro reductases (TcNTR I), contributing to a likely potential mechanism of action for antichagasic activity. Finally, 15g showed nonmutagenic potential against Salmonella typhimurium strains (TA98, TA100, and TA102). Therefore, 3-nitro-1H-1,2,4-triazole 15g is a promising antitrypanosomatid candidate for in vivo studies.
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Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Vir: Osebne bibliografije
in: SICRIS
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