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Design and Synthesis of Novel 3-Nitro-1 H -1,2,4-triazole-1,2,3-triazole-1,4-disubstituted Analogs as Promising Antitrypanosomatid Agents: Evaluation of In Vitro Activity against Chagas Disease and Leishmaniasis.
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- Author(s): Pelizaro BI;Pelizaro BI; Batista JCZ; Batista JCZ; Portapilla GB; Portapilla GB; das Neves AR; das Neves AR; das Neves AR; Silva F; Silva F; Carvalho DB; Carvalho DB; Shiguemoto CYK; Shiguemoto CYK; Pessatto LR; Pessatto LR; Paredes-Gamero EJ; Paredes-Gamero EJ; Cardoso IA; Cardoso IA; Luccas PH; Luccas PH; Nonato MC; Nonato MC; Lopes NP; Lopes NP; Galvão F; Galvão F; Oliveira KMP; Oliveira KMP; Cassemiro NS; Cassemiro NS; Silva DB; Silva DB; Piranda EM; Piranda EM; Arruda CCP; Arruda CCP; de Albuquerque S; de Albuquerque S; Baroni ACM; Baroni ACM
- Source:
Journal of medicinal chemistry [J Med Chem] 2024 Feb 22; Vol. 67 (4), pp. 2584-2601. Date of Electronic Publication: 2024 Feb 02.- Publication Type:
Journal Article; Research Support, Non-U.S. Gov't- Language:
English - Source:
- Additional Information
- Source: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
- Publication Information: Publication: Washington Dc : American Chemical Society
Original Publication: [Easton, Pa.] : American Chemical Society, [c1963- - Subject Terms:
- Abstract: A series of 28 compounds, 3-nitro-1 H -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 (R
1 = 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-1 H -1,2,4-triazole 15g is a promising antitrypanosomatid candidate for in vivo studies. - Accession Number: 288-88-0 (1,2,4-triazole)
0 (Trypanocidal Agents)
0 (Triazoles) - Publication Date: Date Created: 20240202 Date Completed: 20240223 Latest Revision: 20241002
- Publication Date: 20241002
- Accession Number: 10.1021/acs.jmedchem.3c01745
- Accession Number: 38305199
- Source:
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