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Recenzirano
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da Rosa, Rafael; Zimmermann, Lara Almida; de Moraes, Milene Höehr; Schneider, Naira Fernanda Zanchett; Schappo, Alice Duarte; Simões, Claudia Maria de Oliveira; Steindel, Mario; Schenkel, Eloir Paulo; Bernardes, Lílian Sibelle Campos
Bioorganic & medicinal chemistry letters, 11/2018, Letnik: 28, Številka: 20Journal Article
Display omitted •Synthesis and characterization of 20 isoxazolyl-sulfonamides are reported.•The compounds were active against T. cruzi, L. amazonensis, and HSV-1.•Druglikeness evaluation showed potential for further pre-clinical development. In this study we report the synthesis, characterization, biological evaluation, and druglikeness assessment of a series of 20 novel isoxazolyl-sulfonamides, obtained by a four-step synthetic route. The compounds had their activity against Trypanosoma cruzi, Leishmania amazonensis, Herpes Simplex Virus type 1 and cytotoxicity evaluated in phenotypic assays. All compounds have drug-like properties, showed low cytotoxicity and were promising regarding all other biological activities reported herein, especially the inhibitory activity against T. cruzi. The compounds 8 and 16 showed significant potency and selectivity against T. cruzi (GI50 = 14.3 µM, SI > 34.8 and GI50 = 11.6 µM, SI = 29.1, respectively). These values, close to the values of the reference drug benznidazole (GI50 = 10.2 µM), suggest that compounds 8 and 16 represent promising candidates for further pre-clinical development targeting Chagas disease.
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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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