دورية أكاديمية
Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus.
| العنوان: | Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus. |
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| المؤلفون: | da Rosa R; Graduate Program in Pharmacy, Pharmaceutical and Medicinal Chemistry Laboratory, Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Zimmermann LA; Graduate Program in Pharmacy, Pharmaceutical and Medicinal Chemistry Laboratory, Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., de Moraes MH; Protozoology Laboratory, Department of Microbiology, Immunology and Parasitology, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Schneider NFZ; Applied Virology Laboratory, Department of Microbiology, Immunology and Parasitology, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Schappo AD; Graduate Program in Pharmacy, Pharmaceutical and Medicinal Chemistry Laboratory, Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Simões CMO; Applied Virology Laboratory, Department of Microbiology, Immunology and Parasitology, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Steindel M; Protozoology Laboratory, Department of Microbiology, Immunology and Parasitology, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Schenkel EP; Graduate Program in Pharmacy, Pharmaceutical and Medicinal Chemistry Laboratory, Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil., Bernardes LSC; Graduate Program in Pharmacy, Pharmaceutical and Medicinal Chemistry Laboratory, Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis 88040-900 SC, Brazil. Electronic address: l.bernardes@ufsc.br. |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Nov 01; Vol. 28 (20), pp. 3381-3384. Date of Electronic Publication: 2018 Aug 31. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Antiviral Agents/*pharmacology , Isoxazoles/*pharmacology , Sulfonamides/*pharmacology , Trypanocidal Agents/*pharmacology, Animals ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/toxicity ; Cell Line, Tumor ; Cell Survival/drug effects ; Chlorocebus aethiops ; Humans ; Isoxazoles/chemical synthesis ; Isoxazoles/chemistry ; Isoxazoles/toxicity ; Leishmania/drug effects ; Molecular Structure ; Simplexvirus/drug effects ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/chemistry ; Sulfonamides/toxicity ; Trypanocidal Agents/chemical synthesis ; Trypanocidal Agents/chemistry ; Trypanocidal Agents/toxicity ; Trypanosoma cruzi/drug effects ; Vero Cells |
| مستخلص: | 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 (GI (Copyright © 2018 Elsevier Ltd. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Herpes Simplex Virus; Isoxazole; Leishmania amazonensis; Sulfonamide; Trypanosoma cruzi |
| المشرفين على المادة: | 0 (Antiviral Agents) 0 (Isoxazoles) 0 (Sulfonamides) 0 (Trypanocidal Agents) |
| تواريخ الأحداث: | Date Created: 20180909 Date Completed: 20190603 Latest Revision: 20191210 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1016/j.bmcl.2018.08.040 |
| PMID: | 30194008 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2018.08.040 |