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Design and Synthesis of 1,3-Diarylpyrazoles and Investigation of Their Cytotoxicity and Antiparasitic Profile.

التفاصيل البيبلوغرافية
العنوان: Design and Synthesis of 1,3-Diarylpyrazoles and Investigation of Their Cytotoxicity and Antiparasitic Profile.
المؤلفون: Bozdag M; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Mertens F; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Matheeussen A; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Van Pelt N; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Foubert K; Natural Products and Food Research and Analysis-Pharmaceutical Technology, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Hermans N; Natural Products and Food Research and Analysis-Pharmaceutical Technology, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., De Meyer GRY; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Augustyns K; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Martinet W; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Caljon G; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Van der Veken P; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium.
المصدر: International journal of molecular sciences [Int J Mol Sci] 2024 Apr 25; Vol. 25 (9). Date of Electronic Publication: 2024 Apr 25.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 101092791 Publication Model: Electronic Cited Medium: Internet ISSN: 1422-0067 (Electronic) Linking ISSN: 14220067 NLM ISO Abbreviation: Int J Mol Sci Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, [2000-
مواضيع طبية MeSH: Pyrazoles*/pharmacology , Pyrazoles*/chemistry , Pyrazoles*/chemical synthesis , Trypanosoma cruzi*/drug effects, Humans ; Antiparasitic Agents/pharmacology ; Antiparasitic Agents/chemical synthesis ; Antiparasitic Agents/chemistry ; Drug Design ; Leishmania infantum/drug effects ; Structure-Activity Relationship ; Trypanosoma brucei rhodesiense/drug effects ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/chemical synthesis ; Antiprotozoal Agents/chemistry
مستخلص: Herein, we report a series of 1,3-diarylpyrazoles that are analogues of compound 26 /HIT 8. We previously identified this molecule as a 'hit' during a high-throughput screening campaign for autophagy inducers. A variety of synthetic strategies were utilized to modify the 1,3-diarylpyrazole core at its 1-, 3-, and 4-position. Compounds were assessed in vitro to identify their cytotoxicity properties. Of note, several compounds in the series displayed relevant cytotoxicity, which warrants scrutiny while interpreting biological activities that have been reported for structurally related molecules. In addition, antiparasitic activities were recorded against a range of human-infective protozoa, including Trypanosoma cruzi , T. brucei rhodesiense , and Leishmania infantum . The most interesting compounds displayed low micromolar whole-cell potencies against individual or several parasitic species, while lacking cytotoxicity against human cells.
معلومات مُعتمدة: CA21111 European Cooperation in Science and Technology; 1244521N Research Foundation - Flanders; iBOF-21-053 University of Antwerp
فهرسة مساهمة: Keywords: 1,3-diarylpyrazole; antiparasitic activity; cytotoxicity; pyrazole
المشرفين على المادة: 0 (Pyrazoles)
0 (Antiparasitic Agents)
0 (Antiprotozoal Agents)
تواريخ الأحداث: Date Created: 20240511 Date Completed: 20240511 Latest Revision: 20240511
رمز التحديث: 20240512
DOI: 10.3390/ijms25094693
PMID: 38731916
قاعدة البيانات: MEDLINE
الوصف
تدمد:1422-0067
DOI:10.3390/ijms25094693