دورية أكاديمية
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Design, synthesis and trypanocidal evaluation of novel 1,2,4-triazoles-3-thiones derived from natural piperine.

التفاصيل البيبلوغرافية
العنوان: Design, synthesis and trypanocidal evaluation of novel 1,2,4-triazoles-3-thiones derived from natural piperine.
المؤلفون: Franklim TN; Departamento de Química, Instituto de Ciências Exatas, Universidade Federal Rural do Rio de Janeiro, BR 465, Km 07, CEP: 23.890-000, Seropédica, RJ, Brazil., Freire-de-Lima L, de Nazareth Sá Diniz J, Previato JO, Castro RN, Mendonça-Previato L, de Lima ME
المصدر: Molecules (Basel, Switzerland) [Molecules] 2013 May 29; Vol. 18 (6), pp. 6366-82. Date of Electronic Publication: 2013 May 29.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, c1995-
مواضيع طبية MeSH: Alkaloids/*chemistry , Benzodioxoles/*chemistry , Piperidines/*chemistry , Polyunsaturated Alkamides/*chemistry , Thiones/*chemistry , Triazoles/*chemistry , Trypanocidal Agents/*chemistry , Trypanocidal Agents/*pharmacology, Drug Design ; Inhibitory Concentration 50 ; Molecular Structure ; Parasitic Sensitivity Tests ; Thiones/chemical synthesis ; Triazoles/chemical synthesis ; Trypanocidal Agents/chemical synthesis ; Trypanosoma cruzi/drug effects
مستخلص: The work reported herein describes the synthesis and the assessment of the trypanocidal activity of thirteen new 1,2,4-triazole-3-thiones obtained from natural piperine, the main constituent of the dry fruits of Piper nigrum. It is part of a research program aiming to use abundant and easily available natural products as starting materials for the design and synthesis of new molecules potentially useful as antiparasitic drugs. The variously substituted triazole derivatives were synthesized from the natural amide in four steps with the use of microwave irradiation on overall yields ranging from 32% to 51%. The cyclohexyl substituted derivative showed the best trypanocidal profile on proliferative forms of Trypanosoma cruzi (Y strain), with IC₅₀s = 18.3 and 8.87 mM against epimastigotes and amastigotes, respectively.
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المشرفين على المادة: 0 (Alkaloids)
0 (Benzodioxoles)
0 (Piperidines)
0 (Polyunsaturated Alkamides)
0 (Thiones)
0 (Triazoles)
0 (Trypanocidal Agents)
288-88-0 (1,2,4-triazole)
U71XL721QK (piperine)
تواريخ الأحداث: Date Created: 20130614 Date Completed: 20131224 Latest Revision: 20220309
رمز التحديث: 20240829
مُعرف محوري في PubMed: PMC6270562
DOI: 10.3390/molecules18066366
PMID: 23760033
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules18066366