Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi
نویسندگان
چکیده
منابع مشابه
2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.
The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3-thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors and showed excellent inhibition on the trypomastigote form of the parasite, and the resulting structure-activity relationships are discussed. T...
متن کاملDesign, Synthesis, Antimicrobial Evaluation and Molecular Modeling Study of 1,2,4-Triazole-Based 4-Thiazolidinones.
A series of 3-(2H-1,2,4-triazol-5-yl)-1,3-thiazolidin-4-one derivatives (7c-l) was designed and synthesized. Their structures have been elucidated based on analytical and spectral data. They were evaluated for their antibacterial and antifungal activities. Compound 7h showed the highest activity against all tested strains, except P. vulgaris, with MIC 8 μg/mL and 4 μg/mL against S. aureus and C...
متن کاملStructural organization of Trypanosoma cruzi.
Since the initial description of Trypanosoma cruzi by Carlos Chagas in 1909, several research groups have used different microscopic techniques to obtain detailed information about the various developmental stages found in the life cycle of this intracellular parasite. This review describes the present knowledge on the organization of the most important structures and organelles found in the pr...
متن کاملSynthesis of New Pyridine Based 4-Thiazolidinones Incorporated Benzothiazoles and Evaluation of Their Antimicrobial Activity
Substituted Schiff bases (hydrazones) 5a-j have been prepared from the starting material 2-chloro pyridine-3-carboxylic acid 1 by a sequence of reactions like reaction with 2-amino-6-nitro benzothiazole (Ullamann condensation), thionyl chloride, hydrazine hydrate and different aromatic aldehydes. On cyclocondensation of 5a-j with thioglycolic acid in dry 1,4-dioxane furnished desired compounds ...
متن کاملDesign, synthesis, and biological evaluation of new growth inhibitors of Trypanosoma cruzi (epimastigotes).
As a continuation of our project aimed at the search for new chemotherapeutic agents against Chagas' disease, several drugs structurally related to the insect growth regulator Fenoxycarb and the naturally occurring juvenile hormone of insects were designed, synthesized, and evaluated as antiproliferative agents against the parasite responsible of this disease. Isoprenoid derivatives (compounds ...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2015
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2015.10.048