Coccidiosis is one of the most common parasitic diseases affecting many species of domestic animals. This disease has a major economic significance and the search for new compounds having anticoccidial activity is of great importance. In this article, different levels of protection from coccidian infection by Eimeria stiedae were developed in rabbits by treatment with compounds incorporating the skeleton of thiourea. These compounds include 4,5-diphenylimidazole-2-thione (1), 4,5-Diphenyl-1,2,4-triazole-3-thiol (2) and 5-(2-Hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thiol (3) compared to the anticoccidial drug toltrazuril as a reference compound. Compounds 1-3 inhibit coccidiosis-induced activity of α-glucosidase. The protection from coccidial infection by compound 1 was higher than that shown for compounds 2 and 3. These data suggest that diazole and triazole thione derivatives have a mimetic effect for anticoccidial drugs through their inhibition of glycosidases.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Novel Antimicrobial and Antitumor Agents Bearing Pyridine-1,2,4-triazole-3-thione-hydrazone Scaffold: Synthesis, Biological Evaluation, and Molecular Docking Investigation.
Biomolecules
November 2024
Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų pl. 19, 50254 Kaunas, Lithuania.
A series of target 4-substituted-5-(2-(pyridine-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thiones and their chloro analogs - were synthesized in a reaction of the selected aldehydes with the corresponding 4-amino-1,2,4-triazole-3-thiones and , which were obtained from 3-(pyridin-2-ylamino)propanoic acid () or 3-((5-chloropyridin-2-yl)amino)propanoic acid (), respectively, with thioacetohydrazide. The antibacterial and antifungal activities of the synthesized hydrazones were screened against the bacteria , , and and the fungi and by agar diffusion and serial dilution methods. 4-Amino-5-(2-((5-chloropyridin-2-yl)amino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () and 4-(benzylideneamino)-5-(2-(pyridin-2-ylamino)ethyl)-2,4-dihydro-3-1,2,4-triazole-3-thione () were identified as exceptionally active (MIC 0.
View Article and Find Full Text PDFTheoretical insights into fluorescent properties and ESIPT behavior of novel flavone-based fluorophore and its thiol and thione derivatives.
Spectrochim Acta A Mol Biomol Spectrosc
December 2024
Department of Chemistry and Material Science, College of Science, Nanjing Forestry University, Nanjing 210037, People's Republic of China. Electronic address:
For the typical ESIPT process, the proton transfer process is often completed via the intramolecular hydrogen bond (IHB) with oxygen or nitrogen as proton donor or proton acceptor. In recent years, the ESIPT process for sulfur-containing hydrogen bonds has received more and more attention, but it has been rarely reported. We systematically studied the ESIPT processes and photophysical properties of 2-(benzothiophene-2-yl)-3-hydroxy-4H-chromen-4-one (BTOH), 2-(benzothiophene-2-yl)-3-mercapto-4H-chromen-4-one (BTSH) and 2-(benzothiophen-2-yl)-3-hydroxy-4H-chromene-4-thione (BTS) at the HISSbPBE/6-31+G(d,p) and TD-HISSbPBE/6-31+G(d,p) computational level.
View Article and Find Full Text PDFSulfur and Oxygen Transfer Reactions with Simultaneous NHC-Coordination from Cyclic Thioureas and Ureas to a Stable Silylene.
Chemistry
December 2024
Department of Chemistry, Graduate School of Science, Tohoku University, Aoba-ku, Sendai, 980-8578, Japan.
Reactions of cyclic thioureas (1,3,4,5-tetramethylimidazol-2-thione and 1,3-dimethylimidazolidin-2-thione) and ureas (1,3,4,5-tetramethylimidazol-2-one and 1,3-dimethylimidazolidin-2-one) with an isolable dialkylsilylene were examined. In these reactions, cyclic thioureas served as sulfur and NHC (N-heterocyclic carbene) sources, and the corresponding silanethione and NHC-derived products formed via silanethione-NHC complexes. Reactions of cyclic ureas with the silylene afforded a new NHC and an isolable azomethine ylide.
View Article and Find Full Text PDFEffects of Oltipraz on the Glycolipid Metabolism and the Nrf2/HO-1 Pathway in Type 2 Diabetic Mice.
Drug Des Devel Ther
December 2024
Department of Endocrinology and Metabolism of the Second Affiliated Hospital, Jiangxi Medical College, Nanchang University, Nanchang, Jiangxi, 330031, People's Republic of China.
Purpose: Oltipraz has various applications, including for treating cancer, liver fibrosis, and cirrhosis. However, its role in regulating metabolic processes, inflammation, oxidative stress, and insulin resistance in STZ-induced T2DM remains unclear. Hence, a comprehensive understanding of how oltipraz ameliorates diabetes, particularly inflammation and oxidative stress, is imperative.
View Article and Find Full Text PDFEfficient synthesis of promising antidiabetic triazinoindole analogues a solvent-free method: investigating the reaction of 1,3-diketones and 2,5-dihydro-3-[1,2,4]triazino[5,6-]indole-3-thione.
Org Biomol Chem
December 2024
Department of Chemistry, Kurukshetra University, Kurukshetra-136119, Haryana, India.
Article Synopsis
- Diabetes is a major global health issue, leading researchers to explore new management strategies using α-amylase inhibitors.
- A series of novel compounds, specifically 3-methyl-2-aroylthiazolo derivatives, were synthesized and tested for their effectiveness in inhibiting the α-amylase enzyme, showing moderate to excellent activity levels.
- Notably, compounds with halogen groups demonstrated stronger inhibition than the standard drug Acarbose, with specific derivatives showing the best results and supporting theoretical findings through molecular docking studies.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!