Article
Environmental Sciences
Antonio Casas-Rodriguez, Rosario Moyano, Veronica Molina-Hernandez, Ana Maria Camean, Angeles Jos
Summary: This study conducted uterotrophic bioassay in ovariectomized rats to investigate the estrogenic properties of MC-LR and CYN. The results showed no changes in uterus growth but potential thyroid disruption effects.
ENVIRONMENTAL RESEARCH
(2023)
Article
Medicine, Legal
Lauren K. Markell, John C. O'Connor, Ruijuan Luo, Joseph P. Klems, Brian C. Sayers, Robert T. Mingoia
Summary: The study compared the effects of dietary and gavage administration routes for positive control chemicals in experimental animals, finding significant changes in organ weights and decreased food consumption in both routes. Additionally, dietary administration may lead to exceeding the maximum tolerated dose.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Shima Nasri, Mohammad Bayat, Khudaidad Kochia
Summary: Compounds containing 1,2,4-triazole scaffolds play a crucial role in drug discovery, this review article summarizes their pharmacological significance and synthesis strategies, encouraging further research to discover new drug candidates.
MOLECULAR DIVERSITY
(2022)
Article
Plant Sciences
Namkyu Lee, Ju Hyeong Lee, Ji Eun Won, Youn Ji Lee, Sun Hee Hyun, Yeong-Deuk Yi, Gyo In, Hee Dong Han, YoungJoo Lee
Summary: According to the study conducted in compliance with OECD guidelines, Korean Red Ginseng and its components do not interfere with the synthesis of estrogen and testosterone. It also does not affect uterine weight or serum estrogen and testosterone levels. It is concluded that ginseng does not have steroidogenic activity and does not disrupt the hypothalamic-pituitary-gonadal axis.
JOURNAL OF GINSENG RESEARCH
(2023)
Article
Environmental Sciences
Anastasiia E. Karnaeva, Aleksey L. Milyushkin, Zoya B. Khesina, Alexey K. Buryak
Summary: This study investigated the exposure of 1,1-dimethylhydrazine in garden cress and zucchini plants using a GC-MS system. The main transformation product of 1,1-dimethylhydrazine in plant tissue was found to be 1-methyl-1H-1,2,4-triazole.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2022)
Article
Toxicology
Marcella Tapias Passoni, Gabriele Palu, Nicole Grechi, Bruna Andreotti da Silva Amaral, Caroline Gomes, Claudia Ruelker, Bennard van Ravenzwaay, Anderson Joel Martino-Andrade
Summary: Through in vivo and in vitro studies, it was found that dipyrone and its metabolites do not exhibit estrogenic or antiestrogenic activity in rats and yeast cells.
TOXICOLOGY LETTERS
(2021)
Review
Chemistry, Medicinal
Jie Li, Junwei Zhang
Summary: This review provides an update on the latest developments of 1,2,3-triazole and 1,2,4-triazole-containing hybrids with anti-S. aureus activity.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Ojasvi Gupta, Tathagata Pradhan, Gita Chawla
Summary: The 1,2,4-triazole ring has gained significant attention in medicinal chemistry due to its diverse range of biological activities. This review summarizes the synthetic approaches and various biological activities of 1,2,4-triazole-based compounds reported in the last decade. It aims to provide valuable information for researchers and medicinal chemists interested in using 1,2,4-triazole as a potential lead for drug design and discovery.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Mao-Tsu Fuh, Ching-Chun Tseng, Sin-Min Li, Shuo-En Tsai, Tsung-Jui Chuang, Chih-Hao Lu, Ya-Chen Yang, Henry J. Tsai, Fung Fuh Wong
Summary: By modifying the skeleton of Sitagliptin and Vildagliptin, four series of 1,2,4-triazole derivatives were successfully synthesized, with beta-amino ester and beta-amino amide compounds showing significant inhibition of DPP-4. These compounds could be promising lead compounds for further development of DPP-4 inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Applied
Kanae Mori, Mieko Kumasaki, Mahito Atobe
Summary: In this study, electrolytic oxidation was used to alter the electronic state of azoles, resulting in changes in their energy release properties. The thermal stability of the products differed from the reactant azoles, with some products becoming more stable while others were destabilized. Gasification rates significantly increased after electrolytic oxidation, indicating the potential of this method for developing new energetic materials.
SCIENCE AND TECHNOLOGY OF ENERGETIC MATERIALS
(2021)
Article
Chemistry, Multidisciplinary
Leila Emami, Sara Sadeghian, Ayyub Mojaddami, Soghra Khabnadideh, Amirhossein Sakhteman, Hossein Sadeghpour, Zeinab Faghih, Masood Fereidoonnezhad, Zahra Rezaei
Summary: In this study, we synthesized nineteen novel 1,2,4-triazole derivatives and confirmed their structures using spectroscopic techniques. The cytotoxic activities of the synthesized compounds were evaluated against human cancer cell lines, and several compounds showed promising cytotoxic activity against the Hela cell line. The safety of these compounds was also assessed, and they exhibited proper selectivity against normal and cancerous cell lines. Additionally, molecular docking studies were conducted to understand the binding modes and mechanisms of these derivatives in the binding pocket of the aromatase enzyme as a potential target.
Article
Chemistry, Medicinal
Ilenia Grieco, Maicol Bissaro, Davide Benedetto Tiz, Daniel Perez, Conception Perez, Ana Martinez, Sara Redenti, Elena Mariotto, Roberta Bortolozzi, Giampietro Viola, Giorgio Cozza, Giampiero Spalluto, Stefano Moro, Stephanie Federico
Summary: Protein kinase CK1 delta plays a crucial role in various neuroinflammatory and neurodegenerative diseases, making it a potential therapeutic target. The development of ATP competitive inhibitors for CK1 delta, such as [1,2,4]triazolo[1,5-c]pyrimidines and [1,2,4]triazolo[1,5-a][1,3,5] triazines, represents a promising approach for future treatments. By identifying key interactions and structures, researchers aim to develop new inhibitors capable of crossing the blood-brain barrier for more effective treatment options.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Analytical
Demet Uzun
Summary: In this study, an electroanalytical method using DPV at 3AT coated GC electrode was developed to determine paracetamol. The electrochemical characterization and electron transfer behavior of the prepared electrode in a specific mixture were confirmed, and the effect of pH on the redox reaction of paracetamol was investigated. The developed electrode showed a detection limit of 0.043 mu M and was successfully applied in pharmaceutical samples.
Article
Chemistry, Medicinal
Fang Yang, Lin Chen, Jin-Mei Lai, Xie-Er Jian, Dong-Xin Lv, Li-Li Yuan, Yu-Xia Liu, Feng-Ting Liang, Xiao-Lan Zheng, Xiong-Li Li, Li-Yuan Wei, Wen-Wei You, Pei-Liang Zhao
Summary: Thirty new 5-amino-1H-1,2,4-triazoles were synthesized and evaluated for antiproliferative activities, with compounds IIa, IIIh, and IIIm showing significant activity. Compound IIIm caused G2/M phase arrest in HeLa cells, while IIa exhibited the most potent tubulin polymerization inhibitory activity. Molecular modeling studies suggest that these compounds have potential for developing novel tubulin polymerization inhibitors with anticancer activity.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Nikolia Lalioti, Alexander Charitos, John Parthenios, Ondrej Malina, Michaela Polaskova, Martin Petr, Vassilis Tangoulis
Summary: A novel experimental protocol based on a reverse micellar method is presented for the synthesis of graphene oxide (GO)-based hybrids with spin crossover nanoparticles (SCO NPs) of the 1D iron(II) coordination polymer.The NP4 and NP5 hybrids synthesized by introducing different quantities of GO into the aqueous phase show improved morphological homogeneity compared to the pristine [Fe(NH(2)trz)(3)](Br-2) NPs. Magnetic observations reveal a two-step hysteresis behavior for NP4 and NP5, with the critical temperatures observed at different sweep rates.