Results 131 to 140 of about 15,779 (274)

Xanthohumol Pyrazole Derivative Improves Diet-Induced Obesity and Induces Energy Expenditure in High-Fat Diet-Fed Mice. [PDF]

ACS Pharmacol Transl Sci, 2021
Paraiso IL, Mattio LM, Alcázar Magaña A, Choi J, Plagmann LS, Redick MA, Miranda CL, Maier CS, Dallavalle S, Kioussi C, Blakemore PR, Stevens JF.   +11 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

5‐HT2A receptor agonism by tert‐leucinamide and valinamide synthetic cannabinoids: In vitro and in vivo evidence

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose New synthetic cannabinoid receptor agonists (SCRAs) are associated with severe adverse effects, including unexpected psychiatric symptoms. These compounds are mainly active through their potent agonism on the cannabinoid receptors CB1 and CB2.
Giorgia Corli, Deborah Rudin, Dino Luethi, Matthias E. Liechti, Sabrine Bilel, Matteo Marti, Henrik Green, Manuela Carla Monti, Caitlyn Norman   +8 more
wiley   +1 more source

The Effect of Nano-Pyrazole Derivative of Thiosemicarbazone Magnetite on BRCA1, p53 and Bcl-2 Gene Expression in MCF-7 Breast Cancer Cell Line

Journal of Ardabil University of Medical Sciences, 2019
Background & objectives: Breast cancer is one of the most important causes of cancer deaths especially in developing countries. However, some synthetic compounds such as thiosemicarbazone and its metal derivatives can play a very significant role in ...
Mohammad Reza Izadpanah, Ali Saleh zadeh, Mohammad Zaiefi zadeh, Mohammad Nik pasand   +3 more
doaj  

Plasma Pharmacokinetic Profile of Fipronil 1% Pour‐On in Cattle: Photodegradation and the Sustained Systemic Persistence of Fipronil Sulfone

Journal of Veterinary Pharmacology and Therapeutics, EarlyView.
ABSTRACT This study characterized the long‐term pharmacokinetic profile of a 1% fipronil pour‐on formulation in Nellore bulls under field conditions. Seventeen animals received a single topical dose (1 mg/kg), and plasma concentrations of fipronil and its metabolites (sulfone and desulfinyl) were monitored for 175 days using LC–MS/MS.
Stefani Maria Ferreira, Leonila Ester Reinert Raspantini, Giselle Kindlein, Fabiano Barreto, Caroline Andrade Tomaszewski, Tamara dos Santos Castilhos, Daniel Rodrigo Hillesheim, Silvana Lima Górniak, André Tadeu Gotardo   +8 more
wiley   +1 more source

An Exploration of Vinamidinium Salts for Frame‐Shifted Synthesis

Israel Journal of Chemistry, Volume 66, Issue 4, July 2026.
Oligoheterocycles are widely used in drug discovery and materials science, where they serve as attractive alternatives to peptide fragments. There is strong interest in understanding the structural correspondence between heterocycles and amino acid motifs to recapitulate key binding elements while improving metabolic stability.
Morgan J. Cordell, Chelsey Brien, Thomas Sidarta Setio, Andrei K. Yudin   +3 more
wiley   +1 more source

Synthesis and Anti-Trypanosoma cruzi Activity of New Pyrazole-Thiadiazole Scaffolds

Molecules
Chagas disease, a silent but widespread disease that mainly affects a socioeconomically vulnerable population, lacks innovative safe drug therapy. The available drugs, benznidazole and nifurtimox, are more than fifty years old, have limited efficacy, and
Thamyris Perez de Souza, Lorraine Martins Rocha Orlando, Leonardo da Silva Lara, Vitoria Barbosa Paes, Lucas Penha Dutra, Mauricio Silva dos Santos, Mirian Claudia de Souza Pereira   +6 more
doaj   +1 more source

Design and Synthesis of Pyrimidino[4,5‐d]Pyrimidine‐Based Compounds as Potent B‐RAF V600E Inhibitors

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
Novel pyrimido[4,5‐d]pyrimidine‐based inhibitors selectively target B‐RAF V600E with nanomolar affinity and adopt distinct type‐II binding modes. Complementary cellular profiling reveals highly active analogs, underscoring the versatility of this chemotype and establishing it as a promising scaffold for the development of next‐generation kinase ...
Eleftheria A. Georgiou, Kalliopi Christopoulou, Amalia D. Kalampaliki, Aikaterini F. Giannopoulou, Eleftheria Chatziorfanou, Vivi Bafiti, Andreas Krämer, Athanasios Papakyriakou, Dimitrios J. Stravopodis, Stefan Knapp, Ioannis K. Kostakis   +10 more
wiley   +1 more source

DNA‐Binding Properties of Iridium(III) Complexes Encompassing Design, Function and Biophysical Assessments

ChemPhysChem, Volume 27, Issue 11, 15 June 2026.
This review describes the biophysical techniques used to investigate DNA‐binding phenomena and the progress made so far in the application of iridium(III) complexes for this purpose. Ir(III) complexes offer myriad opportunities in the design and study of DNA‐binding agents and discussed examples are contextualised with complementary studies in ...
Ibrahim S. Alkhaibari, Niklaas J. Buurma, Simon J. A. Pope   +2 more
wiley   +1 more source

Synthesis of Heterocyclic Compounds Derived from 2-Mercapto Quinoline

Ibn Al-Haitham Journal for Pure and Applied Sciences, 2017
2-Mercapto quinoline was used as precursor for synthesis of new heterocyclic derivatives of quinoline nucleus such as pyrazole (3), pyrazolone (4), 1,3,4-oxadiazole (5) and 1,2,4-triazole (8). New Schiff bases (9a-e) were obtained from the reaction of
A. H. Sharba, H. A. Hassan, D. F. Hassan
doaj