Results 51 to 60 of about 26,232 (247)

Exploration of Novel Biomarkers for Neurodegenerative Diseases Using Proteomic Analysis and Ligand-Binding Assays

Biomedicines
Background/Objectives: Neurodegenerative diseases are a major cause of morbidity and mortality worldwide, and their public health burden continues to increase.
Annalena Kenzelmann, Christina Boch, Ronny Schmidt, Mario Richter, Michael Schulz   +4 more
doaj   +1 more source

Synthesis, Antiproliferative Activity and In Silico Studies of Chalcones Derived From 4-(Imidazole-1-yl)Acetophenone

Journal of the Turkish Chemical Society, Section A: Chemistry, 2023
In this study, the synthesis of chalcone compounds (1-11) derived from 4-(imidazol-1-yl)acetophenone and the structure determination of these compounds by various spectroscopic methods were carried out.
Bedriye Seda KURŞUN AKTAR, Abdulraheem Mustafa ALKARABASH , Ayşe ŞAHİN YAĞLIOĞLU, Emine Elçin ORUÇ-EMRE   +3 more
doaj   +1 more source

Structure-Based Virtual Screening of Pseudomonas aeruginosa LpxA Inhibitors using Pharmacophore-Based Approach

Biomolecules, 2020
Multidrug resistance in Pseudomonas aeruginosa is a noticeable and ongoing major obstacle for inhibitor design. In P. aeruginosa, uridine diphosphate N-acetylglucosamine (UDP-GlcNAc) acetyltransferase (PaLpxA) is an essential enzyme of lipid A ...
Baki Vijaya Bhaskar, Tirumalasetty Muni Chandra Babu, Aluru Rammohan, Gui Yu Zheng, Grigory V. Zyryanov, Wei Gu   +5 more
doaj   +1 more source

Mechanistically transparent models for predicting aqueous solubility of rigid, slightly flexible, and very flexible drugs (MW<2000) Accuracy near that of random forest regression

ADMET and DMPK, 2023
Yalkowsky’s General Solubility Equation (GSE), with its three fixed constants, is popular and easy to apply, but is not very accurate for polar, zwitterionic, or flexible molecules. This review examines the findings of a series of studies, where we have
Alex Avdeef
doaj   +1 more source

Acetylpromazine maleate revisited: deep-dive equilibrium analysis revealing drug salt acting as a pH- and pS-stat counter-titrant

AAPS Open
Acetylpromazine is a phenothiazine derivative that is prone to form sub-micellar aggregates and micelles in water above pH 5. This study revisits the determination of the equilibrium constants (Avdeef et al., ADMET DMPK 4:117-178, 2016) describing the ...
Alex Avdeef
doaj   +1 more source

Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
In this study, newly synthesised compounds 6, 8, 10 and other compounds (1–5, 7 and 9) and their inhibitory properties against the human isoforms hCA I and hCA II were reported for the first time.
Yazgı Dizdaroglu, Canan Albay, Tayfun Arslan, Abdulilah Ece, Emir A. Turkoglu, Asiye Efe, Murat Senturk, Claudiu T. Supuran, Deniz Ekinci   +8 more
doaj   +1 more source

Use of Clotrimazole in Finfish Aquaculture: Mechanistic Insights, Limitations, and Future Directions for Antifungal Therapy

Animal Research and One Health, EarlyView.
This review critically evaluates clotrimazole as a potential antifungal for finfish aquaculture, highlighting strong mechanistic and in vitro efficacy against aquatic mycoses alongside major gaps in in vivo evidence, toxicokinetics, residue safety, and environmental risk, outlining priorities for responsible therapeutic development and regulatory ...
Arya Sen, Debashri Mondal, Thangapalam Jawahar Abraham   +2 more
wiley   +1 more source

Setting up mother–infant pair lactation studies with biobanking for research according to regulatory requirements

British Journal of Clinical Pharmacology, EarlyView.
Within the ConcePTION project we set out to design two mother–infant pair studies collecting breast milk and plasma from the mother and plasma from the infant (for metformin and prednisolone) in order to demonstrate the premises and conditions for investigating potential drug transfer in association with breastfeeding.
Mats Hansson, Ida Björkgren, Jenny Svedenkrans, Helena Backman, Jarl Hellman, Linda Englund‐Ögge, Mikaela Magnusson, Inger Lindström, Andrea Wutte, Erica Sundell, Pawel Baranczewski, Laura Shaughnessy   +11 more
wiley   +1 more source

Extrapolation and pharmacokinetic protocol design optimization for ceftriaxone as an exemplar for the development of antibiotics for children

British Journal of Clinical Pharmacology, EarlyView.
Aim Ceftriaxone is a cephalosporin commonly used for the treatment of acute, severe infections; however, there are conflicting data on its disposition properties in children, making it a suitable case study for the evaluation of the appropriateness of extrapolation approaches based on exposure matching principles for paediatric patients and exploring ...
Daniel Valente Neves, Umberto Villani, Salvatore D'Agate, Sean Oosterholt, Ricardo de Carvalho Cavalli, Fabio Carmona, Vera Lucia Lanchote, Oscar Della Pasqua   +7 more
wiley   +1 more source

Hypertension in obesity: A focus on individualized pharmacotherapy and the role of body composition, on behalf of the European Society of Hypertension Working Group on Diabetes and Metabolic Risk Factors and Working Group on Lifestyle, Cardiovascular Pharmacotherapy and Adherence

British Journal of Clinical Pharmacology, EarlyView.
Hypertension in obesity represents a major global health challenge, closely linked to the global epidemics of obesity, type 2 diabetes and metabolic dysfunction. Excess adiposity contributes to elevated blood pressure through multiple, interrelated mechanisms, including activation of the renin–angiotensin–aldosterone system, sympathetic nervous system ...
Christina Antza, Andrej Belancic, Jens Jordan, Alberto Esteban, Anna Oliveras, Ryan McNally, Panagiota Anyfanti, Jorie Versmissen, María S. Fernández‐Alfonso, Vasilios Kotsis, Thomas Weber, Alexandre Persu, Reinhold Kreutz   +12 more
wiley   +1 more source