Results 21 to 30 of about 7,095 (171)

Genome‐Guided Discovery of Antimalarial 4‐Amino‐2,4‐Pentadienoate‐Containing Cyclolipodepsipeptides

Angewandte Chemie, Volume 138, Issue 18, 27 April 2026.
Halogenated and glycosylated 4‐amino‐2,4‐pentadienoate‐containing cyclolipodepsipeptides (APD‐CLDs) exhibit potent antiplasmodial activity (IC50 = 25–161 nM) against drug‐sensitive and resistant Plasmodium falciparum strains. ABSTRACT 4‐Amino‐2,4‐pentadienoate‐containing cyclolipodepsipeptides (APD‐CLDs) represent a structurally distinctive family of ...
Hartono Candra, Xue‐Jiao Wang, Ka Diam Go, Li Feng, Miaomiao Cai, Guang‐Lei Ma, Clarissa Widyantoro, Lik Tong Tan, Zbynek Bozdech, Zhe Wang, Zhao‐Xun Liang   +10 more
wiley   +2 more sources

Identification of a Functional CYP2C8 Variant Allele that Alters Splicing, Reduces Protein Expression, and Increases Drug Exposure

Clinical Pharmacology &Therapeutics, Volume 120, Issue 4, Page 966-978, October 2026.
This study investigated genetic determinants of the pharmacokinetics of the CYP2C8 index drugs repaglinide and gemfibrozil, and their interaction in healthy participants. Sequencing data from a study with montelukast revealed a novel functional CYP2C8 allele (rs2071426, CYP2C8*19), predicted to create an intronic splice donor site.
Anssi J. H. Mykkänen, Päivi Hirvensalo, Kathrin Klein, Dorota Kaminska, Markus Grube, Tuija Tapaninen, Johanna I. Kiiski, Mikko Neuvonen, Ville T. Männistö, Jussi Pihlajamäki, Mladen Tzvetkov, Matthias Schwab, Aleksi Tornio, Janne T. Backman, Mikko Niemi   +14 more
wiley   +1 more source

Artesunate + amodiaquine versus artemether-lumefantrine for the treatment of uncomplicated Plasmodium falciparum malaria in the Colombian Pacific region: a noninferiority trial

Revista da Sociedade Brasileira de Medicina Tropical, 2012
INTRODUCTION: In Colombia, there are no published studies for the treatment of uncomplicated Plasmodium falciparum malaria comparing artemisinin combination therapies.
Fernando De la Hoz Restrepo, Alexandra Porras Ramírez, Alejandro Rico Mendoza, Freddy Córdoba, Diana Patricia Rojas   +4 more
doaj   +1 more source

Recent Advances in Microwave and Ultrasound Assisted Synthesis of Quinoline Derivatives as Anticancer Agents

Chemistry &Biodiversity, Volume 23, Issue 9, September 2026.
Green microwave‐ and ultrasound‐assisted synthesis enables the rapid, sustainable preparation of quinoline‐based anticancer agents with improved reaction efficiency, higher yields, and enhanced biological activity. ABSTRACT Quinoline derivatives represent a privileged class of heterocyclic compounds with remarkable structural diversity and broad ...
Rohit Pal, Gurubasavaraja Swamy Purawarga Matada, Ghanshyam Teli, Manjushree B V, Vipin K. Pandey, Shourya Pratap   +5 more
wiley   +1 more source

DDIapp—A Web‐Based Application for Static Drug–Drug Interaction Assessment

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 8, August 2026.
ABSTRACT In this work we describe the development of a web‐based application for static drug–drug interaction (DDI) risk assessment in accordance with the International Council for Harmonization (ICH) M12 guidance. The app was built using the Shiny for Python framework and it employs a modular mathematical modeling structure that incorporates models ...
Hirotaka Watase, Sylvie Klieber, Yorgos M. Psarellis, Nikhil Pillai, Panteleimon D. Mavroudis, Saroj Dhakal   +5 more
wiley   +1 more source

Low-Cost and Portable Biosensor Based on Monitoring Impedance Changes in Aptamer-Functionalized Nanoporous Anodized Aluminum Oxide Membrane

Micromachines
We report a low-cost, portable biosensor composed of an aptamer-functionalized nanoporous anodic aluminum oxide (NAAO) membrane and a commercial microcontroller chip-based impedance reader suitable for electrochemical impedance spectroscopy (EIS)-based ...
Nianyu Jiang, Pranav Shrotriya
doaj   +1 more source

Synthesis and Evaluation of Some New Isoquine Analogues for Antimalarial Activity

E-Journal of Chemistry, 2009
Amodiaquine is a 4-aminoquinoline antimalarial that can cause adverse side effects including hepatic and haematological toxicity. The drug toxicity involves the formation of an electrophilic metabolite, amodiaquine quinoneimine (AQQI), which binds to ...
Chandra Nath Saha, Sanjib Bhattacharya, Dipak Chetia   +2 more
doaj   +1 more source

Amodiaquine resistance in Plasmodium berghei is associated with PbCRT His95Pro mutation, loss of chloroquine, artemisinin and primaquine sensitivity, and high transcript levels of key transporters [version 2; referees: 2 approved, 1 approved with reservations]

Wellcome Open Research, 2018
Background: The human malaria parasite Plasmodium falciparum has evolved drug evasion mechanisms to all available antimalarials. The combination of amodiaquine-artesunate is among the drug of choice for treatment of uncomplicated malaria.
Loise Ndung'u, Benard Langat, Esther Magiri, Joseph Ng'ang'a, Beatrice Irungu, Alexis Nzila, Daniel Kiboi   +6 more
doaj   +1 more source

A Systematic Review of Published Physiologically Based Pharmacokinetic Models for Drug Excretion Into Human Breastmilk: Knowledge Gaps and Opportunities to Optimize Reporting and Modeling Practices

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 8, August 2026.
ABSTRACT Physiologically based pharmacokinetic (PBPK) modeling is increasingly used to predict infant exposure to medications via breast milk. Existing guidance on reporting of PBPK modeling analyses is unstructured and nonbinding to researchers. We evaluated reporting practices and modeling approaches in published PBPK modeling studies.
Joshua Kiptoo, Davies Otieno, Kenta Yoshida, Neel Deferm, Aida Nakayiwa Kawuma, Francis Williams Ojara, Adeniyi Olagunju, Jackson K. Mukonzo, Catriona Waitt   +8 more
wiley   +1 more source

Development of a Brain‐Penetrant Nurr1 Agonist Tool

ChemMedChem, Volume 21, Issue 11, 15 June 2026.
Nuclear receptor‐related 1 (Nurr1) is a ligand‐activated transcription factor with neuroprotective properties, thought to hold therapeutic potential in neurodegeneration. Here, we developed a potent, brain‐penetrant Nurr1 agonist to study the effects of pharmacological Nurr1 activation in the CNS in vivo. The ligand‐sensing transcription factor nuclear
Jan Vietor, Tanja Stiller, Christian Gege, Wael Saeb, Úrsula López‐García, Hella Kohlhof, Daniel Vitt, Daniel Merk   +7 more
wiley   +1 more source