Results 151 to 160 of about 127,252 (263)

Isoniazid‐Dihydropyrimidinone Molecular Hybrids: Design, Synthesis, Antitubercular Activity, and Cytotoxicity Investigations with Computational Validation

open access: yesChemMedChem, EarlyView.
Antitubercular evaluation of a novel library of isoniazid‐dihydropyrimidinone molecular hybrids (8a–8n) discloses a potent compound with MIC = 0.39μg mL−1 against M. tuberculosis mc26230. Cytotoxicity, stability, and in silico studies, including molecular docking and ADME/T (absorption, distribution, metabolism, excretion, and toxicity) analysis ...
Gobind Kumar   +10 more
wiley   +1 more source

Systematic Review on 1,2,3‐Oxadiazoles, 1,2,4‐Oxadiazoles, and 1,2,5‐Oxadiazoles in the Antimycobacterial Drug Discovery

open access: yesChemMedChem, EarlyView.
The review focuses on relationships of oxadiazole derivative structures and their antimycobacterial activity including target structures in mycobacteria, in vitro or in vivo pharmacokinetic parameters, and toxicity. Apart from direct antimycobacterial activity, some 1,2,4‐oxadiazole derivatives can potentiate the antimycobacterial effect of ethionamide
Marta Kučerová‐Chlupáčová
wiley   +1 more source

Influence of Renal Function on Phosphoramide Mustard Exposure: A Nonlinear Mixed‐Effects Analysis

open access: yesThe Journal of Clinical Pharmacology, Volume 63, Issue 1, Page 135-142, January 2023., 2023
Abstract Phosphoramide mustard (PM) is the final cytotoxic metabolite formed from the parent compound cyclophosphamide through a complex metabolic pathway, primarily through hepatic metabolism. Little is known about the effect of renal elimination on the disposition of PM.
Mutaz M. Jaber   +5 more
wiley   +1 more source

Hybrid Molecules as Efficient Drugs against Multidrug‐Resistant Malaria Parasites

open access: yesChemMedChem, EarlyView.
Among hybrid molecules currently developed as antimalarial drug candidates, emoquine‐1 exhibits high activity against all the multidrug‐resistant Plasmodium strains tested up to now, including artemisinin‐resistant quiescent parasites, critical parameters for promising antimalarial drugs. It is also curative in mouse malaria.
Anne Robert   +6 more
wiley   +1 more source

Evaluation of the Pharmacokinetic Drug Interaction of Capmatinib With Itraconazole and Rifampicin and Potential Impact on Renal Transporters in Healthy Subjects

open access: yesThe Journal of Clinical Pharmacology, Volume 63, Issue 2, Page 228-238, February 2023., 2023
Abstract Capmatinib is a highly specific, potent, and selective mesenchymal–epithelial transition factor inhibitor predominantly eliminated by cytochrome P450 (CYP) 3A4 and aldehyde oxidase. Here, we investigated the effects of a strong CYP3A inhibitor (itraconazole) and a strong CYP3A inducer (rifampicin) on single‐dose pharmacokinetics of capmatinib.
Xiaoming Cui   +6 more
wiley   +1 more source

Exploring Bonding in Bioinorganic Chemistry: Ab Initio Valence Bond Calculations of Iron(II)‐CO and Iron(IV)‐Oxo Units in Cytochrome P450 under Oriented External Electric Fields

open access: yesChemistry–Methods, EarlyView.
Ab initio valence bond calculations under oriented electric fields along the bond axis of Fe(II)‐CO and Fe(IV)‐oxo units in cytochrome P450 enzymes highlight their effectiveness in probing complex bonding characteristics and ligand effects in bioinorganic systems.
Enhua Zhang, Hajime Hirao
wiley   +1 more source

Maribavir Pharmacokinetics and Safety in Participants With Moderate Hepatic Impairment: A Phase 1, Open‐Label, Single‐Dose, Parallel Group Study

open access: yesThe Journal of Clinical Pharmacology, Volume 63, Issue 2, Page 250-258, February 2023., 2023
Abstract Maribavir, an orally bioavailable antiviral, has shown superior activity against posttransplant cytomegalovirus infection compared with conventional antivirals. It is primarily metabolized in the liver. This open‐label, single‐center study evaluated the effect of hepatic impairment on the pharmacokinetics of maribavir in nontransplant ...
Ivy Song   +3 more
wiley   +1 more source

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