Results 21 to 30 of about 65,300 (300)
Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis
, 2021 A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective N-Boc protection and formaldehyde ...
Jan E., Waters +8 more
core +1 more source
Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats [PDF]
, 2002 The purpose of this study was to modify the biodistribution and pharmacokinetics of tilisolol, a β-blocker, using the palmitoyl prodrug approach. After intravenous administration of tilisolol and O-palmitoyl tilisolol in rats, drug concentrations were ...
Sasaki, Hitoshi +10 more
core +1 more source
Pharmaceuticals, 2014 The N-ethoxycarbonylmorpholine moiety was evaluated as a novel prodrug moiety for carboxylic acid containing drugs represented by diclofenac (1).
Jamal A. Jilani +2 more
doaj +1 more source
A New Classification of Prodrugs: Regulatory Perspectives
Pharmaceuticals, 2009 Many therapeutic agents are manufactured and administered in prodrug forms. In this paper, a new classification system for prodrugs is proposed to provide useful information about where in the body a prodrug is converted to the active drug.
Kuei-Meng Wu
doaj +1 more source
Cyclization-activated Prodrugs [PDF]
Molecules, 2007 Many drugs suffer from an extensive first-pass metabolism leading to druginactivation and/or production of toxic metabolites, which makes them attractive targets forprodrug design. The classical prodrug approach, which involves enzyme-sensitive covalentlinkage between the parent drug and a carrier moiety, is a well established strategy toovercome ...
Paula Gomes, Nuno Vale, Rui Moreira
openaire +5 more sources
Reduction-Responsive Stearyl Alcohol-Cabazitaxel Prodrug Nanoassemblies for Cancer Chemotherapy
Pharmaceutics, 2023 Cabazitaxel (CTX) has distinct therapeutic merits for advanced and metastatic cancer. However, the present clinical formulation (Jevtana®) has several defects, especially for undesirable tumor-targeting and serious side effects, greatly limiting the ...
Yuting Liu +6 more
doaj +1 more source
Pharmaceutics, 2020 Self-assembled prodrugs (SAPDs), which combine prodrug strategy and the merits of self-assembly, not only represent an appealing type of therapeutics, enabling the spontaneous organization of supramolecular nanocomposites with defined structures in ...
Jingyan Gao +7 more
doaj +1 more source
Antibody-based Imaging of Bioreductive Prodrug Release in Hypoxia
, 2023 Regions of hypoxia occur in most tumors and predict for poor patient prognosis. Hypoxia-activated prodrugs provide an ideal strategy to target the aggressive, hypoxic fraction of a tumor while protecting the normal tissue from toxicity.
Antoine, Wallabregue +6 more
core +1 more source
Iraqi Journal of Pharmaceutical Sciences, 2017 On the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in ...
Yasser F. Mustafa, Nohad A. Al-Omari
doaj +3 more sources
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators
, 2020 Neurodegenerative diseases lack a breadth of treatment options due, in part, to the known difficulties associated with a drug’s passage across the blood-brain barrier.
Skylar, Ferrara, Thomas, Scanlan
core +1 more source