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Related Concept Videos

Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
Drug Metabolism: Phase I Reactions01:17

Drug Metabolism: Phase I Reactions

A phase I reaction is a biochemical process that introduces a functionally reactive polar group to a substance. This transformation predominantly occurs in the liver, facilitated by the cytochrome P450 system of hemoproteins situated in the lipophilic endoplasmic reticulum of cells. The metabolite generated through this process can have varying polarities. If it is sufficiently polar, it can be easily excreted in the urine due to its water compatibility. However, if the metabolite is nonpolar,...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
Cationic Chain-Growth Polymerization: Mechanism00:57

Cationic Chain-Growth Polymerization: Mechanism

The cationic polymerization mechanism consists of three steps: initiation, propagation, and termination. In the initiation step of the polymerization process, the π bond of a monomer gets protonated by the Lewis acid catalyst, which is formed from boron trifluoride and water. The protonation of the π bond generates a carbocation stabilized by the electron‐donating group. In the propagation step, the π bond of the second monomer acts as a nucleophile and attacks the generated carbocation,...
Cycloaddition Reactions: MO Requirements for Photochemical Activation01:12

Cycloaddition Reactions: MO Requirements for Photochemical Activation

Some cycloaddition reactions are activated by heat, while others are initiated by light. For example, a [2 + 2] cycloaddition between two ethylene molecules occurs only in the presence of light. It is photochemically allowed but thermally forbidden.

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Related Experiment Video

Updated: Jul 9, 2026

Activation and Conjugation of Soluble Polysaccharides using 1-Cyano-4-Dimethylaminopyridine Tetrafluoroborate (CDAP)
07:20

Activation and Conjugation of Soluble Polysaccharides using 1-Cyano-4-Dimethylaminopyridine Tetrafluoroborate (CDAP)

Published on: June 14, 2021

Cyclization-activated prodrugs.

Paula Gomes1, Nuno Vale, Rui Moreira

  • 1Centro de Investigação em Química da Universidade do Porto, Departamento de Química, Faculdade de Ciências, Universidade do Porto, Porto, Portugal. pgomes@fc.up.pt

Molecules (Basel, Switzerland)
|December 11, 2007
PubMed
Summary
This summary is machine-generated.

Cyclization-activated prodrugs offer a non-enzymatic approach to drug delivery, bypassing metabolism variability. This strategy enhances drug bioavailability and reduces toxicity by utilizing intramolecular cyclization for parent drug release.

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Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
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Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

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Area of Science:

  • Medicinal Chemistry
  • Drug Delivery Systems
  • Pharmacology

Background:

  • Many drugs undergo extensive first-pass metabolism, leading to inactivation or toxic byproducts.
  • Classical prodrugs use enzyme-sensitive linkages, but enzymatic variability can affect drug release.
  • Non-enzymatic prodrug activation offers a stable alternative to overcome these limitations.

Purpose of the Study:

  • To provide an overview of research on cyclization-activated prodrugs over the last two decades.
  • To highlight the development and application of prodrugs utilizing intramolecular activation pathways.
  • To discuss the advantages of non-enzymatic prodrug activation in overcoming drug bioavailability and toxicity issues.

Main Methods:

  • Review of scientific literature on cyclization-activated prodrugs from the past 20 years.
  • Analysis of strategies involving intramolecular cyclization for prodrug activation.
  • Examination of prodrugs designed for various therapeutic areas, including analgesics and anti-HIV agents.

Main Results:

  • Cyclization-activated prodrugs have matured as a significant strategy in prodrug design since the late 1990s.
  • Intramolecular cyclization enables non-enzymatic drug release, independent of enzymatic activity.
  • These prodrugs are employed in diverse therapeutic applications, demonstrating broad utility.

Conclusions:

  • Cyclization-activated prodrugs represent a valuable approach to enhance drug efficacy and safety.
  • Non-enzymatic activation pathways provide predictable drug release kinetics.
  • Continued research in this area holds promise for developing improved therapeutics.