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Related Concept Videos

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
Acid Strength and Molecular Structure03:05

Acid Strength and Molecular Structure

Binary Acids and Bases
In the absence of any leveling effect, the acid strength of binary compounds of hydrogen with nonmetals (A) increases as the H-A bond strength decreases down a group in the periodic table. For group 17, the order of increasing acidity is HF < HCl < HBr < HI. Likewise, for group 16, the order of increasing acid strength is H2O < H2S < H2Se < H2Te. Across a row in the periodic table, the acid strength of binary hydrogen compounds increases with increasing...
Structures of Carboxylic Acid Derivatives01:28

Structures of Carboxylic Acid Derivatives

Structure of Carboxylic Acid Derivatives
Carboxylic acid derivatives contain an acyl group attached to a heteroatom such as chlorine, oxygen, or nitrogen. The carbonyl carbon and oxygen are both sp2-hybridized with an unhybridized p orbital.
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Related Experiment Video

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Analyzing Protein Dynamics Using Hydrogen Exchange Mass Spectrometry
11:37

Analyzing Protein Dynamics Using Hydrogen Exchange Mass Spectrometry

Published on: November 29, 2013

Hydroxamates: relationships between structure and plasma stability.

Marion Flipo1, Julie Charton, Akila Hocine

  • 1INSERM U761 Biostructures and Drug Discovery, Univ Lille Nord de France, Lille F-59006, France.

Journal of Medicinal Chemistry
|October 14, 2009
PubMed
Summary

This study introduces structural rules for predicting and improving hydroxamate plasma stability, crucial for drug development. Understanding these rules aids medicinal chemists in designing more stable drug candidates.

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Analyzing Protein Dynamics Using Hydrogen Exchange Mass Spectrometry
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Mass Spectrometric Approaches to Study Protein Structure and Interactions in Lyophilized Powders
11:14

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Published on: April 14, 2015

Area of Science:

  • Medicinal Chemistry
  • Chemical Biology
  • Pharmacology

Background:

  • Hydroxamates are vital in chemical biology and as drug leads, with some showing high activity against metalloproteases.
  • Despite potential, few hydroxamates reach the market due to issues like poor stability, toxicity, and lack of selectivity.
  • Vorinostat, an HDAC inhibitor, is one of the few approved hydroxamate drugs.

Purpose of the Study:

  • To conduct the first preliminary study on the relationship between hydroxamate structure and plasma stability.
  • To provide medicinal chemists with insights into improving hydroxamate stability during the preclinical drug development phase.

Main Methods:

  • Analysis of hydroxamate chemical structures.
  • Evaluation of hydroxamate stability in plasma.
  • Identification of structure-stability relationships.

Main Results:

  • Establishment of preliminary structure-plasma stability rules for hydroxamates.
  • Identification of key structural features influencing hydroxamate stability in biological fluids.

Conclusions:

  • Hydroxamates' plasma stability can be predicted and potentially improved by understanding specific structural features.
  • The developed rules offer a valuable tool for medicinal chemists to enhance the preclinical drug design process for hydroxamate-based therapeutics.