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Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Photoluminescence offers a wide range of applications due to its inherent sensitivity and selectivity. This technique allows for both direct and indirect analyses of the analyte. Direct quantitative analysis is possible when the analyte exhibits a favorable quantum yield for fluorescence or phosphorescence. However, an indirect analysis may be feasible if the analyte is not fluorescent or phosphorescent, or if the quantum yield is unfavorable. Indirect methods include reacting the analyte with...
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Fluorescence in situ hybridization, or FISH, was developed in the early 1980s and has quickly become one of the most widely used techniques in cytogenetics. Labeled probes are used to bind complementary DNA or RNA sequences on a chromosome or in a region within a cell. Earlier, the probes could only be obtained by cloning or reverse transcription of a DNA template. Currently, the probe oligonucleotides can be synthesized synthetically. Additionally, with the advancement of optical techniques,...
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Fluorination methods for drug discovery and development.

Paul Richardson1

  • 1a Oncology Medicinal Chemistry , Pfizer-La Jolla , La Jolla , CA , USA.

Expert Opinion on Drug Discovery
|August 23, 2016
PubMed
Summary
This summary is machine-generated.

Fluorine incorporation in drugs has surged, driving innovation in synthetic organic chemistry. New, milder methods now enable precise fluorination for drug discovery and development.

Keywords:
FluorinePET (positron emission tomography)chemistry under microfluidic conditionsdeoxyfluorinationdrug discoveryfluorine-18metal-mediated fluorination

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Area of Science:

  • Organic Chemistry
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Fluorine's role in modulating bioactive molecule properties is critical.
  • The percentage of approved drugs containing fluorine increased from 2% in 1970 to 25% by 2011.
  • Synthetic methods for fluorination have advanced from hazardous reagents to milder, precise techniques.

Purpose of the Study:

  • To review the importance of fluorinated compounds in drug discovery.
  • To provide an overview of synthetic strategies for accessing fluorinated compounds.
  • To highlight advancements in fluorination methodologies for drug development.

Main Methods:

  • Review of literature on synthetic strategies for fluorination.
  • Overview of deoxyfluorination reagents.
  • Discussion of metal-mediated fluorination techniques.

Main Results:

  • Significant progress in developing safe and precise regioselective fluorination reagents.
  • Emergence of practical metal-mediated techniques for efficient late-stage fluorination.
  • Investigation into extending fluorination methods for Positron Emission Tomography (PET) labeling.

Conclusions:

  • Developing novel reagents for safe and precise fluorination of biologically relevant compounds is an ongoing challenge.
  • New deoxyfluorination reagents and metal-mediated techniques facilitate efficient late-stage fluorination of drug-like compounds.
  • Further research is exploring the application of these methods for PET imaging.