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Related Concept Videos

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids01:19

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

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Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
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Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
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Drug Metabolism: Phase II Reactions01:14

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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...
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Sulfides are the sulfur analog of ethers, just as thiols are the sulfur analog of alcohol. Like ethers, sulfides also consist of two hydrocarbon groups bonded to the central sulfur atom. Depending upon the type of groups present, sulfides can be symmetrical or asymmetrical. Symmetrical sulfides can be prepared via an SN2 reaction between 2 equivalents of an alkyl halide and one equivalent of sodium sulfide.
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Enzyme Inhibition01:30

Enzyme Inhibition

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Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.
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Amines to Sulfonamides: The Hinsberg Test01:23

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The Hinsberg test is a method to identify primary, secondary and tertiary amines, named after its pioneer, Oscar Hinsberg. Here, amines are treated with benzenesulfonyl chloride, also known as the Hinsberg reagent, in the presence of an excess of aqueous base, followed by acidification. Based on the nature of the amines, different changes are observed.
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Updated: Nov 27, 2025

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SARS-CoV-2 Inhibition by Sulfonated Compounds.

Matteo Gasbarri1, Philip V'kovski2,3, Giulia Torriani4

  • 1Institute of Materials, Ecole Polytechnique Fédérale de Lausanne, 1015 Lausanne, Switzerland.

Microorganisms
|December 3, 2020
PubMed
Summary
This summary is machine-generated.

Sulfated molecules inhibit SARS-CoV-2 entry by targeting heparan sulfates. Unlike other viruses, the inhibition of SARS-CoV-2 by these compounds is reversible, offering a unique therapeutic avenue.

Keywords:
SARS-CoV-2antiviralattachment inhibitorheparan sulfates

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Area of Science:

  • Virology
  • Biochemistry
  • Drug Discovery

Background:

  • Severe acute respiratory syndrome-related coronavirus 2 (SARS-CoV-2) utilizes angiotensin converting enzyme 2 (ACE2) for cell entry.
  • Emerging evidence suggests SARS-CoV-2 spike protein also interacts with heparan sulfates as attachment receptors.
  • Previous studies show reduced SARS-CoV-2 binding upon heparin treatment or heparinase digestion.

Purpose of the Study:

  • To investigate the inhibitory potential of sulfated and sulfonated molecules against SARS-CoV-2.
  • To explore the mechanism of inhibition, particularly concerning heparan sulfate interactions.
  • To assess the efficacy of these compounds against both pseudotyped and authentic SARS-CoV-2.

Main Methods:

  • Utilized vesicular stomatitis virus (VSV)-pseudotyped SARS-CoV-2 and authentic SARS-CoV-2.
  • Tested various sulfated and sulfonated molecules, including sulfonated cyclodextrins and nanoparticles.
  • Assessed inhibitory activity and reversibility of the inhibition mechanism.

Main Results:

  • Sulfonated cyclodextrins and nanoparticles demonstrated inhibitory activity against SARS-CoV-2 in micromolar and nanomolar ranges, respectively.
  • These compounds function by preventing the interaction between the SARS-CoV-2 spike protein and heparan sulfates.
  • Inhibition of SARS-CoV-2 by these molecules was found to be reversible, differing from their action on other viruses.

Conclusions:

  • Sulfated and sulfonated molecules are effective inhibitors of SARS-CoV-2 infection by targeting heparan sulfate binding.
  • The reversible nature of this inhibition presents a distinct characteristic compared to their effects on other viruses.
  • These findings suggest potential for developing novel antiviral strategies targeting heparan sulfate interactions for SARS-CoV-2.