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Related Concept Videos

Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
Aryldiazonium Salts to Azo Dyes: Diazo Coupling01:11

Aryldiazonium Salts to Azo Dyes: Diazo Coupling

The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para position.
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN101:14

Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1

Treating arylamines with nitrous acid gives aryldiazonium salts that are effective substrates in nucleophilic aromatic substitution reactions. The diazonio group in these salts can be easily displaced by different nucleophiles, yielding a wide variety of substituted benzenes. The leaving group departs as nitrogen gas, and this easy elimination is the driving force for the substitution reaction.
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo, or cyano...
Diazonium Group Substitution: –OH and –H01:19

Diazonium Group Substitution: –OH and –H

Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions01:20

Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions

Arenediazonium substitution reactions occur when the diazonium group is substituted by various functional groups such as halides, hydroxyl, nitrile, etc. For instance, arenediazonium salts react with copper(I) salts of chloride, bromide, or cyanide to form corresponding aryl chlorides, bromides, and nitriles. These reactions are named Sandmeyer reactions. Although the mechanism of this reaction is complicated, as illustrated in Figure 1, they are believed to progress via an aryl copper...

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Facile Preparation of 4-Substituted Quinazoline Derivatives
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Praziquantel derivatives with antischistosomal activity: aromatic ring modification.

Zhi-xia Wang1, Jing-lei Chen, Chunhua Qiao

  • 1College of Pharmaceutical Science, Soochow University, 199 RenAi Road, Suzhou 215123, Jiangsu, China.

Chemical Biology & Drug Design
|April 27, 2013
PubMed
Summary

Researchers synthesized new praziquantel derivatives to combat Schistosoma japonicum. A modified compound with bromine in the aromatic ring showed significant antischistosomal activity, comparable to praziquantel in vivo.

Keywords:
antischistosomalaromatic ring modificationpraziquantel derivatives

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Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Schistosomiasis japonica remains a significant human health concern, primarily treated with praziquantel.
  • There is a continuous need for novel antischistosomal agents with improved efficacy or different resistance profiles.
  • Modifying existing drug structures is a key strategy in developing new therapeutic agents.

Purpose of the Study:

  • To synthesize and evaluate novel aromatic ring-modified praziquantel derivatives.
  • To identify compounds with potent activity against both juvenile and adult Schistosoma japonicum.
  • To elucidate the structure-activity relationship (SAR) of these modified praziquantel analogs.

Main Methods:

  • Synthesis of a series of praziquantel derivatives with modifications on the aromatic ring.
  • In vitro and in vivo assays to assess the viability of Schistosoma japonicum (japonica schistosomes) worms.
  • Comparative analysis of the antischistosomal activity of synthesized derivatives against the standard drug, praziquantel.

Main Results:

  • Several synthesized praziquantel derivatives exhibited comparable antischistosomal activity to praziquantel.
  • A specific derivative, featuring a bromine substitution on the aromatic ring, demonstrated potent in vivo efficacy.
  • The study revealed key insights into the SAR of aromatic ring-modified praziquantel compounds.

Conclusions:

  • Aromatic ring modification of praziquantel can yield potent antischistosomal agents.
  • Bromine substitution in the aromatic ring represents a promising modification for enhancing antischistosomal activity.
  • The identified derivatives warrant further investigation as potential new treatments for Schistosoma japonicum infections.