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Aryldiazonium Salts to Azo Dyes: Diazo Coupling01:11

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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...
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Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
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Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
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ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH301:11

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All ortho–para directors, excluding halogens, are activating groups. These groups donate electrons to the ring, making the ring carbons electron-rich. Consequently, the reactivity of the aromatic ring towards electrophilic substitution increases. For instance, the nitration of anisole is about 10,000 times faster than the nitration of benzene. The electron-donating effect of the methoxy group in anisole activates the ortho and para positions on the ring and stabilizes the corresponding...
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Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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Antiprotozoal Activity of Highly Substituted Pyrazole and Pyrimidine Derivatives.

Matteo Lusardi1,2, Nicoletta Basilico3, Erika Iervasi4

  • 1Department of Pharmacy, Università degli Studi di Genova, viale Benedetto XV, 3, 16132, Genova, Italy.

Chemmedchem
|June 12, 2025
PubMed
Summary

Novel pyrazole and pyrimidine derivatives were synthesized and found to be effective antimalarial agents against Plasmodium falciparum strains. These compounds also showed activity against Leishmania protozoa with promising pharmacokinetic and toxicity profiles.

Keywords:
antileishmanial agentsantimalarial agentspyrazole compoundspyrimidine derivatives

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Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • Previous research established structure-activity relationships for antimalarial anilino-pyrazoles.
  • There is a continuous need for novel antimalarial and antileishmanial agents, particularly those effective against resistant strains.

Purpose of the Study:

  • To design and synthesize novel trisubstituted pyrazoles and pyrimidines.
  • To evaluate the antimalarial and antileishmanial activities of these new compounds.
  • To assess the cytotoxicity of the synthesized derivatives against human fibroblasts.

Main Methods:

  • Synthesis of pyrazoles (13-15) and pyrimidines (16-17) via a chemo-selective approach using N,S-acetal intermediates.
  • In vitro testing for antimalarial activity against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains.
  • In vitro testing for antileishmanial activity against Leishmania infantum and Leishmania tropica.
  • Cytotoxicity evaluation against human fibroblast cell lines.

Main Results:

  • Pyrazoles 14d,e and pyrimidine 17e demonstrated significant antiplasmodial activity at micromolar concentrations.
  • These compounds effectively inhibited both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains.
  • Activity was also observed against Leishmania infantum and Leishmania tropica protozoa.
  • Favorable pharmacokinetic and toxicity profiles were predicted for the active compounds.

Conclusions:

  • Pyrazoles 14d,e and pyrimidine 17e represent novel and effective agents against malaria and leishmaniasis.
  • The synthesized compounds exhibit broad-spectrum protozoal activity.
  • The predicted favorable drug-like properties warrant further investigation of these compounds.