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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...

Cholinergic Antagonists: Pharmacokinetics

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations, while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...

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An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity

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Published on: November 2, 2016

Acylpyrazoline-Based Third-Generation Selective Antichlamydial Compounds with Enhanced Potency.

Bin Lu^1,2, Qi Qiao³, Elizabeth R Park^3,4

¹Department of Parasitology, Central South University Xiangya Medical School, Changsha, Hunan 410013, China.

|February 27, 2023

Summary

Researchers developed novel third-generation selective antichlamydials (SACs) that are more potent against Chlamydia infections than previous generations. These compounds show promise for treating infections without harming beneficial bacteria or host cells.

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Targeted Antibody Blocking by a Dual-Functional Conjugate of Antigenic Peptide and Fc-III Mimetics DCAF

Targeted Antibody Blocking by a Dual-Functional Conjugate of Antigenic Peptide and Fc-III Mimetics DCAF

Published on: September 17, 2019

Area of Science:

Microbiology
Medicinal Chemistry
Infectious Diseases

Background:

Chlamydiae are significant bacterial pathogens requiring effective treatments.
Current broad-spectrum antibiotics can disrupt beneficial gut and vaginal microbiota.
Previous benzal acylhydrazones showed selective antichlamydial activity without harming beneficial bacteria.

Purpose of the Study:

To identify and characterize novel, more potent selective antichlamydials (SACs).
To evaluate the efficacy and safety of third-generation acylpyrazoline-based SACs against Chlamydia species.
To assess the impact of these new compounds on beneficial bacteria and host cells.

Main Methods:

Synthesis and characterization of acylpyrazoline-based compounds.
Determination of minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC) against Chlamydia trachomatis and Chlamydia muridarum.
In vitro testing for toxicity against Lactobacillus, Escherichia coli, Klebsiella, Salmonella, and host cells.

Main Results:

Two novel acylpyrazoline-based SACs were identified.
These compounds demonstrated 2- to 5-fold increased potency against Chlamydia species compared to second-generation leads.
The SACs exhibited excellent tolerability towards beneficial bacteria (Lactobacillus) and other microbes, as well as host cells.

Conclusions:

Third-generation acylpyrazoline-based SACs represent a significant advancement in selective antichlamydial drug development.
These compounds offer improved potency and selectivity, addressing the limitations of broad-spectrum antibiotics.
Further investigation is warranted to explore their therapeutic potential for chlamydial infections.