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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...

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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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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 antagonists are called...

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Solid-phase Synthesis of [4.4] Spirocyclic Oximes

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Published on: February 6, 2019

Halogenated spirotetronates from Actinoallomurus.

Carlo Mazzetti¹, Mirko Ornaghi, Eleonora Gaspari

¹NAICONS, Via G. Fantoli 16/15, 20138, Milan, Italy. dr.carlo.mazzetti@tiscali.it

Journal of Natural Products

|May 24, 2012

Summary

Two novel spirotetronate compounds, nai414-A and nai414-B, were isolated from Actinoallomurus sp. These compounds exhibit antimicrobial and antitumor properties, highlighting their potential therapeutic applications.

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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

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Published on: February 9, 2021

Area of Science:

Natural product chemistry
Microbiology
Pharmacology

Background:

The spirotetronate class of natural products is known for its diverse biological activities.
Actinoallomurus species are a rich source of novel bioactive compounds.

Purpose of the Study:

To discover and characterize new spirotetronate compounds from Actinoallomurus sp.
To evaluate the antimicrobial and antitumor activities of the isolated compounds.

Main Methods:

Isolation and purification of compounds using chromatographic techniques.
Structure elucidation by 1D and 2D NMR, UV-Vis, and Mass Spectrometry (MS).
Chemical degradation for further structural confirmation.

Main Results:

Two new spirotetronates, nai414-A and nai414-B, were identified and structurally characterized.
Both compounds demonstrated antimicrobial activity against Gram-positive bacteria.
Significant antitumor activity was observed against human microvascular endothelial cells.
Brominated derivatives were successfully synthesized by altering the growth medium.

Conclusions:

The discovery of nai414-A and nai414-B expands the known spirotetronate chemical space.
These compounds represent promising leads for the development of new antimicrobial and anticancer agents.
The ability to generate brominated derivatives offers avenues for structure-activity relationship studies.