Schizophrenia is a severe neuropsychiatric disorder that deteriorates perception, affection, and cognitive mental functions. The current treatments are mainly focused on the dopamine system, but the so-named dopamine hypothesis of schizophrenia fails to explain all the symptoms. Previous studies have shown that there is a reciprocal relationship between muscarinic acetylcholine receptors and dopamine receptor function. Some muscarinic ligands show antidopaminergic activity, and therefore, they should have some antipsychotic efficacy. In this work, conceptual density functional theory is employed to analyze the properties of acetylcholine's agonists, partial agonists, or antagonists. The aim is to establish a classification of the antipsychotic-like or pro-psychotic activities of these molecules based on the electron-donor and electron-acceptor properties. Most of the agonists and antagonists are better electron donors and worse electron acceptors than partial agonists. We found that acetylcholine antagonists that clinically promote psychotic symptoms are good electron-donor molecules, and acetylcholine agonists that clinically relieve symptoms of psychosis are good electron donors. These results represent a further advance on the road to understanding the charge-transfer properties of drugs used as possible treatments for schizophrenia.

08 Jun 2021·ChemCatChem

Time‐Economical Synthesis of Diarylacetates Enabled by TfOH‐Catalyzed Arylation of α‐Aryl‐α‐Diazoesters with Arenes

Author: Wu, Jiale ; Chen, Fener ; Hu, Sha ; Lu, Zuolin ; Wang, Jiaqi ; Tao, Yuan ; Jiang, Meifen

AbstractDiarylacetates are privileged structures of many bioactive natural products and pharmaceutical compounds. A time‐economical synthesis of diarylacetates by TfOH‐catalyzed arylation of α‐aryl‐α‐diazoesters with arenes is described. This protocol provides a variety of diarylacetates in good yields with broad substrate scope, excellent functional group compatibility, and mild reaction conditions. Also, a new mechanism for the arylation reaction of α‐aryl‐α‐diazoesters with arenes under TfOH catalysis is presented.

04 May 2020·Chemistry – A European Journal

Room Temperature Coupling of Aryldiazoacetates with Boronic Acids Enhanced by Blue Light Irradiation

Article

Author: Cormanich, Rodrigo A. ; da Silva, Amanda F. ; Jurberg, Igor D. ; Afonso, Marco A. S.

AbstractA visible‐light‐promoted photochemical protocol is reported for the coupling of aryldiazoacetates with boronic acids. This photochemical reaction shows great enhancement compared to the same protocol performed in the absence of light. Except for a few cases, the room temperature coupling in the dark (thermal process) generally does not work. When it does, it is likely to also involve free carbenes as key intermediates. Alternatively, photochemical reactions show a broad scope, can be performed under air and tolerate a wide variety of functional groups. Reaction‐evolution monitoring, DFT calculations and control experiments have been used to evaluate the main aspects of this intricate mechanistic scenario. Biologically active molecules Adiphenine, Benactyzine and Aprophen have been prepared as examples of synthetic applications.

100 Deals associated with Benactyzine Hydrochloride

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KEGG	Wiki	ATC	Drug Bank
-	Benactyzine Hydrochloride	A02B	DB09023

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Indication	Country/Location	Organization	Date
Duodenal Ulcer	China	Hebei Dongfeng Pharmaceutical Co. Ltd.	01 Jan 1995
Duodenal Ulcer	China	Hebei Brics Pharmaceutical Co Ltd	01 Jan 1995
Stomach Ulcer	China	Hebei Brics Pharmaceutical Co Ltd	01 Jan 1995
Stomach Ulcer	China	Hebei Dongfeng Pharmaceutical Co. Ltd.	01 Jan 1995

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