Pharmacology and Chemistry of the Thioxanthenes with Special Reference to Chlorprothixene

Scheckel, Carl L.

doi:10.1159/000387318

Cited by 3 publications

(3 citation statements)

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“…The use of such drugs is very useful in the treatment of patients with severe depression, psychotic features, and organic psychotic disorders. The most important thioxanthene derivative drugs (Figure ) used as medicine are zuclopenthixol, − its cis-isomer clopenthixol, , flupentixol, ,, chlorprothixen, , and thiothixene. ,, However, these drugs have other clinically useful properties such as antiemetic, antinausea, and antihistamine effects, as well as the ability to potentiate analgesics, sedatives, and general anesthetic actions . In addition, some plants, including thioxanthene derivatives, are also traditional drugs used in the treatment of common diseases, such as coryza, fever, diarrhea, ulcers, stomachaches, and itching …”

Section: Introductionmentioning

confidence: 99%

Intramolecular Friedel–Crafts Reaction with Trifluoroacetic Acid: Synthesizing Some New Functionalized 9-Aryl/Alkyl Thioxanthenes

Deniz,

Yıldız,

Başpınar Küçük

2024

ACS Omega

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In this study, a series of halogen-substituted thioxanthenes were synthesized because the most important and biologically active derivatives of xanthenes are thioxanthenes. In order to obtain new thioxanthene derivatives, first, the starting molecules were synthesized by the appropriate reaction methods in two steps. The intramolecular Friedel−Crafts alkylation (FCA) method was used to convert the prepared three aromatic substituted starting alcohol compounds to their corresponding thioxanthenes by cyclization. For the intramolecular FCA reaction of secondary alcohols, which are the starting compounds (1a−1t), organic Bro̷ nsted acids, which require more innovative, easier, and suitable reaction conditions, were used instead of halide reagents with corrosive effects as classical FCA catalysts. Trifluoroacetic acid was determined to be the organocatalyst with the best yield. Therefore, some original 9-aryl/alkyl thioxanthene derivatives (2a−2t) were synthesized using the optimized FCA method. In addition, a new sulfone derivative of thioxanthene 3i was prepared by performing the oxidation reaction with one of the obtained new thioxanthene 2i. Thioxanthenes and their derivatives are important heterocyclic structures that contain pharmacologically valuable sulfur and are used in the treatment of psychotic diseases such as Alzheimer's or schizophrenia, as well as a number of potent biological activities.

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Section: Introductionmentioning

confidence: 99%

Intramolecular Friedel–Crafts Reaction with Trifluoroacetic Acid: Synthesizing Some New Functionalized 9-Aryl/Alkyl Thioxanthenes

Deniz,

Yıldız,

Başpınar Küçük

2024

ACS Omega

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“…Chloroprothixene, a thioxanthene derivative, significantly prolongs ethanol action [ 1 ]. Strong inhibitory activity of a series of phenothiazines on Na, K-ATPase and horse liver alcohol dehydrogenase has been reported [2,3].…”

Section: Introductionmentioning

confidence: 99%

Effect of phenothiazines on the activity of glycogen phosphorylase b

et al. 1978

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“…In some animals, thioxanthenes block conditioned avoidance behavior, suppress central stimulant action of amphetamine, as well as apomorphine-induced emesis; in other animals they induce catalepsy. In general, the effects of thiothixene are similar to thioproperazine (19,26).…”

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confidence: 97%

Effect of Thiothixene upon the Higher Nervous Activity in Chronic Schizophrenics

Saarma¹,

Saarma²,

Sild³

et al. 1974

Int Pharmacopsychiatry

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The clinical effects of thiothixene and its action upon the HNA have been investigated in a sample of 22 chronic schizophrenic patients (mean duration of the disease 9.6 years). In three patients there was a good, and in nine patients there was a moderate, clinical improvement. In HNA there was a marked improvement of the stability of excitatory process, of the equilibrium of excitatory and inhibitory processes and of internal inhibition. Some of the HNA parameters reflecting the intensity of transmarginal inhibition were found to be of prognostic value.

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Pharmacology and Chemistry of the Thioxanthenes with Special Reference to Chlorprothixene

Cited by 3 publications

References 0 publications

Intramolecular Friedel–Crafts Reaction with Trifluoroacetic Acid: Synthesizing Some New Functionalized 9-Aryl/Alkyl Thioxanthenes

Intramolecular Friedel–Crafts Reaction with Trifluoroacetic Acid: Synthesizing Some New Functionalized 9-Aryl/Alkyl Thioxanthenes

Effect of phenothiazines on the activity of glycogen phosphorylase b

Effect of Thiothixene upon the Higher Nervous Activity in Chronic Schizophrenics

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