Tag: 412.9356

Effect of EEG biofeedback combined with ziprasidone and olanzapine on cognitive function and daily living ability in patients with schizophrenia was written by Yan, Li-li;Zhou, Xian-hua;Wang, Tian-ming;Jiang, Yu;Jiang, Xiao-jian. And the article was included in Xiandai Zhenduan Yu Zhiliao in 2021.Application In Synthesis of 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one This article mentions the following:

Objective: To investigate the effect of EEG biofeedback combined with ziprasidone and olanzapine on cognitive function and daily living ability in patients with schizophrenia (SCH). Methods: A total of 100 patients with SCH who were admitted to Shangyou Ankang Hospital and Ruijin Ankang Hospital from Jan. 2019 to March 2020 were selected and randomly divided into the control group and the observation group with 50 cases in each group. The control group was treated with ziprasidone combined with olanzapine, and the observation group was treated with EEG biofeedback combined with ziprasidone and olanzapine for 3 mo. The scores of cognitive function [Mini-Mental State Examination (MMSE)], daily living ability [ADL (ADL)] score, and adverse reactions during treatment were compared between the two groups before treatment and after 3 mo of treatment. Results: After 3 mo of treatment, the MMSE and ADL scores of the two groups were higher than those before treatment, and the observation group was higher than the control group, with statistical significance (P < 0.05). During the treatment, there was no significant difference in the adverse reaction rate between the two groups (P > 0.05). Conclusion: EEG biofeedback combined with ziprasidone and olanzapine in patients with SCH can improve cognitive function and daily living ability without increasing adverse reactions. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Application In Synthesis of 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Similar to other five-membered heterocycles, isothiazoles react with a wide range of electrophilic and nucleophilic reagents to form diverse products. Various penicillins and cephalosporins having an isothiazole ring system have shown considerable antibacterial efficacy against Gram-positive and Gram-negative bacteria.Application In Synthesis of 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Effects of several atypical antipsychotics closapine, sertindole or ziprasidone on hepatic antioxidant enzymes: Possible role in drug-induced liver dysfunction was written by Platanic Arizanovic, Lena;Nikolic-Kokic, Aleksandra;Brkljacic, Jelena;Tatalovic, Nikola;Miler, Marko;Orescanin-Dusic, Zorana;Vidonja Uzelac, Teodora;Nikolic, Milan;Milosevic, Verica;Blagojevic, Dusko;Spasic, Snezana;Miljevic, Cedo. And the article was included in Journal of Toxicology and Environmental Health, Part A: Current Issues in 2021.Reference of 146939-27-7 This article mentions the following:

Chronic use of atypical antipsychotics may produce hepatic damage. Atypical antipsychotics, including clozapine, sertindole, and ziprasidone, are extensively metabolized by the liver and this process generates toxic-free radical metabolic intermediates which may contribute to liver damage. The aim of this study was to investigate whether clozapine, sertindole, or ziprasidone affected hepatic antioxidant defense enzymes which consequently led to disturbed redox homeostasis. The expression and activity of antioxidant enzymes superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GR), catalase (CAT), and glutathione-S-transferases (GST) were measured in rat livers at doses corresponding to human antipsychotic therapy. Clozapine increased activity of SOD types 1 and 2, GR and GST, but reduced CAT activity. Sertindole elevated activities of both SODs. In ziprasidone-treated rats only decreased CAT activity was found. All three antipsychotics produced mild-to-moderate hepatic histopathol. changes categorized as regenerative alterations. No apparent signs of immune cell infiltration, microvesicular or macrovesicular fatty change, or hepatocytes in mitosis were observed In conclusion, a 4-wk long daily treatment with clozapine, sertindole, or ziprasidone altered hepatic antioxidant enzyme activities and induced histopathol. changes in liver. The most severe alterations were noted in clozapine-treated rats. Data indicate that redox disturbances may contribute to liver dysfunction after long-term atypical antipsychotic drug treatment. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Reference of 146939-27-7).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazoles and benzisothiazoles are usually liquids or low-melting-point solids; polar substituents increase the melting points because of the possibility of hydrogen bonding and other interactions in the crystalline state. In general, isothiazole undergoes nitration in the presence of HNO3, sulfuric acid, and sulfonation by using sulfuric acid under thermal conditions to generate corresponding 4-nitro- and 4-sulfonic acid derivatives, respectively.Reference of 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Drug Repurposing to Discover Novel Anti-Inflammatory Agents Inhibiting JAK3/STAT Signaling was written by Sheikh, S. Y.;Hassan, F.;Khan, M. F.;Ahamad, T.;Ansari, W. A.;Akhter, Y.;Khafagy, El-Sayed;Khan, A. R.;Nasibullah, M.. And the article was included in Russian Journal of Bioorganic Chemistry in 2022.Name: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one This article mentions the following:

Among the JAKs, JAK3 is the most important target for the treatment of inflammatory diseases because its inhibition showed the utmost immunosuppression. Many JAK3 inhibitors are already available but most of them showed acquired drug resistance or objectionable side effects. To prevent inflammatory diseases, novel and superior drugs are needed. The drug repositioning is an alternate process that can be used as a fast-track approach. Drugs already approved by regulatory agencies have well-known pharmacokinetics and safety profile. When a new therapeutic activity has been identified, the entities can be rapidly advanced into clin. trials. To identify new promising lead mols., we have selected 1150 approved drugs for their potential to be repurposed for inflammatory diseases. The library of approved drugs was obtained from zinc data base and JAK3 (PDB ID: 3LXK) was retrieved from protein data bank and used for mol. docking simulation and protein-ligand interaction anal. The virtual screening of full library of drugs by AutoDock Vina version PyRx 0.8 and selected 100 drug mols. and further filtered through click-1 docking software. The binding affinity of top 8 drugs ranges between -10.3 to -7.8 kcal/mol. The threshold binding affinity of fluspirilene for JAK3 was -10.3 kcal/mol was repurposed to be promising drug candidate for inflammatory diseases. The results showed that fluspirilene has best docking interaction with JAK3 (PDB ID: 3LXK) and mol. dynamics simulation was also carried out to investigate structural conformations and to explore the key amino acids in the interaction between target and ligands. In conclusion, fluspirilene could be one of the alternative drugs for the treatment of inflammatory diseases. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Name: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazole is more toxic than pyridine. But the more substituted isothiazoles are usually far less toxic. In general, isothiazole undergoes nitration in the presence of HNO3, sulfuric acid, and sulfonation by using sulfuric acid under thermal conditions to generate corresponding 4-nitro- and 4-sulfonic acid derivatives, respectively.Name: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com