Heterocyclic Building Blocks-Isothiazole

Micropollutants in urban stormwater: occurrence, concentrations, and atmospheric contributions for a wide range of contaminants in three French catchments was written by Gasperi, J.;Sebastian, C.;Ruban, V.;Delamain, M.;Percot, S.;Wiest, L.;Mirande, C.;Caupos, E.;Demare, D.;Kessoo, M. Diallo Kessoo;Saad, M.;Schwartz, J. J.;Dubois, P.;Fratta, C.;Wolff, H.;Moilleron, R.;Chebbo, G.;Cren, C.;Millet, M.;Barraud, S.;Gromaire, M. C.. And the article was included in Environmental Science and Pollution Research in 2014.Quality Control of Isothiazol-3(2H)-one This article mentions the following:

This study aimed at: (a) providing information on the occurrence and concentration ranges in urban stormwater for a wide array of pollutants (n = 77); (b) assessing whether despite the differences between various catchments (land use, climatic conditions, etc.), the trends in terms of contamination level are similar; and (c) analyzing the contribution of total atm. fallout (TAF) with respect to sources endogenous to this contamination. The studied contaminants include conventional stormwater contaminants (polycyclic aromatic hydrocarbons (PAHs), Zn, Cu, Pb, etc.), in addition to poorly or undocumented pollutants such as nonylphenol and octylphenol ethoxylates (NPnEO and OPnEO), bisphenol A (BPA), polybrominated di-Ph ethers (PBDEs), a wide variety of pesticides, and various metals of relevance (As, Ti, Sr, V). Sampling and anal. were performed using homogeneous methods on three urban catchments with different land use patterns located in three distinct French towns. For many of these pollutants, the results do not allow highlighting a significant difference in stormwater quality at the scale of the three urban catchments considered. Significant differences were, however, observed for several metals (As, Cr, Cu, Ni, Sr and Zn), PAHs, and PBDEs, though this assessment would need to be confirmed by further experiments The pollutant distributions between dissolved and particulate phases were found to be similar across the three exptl. sites, thus suggesting no site dependence. Lastly, the contributions of TAF to stormwater contamination for micropollutants were quite low. This finding held true not only for PAHs, as previously demonstrated in the literature, but also for a broader range of mols. such as BPA, NPnEO, OPnEO, and PBDEs, whose high local production is correlated with the leaching of urban surfaces, buildings, and vehicles. In the experiment, the researchers used many compounds, for example, Isothiazol-3(2H)-one (cas: 1003-07-2Quality Control of Isothiazol-3(2H)-one).

Isothiazol-3(2H)-one (cas: 1003-07-2) 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. Many compounds with an isothiazole scaffold demonstrated a wide range of biological profiles, including antiinflammatory, antithrombotic, and anticonvulsive agents.Quality Control of Isothiazol-3(2H)-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Genome-wide association study of antipsychotic-induced sinus bradycardia in Chinese schizophrenia patients was written by Weng, Saizheng;Wang, Bo;Li, Mo;Chao, Shan;Lin, Ruiqian;Zheng, Rongyan;Yu, Yinliang;Guo, Shaonan;Lin, Xianhao. And the article was included in PLoS One in 2021.Recommanded Product: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one This article mentions the following:

Second-generation antipsychotics (SGAs) play a critical role in current treatment of schizophrenia (SCZ). It has been observed that sinus bradycardia, rare but in certain situations life threatening adverse drug reaction, can be induced by SGAs across different schizophrenia populations. However, the roles of genetic factors in this phenomenon have not been studied yet. In the present study, a genome-wide association study of single nucleotide polymorphisms (SNPs) was performed on Chinese Han SCZ patients to identify susceptibility loci that were associated with sinus bradycardia induced by SGAs. This study applied microarray to obtain genotype profiles of 88 Han Chinese SCZ patients. Our results found that there were no SNPs had genome-wide significant association with sinus bradycardia induced by SGAs. The top GWAS hit located in gene KIAA0247, which mainly regulated by the tumor suppressor P53 and thus plays a role in carcinogenesis based on resent research and it should not be a susceptibility locus to sinus bradycardia induced by SGAs. Using gene-set functional anal., we tested that if top 500 SNPs mapped genes were relevant to sinus bradycardia. The result of gene prioritization anal. showed CTNNA3 was strongly correlated with sinus bradycardia, hinting it was a susceptibility gene of this ADR. Our study provides a preliminary study of genetic variants associated with sinus bradycardia induced by SGAs in Han Chinese SCZ patients. The discovery of a possible susceptibility gene shed light on further study of this adverse drug reaction in Han Chinese SCZ patients. 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: 146939-27-7Recommanded Product: 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. It has been found that isothiazole-based compounds show synergistic effects when used with other biocidal compounds.Recommanded Product: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Diastereoselective Conjugate Reduction and Enolate Trapping with Glyoxylate Imines. A Concise Approach to β-Lactams that Involves a Ternary Combination of Components was written by Palomo, Claudio;Aizpurua, Jesus M.;Gracenea, Jose Javier. And the article was included in Journal of Organic Chemistry in 1999.Category: isothiazole This article mentions the following:

The conjugate addition of hydride reagents to enolates and subsequent condensation of the resulting enolate with an imine is used to prepare β-lactams. In the experiment, the researchers used many compounds, for example, 1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one (cas: 94594-91-9Category: isothiazole).

1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one (cas: 94594-91-9) belongs to isothiazole derivatives. The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. Isothiazoles are readily prepared from isoxazoles. Thus, reductive ring opening of isoxazoles gives enaminones , which on treatment with phosphorus pentasulfide and chloranil give the corresponding isothiazoles.Category: isothiazole

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Synthesis and CD spectra in MeCN, MeOH, and H₂O of γ-oligopeptides with hydroxy groups on the backbone was written by Brenner, Meinrad;Seebach, Dieter. And the article was included in Helvetica Chimica Acta in 2001.Name: 1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one This article mentions the following:

γ⁴-Tripeptides and γ⁴-hexapeptides, I [n = 1, 2; R¹ = Boc (Boc = tert-butoxycarbonyl), R² = Bn;] and II (n = 1, 2; R¹ = Boc, R² = Bn, or n = 2, R¹ = R² = H) with OH groups in the 2- or 3-position on each residue have been prepared The corresponding 2-hydroxy amino acids were obtained by Si-nitronate (3+2) cycloadditions to the acryloyl derivative of Oppolzer’s sultam and Raney-Ni reduction of the resulting 1,2-oxazolidines. The 3-hydroxy amino acid derivatives were prepared by chain elongation via Claisen condensation of Boc-Ala-OH, Boc-Val-OH, and Boc-Leu-OH, and NaBH₄ reduction of the Me 4-amino 3-oxo carboxylates formed. The N-Boc hydroxy amino acids were coupled in solution to give the γ-peptides. CD spectra of the new types of γ-peptides were recorded and compared with those of simple γ²-, γ³-, γ⁴-, and γ^2,3,4-peptides. An intense Cotton effect at ca. 200 nm ([Θ]= -2.10⁵ deg·cm²·dmol^-1) indicates that the hexapeptide built of (3R,4S)-4-amino-3-hydroxy acids (with the side chains of Val, Ala, Leu) folds to a secondary structure so far unknown. The stability of peptides from β- and γ-amino acids, which carry heteroatoms on their backbones is discussed. Positions on the γ-peptidic 2.6₁₄ helix are identified at which non-H-atoms are “allowed”. In the experiment, the researchers used many compounds, for example, 1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one (cas: 94594-91-9Name: 1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one).

1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one (cas: 94594-91-9) 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.Name: 1-((3aS,6R,7aR)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)prop-2-en-1-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Tetrahydro-3H-pyrazolo[4,3-a]phenanthridine-based CDK inhibitor was written by Opoku-Temeng, Clement;Dayal, Neetu;Hernandez, Delmis E.;Naganna, N.;Sintim, Herman O.. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.Related Products of 53473-85-1 This article mentions the following:

Cyclin-dependent kinases have emerged as important targets for cancer therapy. HSD992, containing a novel scaffold based on the tetrahydro-3H-pyrazolo[4,3-a]phenanthridine core, inhibits CDK2/3 but not other CDKs and also potently inhibits several cancer cell lines. In the experiment, the researchers used many compounds, for example, Benzo[d]isothiazol-5-amine (cas: 53473-85-1Related Products of 53473-85-1).

Benzo[d]isothiazol-5-amine (cas: 53473-85-1) 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. Many compounds with an isothiazole scaffold demonstrated a wide range of biological profiles, including antiinflammatory, antithrombotic, and anticonvulsive agents.Related Products of 53473-85-1

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Conjugate addition of the phenyldimethylsilyl group to αβ-unsaturated carbonyl compounds using a silylzincate in place of the silylcuprate was written by Crump, Roger A. N. C.;Fleming, Ian;Urch, Christopher J.. And the article was included in Journal of the Chemical Society, Perkin Transactions 1 in 1994.Recommanded Product: (E)-1-((3aR,6S,7aS)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)but-2-en-1-one This article mentions the following:

Li phenyldimethylsilyl(dialkyl)zincates add to a number of αβ-unsaturated carbonyl compounds,e.g., PhC:CHCO₂Me, to give, in most cases, higher yields of the conjugate addition product, e.g., PhMe₂SiCHPhCH₂CO₂Me, than the authors had achieved with the corresponding silylcuprate. In the experiment, the researchers used many compounds, for example, (E)-1-((3aR,6S,7aS)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)but-2-en-1-one (cas: 94594-81-7Recommanded Product: (E)-1-((3aR,6S,7aS)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)but-2-en-1-one).

(E)-1-((3aR,6S,7aS)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)but-2-en-1-one (cas: 94594-81-7) 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. The ring structure of isothiazole is incorporated into larger compounds with biological activity such as the pharmaceutical drugs ziprasidone and perospirone.Recommanded Product: (E)-1-((3aR,6S,7aS)-8,8-Dimethyl-2,2-dioxidohexahydro-1H-3a,6-methanobenzo[c]isothiazol-1-yl)but-2-en-1-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Identification of fungi from children’s shoes and application of a novel antimicrobial agent on shoe insole was written by Li, Hui;Zhou, Jin;Shi, Rui;Chen, Wuyong. And the article was included in African Journal of Biotechnology in 2011.Application In Synthesis of Isothiazol-3(2H)-one This article mentions the following:

Thirteen strains of fungi were isolated from 12 shoes worn by children aged 6-12 for a period of more than half a year consisting of 5 strains of yeasts and 8 strains of molds. Through morphol. observation and 18S rDNA sequence anal., the 5 strains of yeasts were identified as follows: Cryptococcus neoformans, Candida albicans, Cryptococcus albidus, Rhodotorula mucilaginosa, and Candida utilis. While the 8 strains of molds characterized and classified by point cropping, insert method, and imprint method were resp. Mucor (2 subspecies), Chain cell mold, Aspergillus (3 subspecies), and Penicillium (2 subspecies). In order to protect children’s feet from being infected by the fungi, a novel nano antimicrobial composite containing nano ZnO and isothiazolinone was prepared and was used to treat the children’s insole by spraying. The inhibitory effects of the nano antimicrobial composite treated insole against yeasts and molds from children’s shoes were evaluated by the inhibition zone and the inhibition ratio method. The results show that the insole treated with 2% nano antimicrobial composite could inhibit the growth of tested microorganism effectively, which could also achieve >97% inhibition ratio against the entire tested fungi. In the experiment, the researchers used many compounds, for example, Isothiazol-3(2H)-one (cas: 1003-07-2Application In Synthesis of Isothiazol-3(2H)-one).

Isothiazol-3(2H)-one (cas: 1003-07-2) belongs to isothiazole derivatives. Isothiazoles and isothiazolium cations are attacked by carbanions at sulfur and on recyclization can give thiophenes. 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 Isothiazol-3(2H)-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

N-Skatyltryptamines-Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential was written by Hogendorf, Agata;Hogendorf, Adam S.;Kurczab, Rafal;Satala, Grzegorz;Szewczyk, Bernadeta;Cieslik, Paulina;Latacz, Gniewomir;Handzlik, Jadwiga;Lenda, Tomasz;Kaczorowska, Katarzyna;Staron, Jakub;Bugno, Ryszard;Duszynska, Beata;Bojarski, Andrzej J.. And the article was included in Molecules in 2021.Product Details of 146939-27-7 This article mentions the following:

A series of N-skatyltryptamines was synthesized and their affinities for serotonin and dopamine receptors were determined Compounds exhibited activity toward 5-HT1A, 5-HT2A, 5-HT6, and D2 receptors. Substitution patterns resulting in affinity/activity switches were identified and studied using homol. modeling. Chosen hits were screened to determine their metabolism, permeability, hepatotoxicity, and CYP inhibition. Several D2 receptor antagonists with addnl. 5-HT6R antagonist and agonist properties were identified. The former combination resembled known antipsychotic agents, while the latter was particularly interesting due to the fact that it has not been studied before. Selective 5-HT6R antagonists have been shown previously to produce procognitive and promnesic effects in several rodent models. Administration of 5-HT6R agonists was more ambiguous-in naive animals, it did not alter memory or produce slight amnesic effects, while in rodent models of memory impairment, they ameliorated the condition just like antagonists. Using the identified hit compounds 15 and 18, we tried to sort out the difference between ligands exhibiting the D2R antagonist function combined with 5-HT6R agonism, and mixed D2/5-HT6R antagonists in murine models of psychosis. 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: 146939-27-7Product Details 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. Some representatives of isothiazoles have proven to be synergists of bioactive substances, which opens the way to lower the doses of drugs used and is especially important in cancer chemotherapy. It has been found that isothiazole-based compounds show synergistic effects when used with other biocidal compounds.Product Details of 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Antipsychotic patterns in outpatients with schizophrenia in China: A cross sectional study was written by Guo, Xiaobing;Yu, Hongye;Wang, Hu. And the article was included in Medicine (Philadelphia, PA, United States) in 2021.HPLC of Formula: 146939-27-7 This article mentions the following:

It is essential to monitor pharmacol. treatment for schizophrenic outpatients regularly in clin. practice. Especially in China, the situation of common prescribing patterns remains unclear. The objective of this study is to reveal real-world treatment prescription patterns of antipsychotics for schizophrenia patients in a representative large tertiary hospital in China.This study is a cross-sectional observational anal. of outpatients with schizophrenia in a large tertiary psychiatric hospital in Beijing, China, from May 11th to 24th, 2019. Data on subjects’ socio-demog. and clin. characteristics, prescriptions of psychotropic drugs were collected from the electronic medical record (EMR) system with a standardized protocol. A multivariate anal. was performed to explore the potential association between antipsychotics treatments and subjects’ characteristics.Of the 1940 patients included in this study, only 1470 (75.77%) patients were prescribed antipsychotic medications. 1228 (83.53%) patients were prescribed second-generation antipsychotics (SGAs), 202 (13.74%) patients were treated only with first-generation antipsychotics (FGAs), 40 (2.72%) were prescribed both SGAs and FGAs. The proportion of single SGAs prescriptions was significantly higher than that of single FGAs antipsychotics in each course of monotherapy group, especially among patients with the course less than 2 years (96.08%). Risperidone was most frequently prescribed antipsychotic medication during the study (29.86%, 439 out of 1470). Intermediate-acting sedative benzodiazepines were the most commonly co-prescribed psychotropic class at 23.66%. Long-acting injectable antipsychotics (LAIs) could be the prescribing trend in clinics. Disease course, self-paying cost and LAI antipsychotic use were independently associated with antipsychotics treatments.Second-generation antipsychotics showed domination in prescriptions. More concerns should be paid with concomitant psychiatric medications in clinics. 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: 146939-27-7HPLC of Formula: 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 their saturated and/or oxygenated analogs play an important role in pharmaceutical research. Many compounds with an isothiazole scaffold demonstrated a wide range of biological profiles, including antiinflammatory, antithrombotic, and anticonvulsive agents.HPLC of Formula: 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Compound preparation of biocide in reclaimed water used as circulating cooling water was written by Han, Yi;Tian, Yi-mei;Wu, Ping;Su, Wei-na;Ma, Yuan. And the article was included in Zhongguo Jishui Paishui in 2013.HPLC of Formula: 1003-07-2 This article mentions the following:

When reclaimed water was used as industrial circulating cooling water, the increasing number of microorganisms would affect heat transfer effect of heat pipes and reduce pipeline service life. The best sterilization doses of four common monomeric biocides in 4 times concentrated water from a Tianjin reclaimed water plant were measured by plate count method. Two kinds of compound biocides were obtained by the orthogonal test at the best doses, and the sterilization effect of the compound biocides was verified through the dynamic experiments The results showed that the best doses of four kinds of biocides were: stabilized chlorine dioxide and sodium hypochlorite 6 mg/L, isothiazolinone 95 mg/L, geramine 120 mg/L, resp., in the condition of the quantity of heterotrophic bacteria about 10⁶ CFU/mL, and the inactivation rate of heterotrophic bacteria was over 94% when used only one of these biocides. The two kinds of compound biocides were: stabilized chlorine dioxide 3 mg/L, isothiazolinone 50 mg/L, geramine 30 mg/L and stabilized chlorine dioxide 4 mg/L, isothiazolinone 40 mg/l., sodium hypochlorite 2 mg/L. Their disinfecting rates were more than 99%. The dynamic test indicated that the disinfecting time of the two kinds of compound biocides could last more than 7 d and bactericidal effect was good when the quantity of heterotrophic bacteria was about 10⁷ CFU/mL. The first kind of compound biocide was more suitable for power plant circulating cooling system sterilization after considering economic factors. In the experiment, the researchers used many compounds, for example, Isothiazol-3(2H)-one (cas: 1003-07-2HPLC of Formula: 1003-07-2).

Isothiazol-3(2H)-one (cas: 1003-07-2) 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.HPLC of Formula: 1003-07-2

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com