Day: October 17, 2022

In 2016,Cheung, Peter K.; Horhant, David; Bandy, Laura E.; Zamiri, Maryam; Rabea, Safwat M.; Karagiosov, Stoyan K.; Matloobi, Mitra; McArthur, Steven; Harrigan, P. Richard; Chabot, Benoit; Grierson, David S. published 《A Parallel Synthesis Approach to the Identification of Novel Diheteroarylamide-Based Compounds Blocking HIV Replication: Potential Inhibitors of HIV-1 Pre-mRNA Alternative Splicing》.Journal of Medicinal Chemistry published the findings.Related Products of 3034-22-8 The information in the text is summarized as follows:

A 256-compound library was evaluated in an anti-HIV screen to identify structural “”mimics”” of the fused tetracyclic indole compound 1 (IDC16) that conserve its anti-HIV activity without associated cytotoxicity. Four diheteroarylamide-type compounds, containing a common 5-nitroisobenzothiazole motif, were identified as active. In subsequent screens, the most potent compound 9 (1C8) was active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50’s of 0.6 and 0.9 μM, resp. Compound 9 also inhibited HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50’s ranging from 0.9 to 1.5 μM. The CC50 value obtained in a cytotoxicity assay for compound 9 was >100 μM, corresponding to a therapeutic index (CC50/EC50) of approx. 100. Further comparison studies revealed that, whereas the anti-HIV activity for compound 9 and the parent mol. 1 are similar, the cytotoxic effect for compound 9 was, as planned, markedly suppressed. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Related Products of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Related Products of 3034-22-8

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

《Redox Properties of Pyrogenic Dissolved Organic Matter (pyDOM) from Biomass-Derived Chars》 was written by Xu, Wenqing; Walpen, Nicolas; Keiluweit, Marco; Kleber, Markus; Sander, Michael. Product Details of 30931-67-0 And the article was included in Environmental Science & Technology on August 17 ,2021. The article conveys some information:

Chars are ubiquitous in the environment and release significant amounts of redox-active pyrogenic dissolved organic matter (pyDOM). Yet, the redox properties of pyDOM remain poorly characterized. This work provides a systematic assessment of the quantity and redox properties of pyDOM released at circumneutral pH from a total of 14 chars pyrolyzed from wood and grass feedstocks from 200 to 700°C. The amount of released pyDOM decreased with increasing pyrolysis temperature of chars, reflecting the increasing degree of condensation and decreasing char polarity. Using flow-injection anal. coupled to electrochem. detection, we demonstrated that electron-donating capacities (EDCpyDOM; up to 6.5 mmole-·gC-1) were higher than electron-accepting capacities (EACpyDOM; up to 1.2 mmole-·gC-1) for all pyDOM specimens. The optical properties and low metal contents of the pyDOM implicate phenols and quinones as the major redox-active moieties. Oxidation of a selected pyDOM by the oxidative enzyme laccase resulted in a 1.57 mmole-·gC-1 decrease in EDCpyDOM and a 0.25 mmole-·gC-1 increase in EACpyDOM, demonstrating a largely irreversible oxidation of presumably phenolic moieties. Non-mediated electrochem. reduction of the same pyDOM resulted in a 0.17 mmole-·gC-1 increase in EDCpyDOM and a 0.24 mmole-·gC-1 decrease in EACpyDOM, consistent with the largely reversible reduction of quinone moieties. Our results imply that pyDOM is an important dissolved redox-active phase in the environment and requires consideration in assessing and modeling biogeochem. redox processes and pollutant redox transformations, particularly in char-rich environments. In the part of experimental materials, we found many familiar compounds, such as ABTS Diammonium(cas: 30931-67-0Product Details of 30931-67-0)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Product Details of 30931-67-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Electric Literature of C7H5ClN2SOn September 15, 2021 ,《Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing a sulfoxide moiety as anaplastic lymphoma kinase (ALK) inhibition agents》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Wu, Feng; Yao, Han; Li, Wei; Zhang, Niuniu; Fan, Yangyang; Chan, Albert S. C.; Li, Xingshu; An, Baijiao. The article contains the following contents:

Herein, 16 new 2,4-diaminopyrimidines I (R1 = H, F, Cl; R2 = EtS, EtSO, i-PrSO; R3 = Me2NCH2CH2NMe, 4-methylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl, 4-dimethylaminopiperidin-1-yl, etc.; R4 = H, H2N, EtCONH) bearing a sulfide or sulfoxide moiety were synthesized and evaluated for anaplastic lymphoma kinase (ALK) inhibitory activity. The optimal compound I [R1 = F; R2 = EtSO; R3 = 4-methylpiperazin-1-yl; R4 = EtCONH; (II)] exhibited excellent antiproliferative activity against non-small cell lung cancer NCI-H2228 cells, which was better than that of Brigatinib and similar to Ceritinib. Mechanism study revealed that the compound II decreased the mitochondrial membrane potential and arrested NCI-H2228 cells in the G0/G1 phase, finally resulting in cellular apoptosis. It is interesting that the compound II could effectively inhibit the migration of NCI-H2228 cells and may be a promising leading compound for chemotherapy of metastatic cancer. In addition to this study using 6-Chlorobenzothiazol-2-ylamine, there are many other studies that have used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Electric Literature of C7H5ClN2S) was used in this study.

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Electric Literature of C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

In 2019,Asian Journal of Organic Chemistry included an article by Song, Xiaoxiao; Gu, Mengjie; Chen, Xiaoyun; Xu, Lei; Ni, Qijian. Synthetic Route of C7H5ClN2S. The article was titled 《Highly Stereoselective Palladium-Catalyzed [3+2] Cycloaddition of Vinyl Epoxides and N-Benzothiazolimines》. The information in the text is summarized as follows:

An asym. [3+2] cycloaddition of racemic vinyl epoxides with N-benzothiazolimines was presented under Pd-catalysis. This transformation provided rapid access to highly functionalized oxazolidine scaffolds such as I [R = H, 4-Me, 5-Br, etc.; Ar = Ph, 1-naphthyl, 2-thienyl, etc.] in generally good yields along with high stereoselectivities (up to 99% ee, 8.5 : 1 d.r.) under mild conditions. The use of chiral BINAP ligand enabled this asym. transformation with a broad substrate tolerance. In addition to this study using 6-Chlorobenzothiazol-2-ylamine, there are many other studies that have used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Synthetic Route of C7H5ClN2S) was used in this study.

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Synthetic Route of C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

In 2019,Polymers (Basel, Switzerland) included an article by Zhang, Shengming; Fang, Guizhen; Chen, Haitao; Lang, Qian. Recommanded Product: ABTS Diammonium. The article was titled 《The effect of degradation of soda lignin using Pd/SO42-/ZrO2 as a catalyst: improved reactivity and antioxidant activity》. The information in the text is summarized as follows:

To the value-added application of the soda lignin by improving its reactivity and antioxidant activity, a self-made Pd/SO42-/ZrO2 catalyst was used to catalyze the degradation reaction of soda lignin. The catalyst was loaded with the palladium of 1.47 weight% while retaining the super acidity of SO4 2-/ZrO2. The reaction condition was determined as follows: the dioxane-water solution was selected as the reaction solution, the addition amount of the catalyst was 5 weight% of the soda lignin, the system was heated at 100°C for 4 h under a hydrogen pressure of 3 MPa. The reactivity of the catalyzed-soda lignin compared to the soda lignin before the reaction was significantly improved: the values of phenolic hydroxyl groups and total hydroxyl groups were increased by 35.3% and 97.1%, resp., and the value of methoxy groups was decreased by 13%. Approx. 63.3% of the β-O-4 bonds were cleaved, which resulted in a reduction of the weight average mol. weight from 8200 g.mol-1 to 4900 gmol-1. At the same time, the EC50 values of the catalyzed-soda lignin on DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS+ 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonate) radicals scavenging were decreased by 20.6% and 32.6%, resp., and the reducing power of catalyzed-soda lignin at the absorption value of 0.5 was increased by 10.5%. The Pd/SO42-/ZrO2catalyst works by breaking the β-O-4 linkages and degrading the methoxy groups. The catalyzed-soda lignin exhibits the possibility of being used as the antioxidants, grafting precursors, adhesive additives, and raw materials for lignin/polymer composites. The experimental process involved the reaction of ABTS Diammonium(cas: 30931-67-0Recommanded Product: ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Recommanded Product: ABTS Diammonium

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Jiang, Chen Hao; Yuan, Xin; Li, Jiang Fen; Xie, Yu Fang; Zhang, An Zhi; Wang, Xue Li; Yang, Lan; Liu, Chun Xia; Liang, Wei Hua; Pang, Li Juan; Zou, Hong; Cui, Xiao Bin; Shen, Xi Hua; Qi, Yan; Jiang, Jin Fang; Gu, Wen Yi; Li, Feng; Hu, Jian Ming published their research in Journal of Translational Medicine on December 31 ,2020. The article was titled 《Bioinformatics-based screening of key genes for transformation of liver cirrhosis to hepatocellular carcinoma》.Recommanded Product: 6-Chlorobenzothiazol-2-ylamine The article contains the following contents:

Abstract: Background: The aims of the present study were to identify key genes related to the transformation of cirrhosis into HCC, and explore the associated mol. mechanisms. Methods: GSE89377, GSE17548, GSE63898 and GSE54236 mRNA microarray datasets from Gene Expression Omnibus (GEO) were analyzed to obtain differentially expressed genes (DEGs) between HCC and liver cirrhosis tissues, and network anal. of protein-protein interactions (PPIs) was carried out. String and Cytoscape were used to analyze modules and identify hub genes, Kaplan-Meier Plotter and Oncomine databases were used to explore relationships between hub genes and disease occurrence, development and prognosis of HCC, and the mol. mechanism of the main hub gene was probed using Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway anal. Results: In total, 58 DEGs were obtained, of which 12 and 46 were up- and down-regulated, resp. Three hub genes (CDKN3, CYP2C9 and LCAT) were identified and associated prognostic information was obtained. CDKN3 may be correlated with the occurrence, invasion, and recurrence of HCC. Genes closely related to changes in the CDKN3 hub gene were screened, and Kyoto Encyclopedia of Genes and Genomes (KEGGs) pathway anal. identified numerous cell cycle-related genes. Conclusion: CDKN3 may affect the transformation of liver cirrhosis into HCC, and represents a new candidate mol. marker of the occurrence and progression of HCC. The experimental part of the paper was very detailed, including the reaction process of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Recommanded Product: 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Luci, Diane K.; Jameson, J. Brian II; Yasgar, Adam; Diaz, Giovanni; Joshi, Netra; Kantz, Auric; Markham, Kate; Perry, Steve; Kuhn, Norine; Yeung, Jennifer; Kerns, Edward H.; Schultz, Lena; Holinstat, Michael; Nadler, Jerry L.; Taylor-Fishwick, David A.; Jadhav, Ajit; Simeonov, Anton; Holman, Theodore R.; Maloney, David J. published an article on January 23 ,2014. The article was titled 《Synthesis and Structure-Activity Relationship Studies of 4-((2-Hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase》, and you may find the article in Journal of Medicinal Chemistry.Synthetic Route of C7H3BrFNS The information in the text is summarized as follows:

Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling mols. are involved in a number of physiol. responses such as platelet aggregation, inflammation, and cell proliferation. Our group has taken a particular interest in platelet-type 12-(S)-LOX (12-LOX) because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Herein, we report the identification and medicinal chem. optimization of a 4-((2-hydroxy-3-methoxybenzyl)-amino)-benzenesulfonamide-based scaffold. Top compounds, exemplified by I [R = 2-benzothiazole, 2-benzoxazole], display nM potency against 12-LOX, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties. In addition, compounds I [R = 2-benzothiazole, 2-benzoxazole] inhibit PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Synthetic Route of C7H3BrFNS) was used in this study.

2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Synthetic Route of C7H3BrFNSTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Shad, Naveed Akhtar; Sajid, Muhammad Munir; Javed, Yasir; Ikram, Muhammad; Hussain, Muhammad Irfan; Nawaz, Somia; Afzal, Amir Muhammad; Hussain, Syed Zajif; Amin, Nasir; Yousuf, Imran published an article on January 31 ,2020. The article was titled 《Lamellar shape lead tungstate (PbWO4) nanostructures as synergistic catalyst for peroxidase mimetic activity》, and you may find the article in Materials Research Express.Recommanded Product: ABTS Diammonium The information in the text is summarized as follows:

Tungstate based nanomaterials have emerged as important class in transition metal oxide. In this study, Lead tungstate (PbWO4) nanostructures with lamellar morphol. were prepared by hydrothermal method. The synthesized materials were characterized by XRD, SEM, FTIR, DLS, BET and PL. Nitrogen adsorption-desorption measurements indicated that the surface area of the synthesized lamellar morphol. was ∼86.225 m2 g-1. The lamellar-like morphol. showed enhanced peroxidase-like activity owing to the large surface area, higher substrate interaction and efficient electron transportation. The results indicated higher reaction velocity (Vmax = 13.56 × 10-8 M s-1) and low Michaelis-Menten constant (km = 0.325 mM) value for nanostructures, providing evidence for higher affinity of novel structures towards the substrate and increased peroxidase-like activity. Finally, biocompatibility test was conducted by performing cytotoxicity experiments of PbWO4 nanostructures on MTT assays. The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0Recommanded Product: ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Recommanded Product: ABTS Diammonium

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Wang, Hefei; Zhao, He-Ping; Zhu, Lizhong published an article in Environmental Science & Technology. The title of the article was 《Role of Pyrogenic Carbon in Parallel Microbial Reduction of Nitrobenzene in the Liquid and Sorbed Phases》.Name: ABTS Diammonium The author mentioned the following in the article:

Surface functional groups and graphitic C comprise the electroactive components of pyrogenic C. The role of pyrogenic C with different electroactive components content in mediating electron transfer in biochem. reactions has not been systematically studied. The authors determined the pyrogenic C electron exchange capacity was 0.067-0.120 mmol e-/g pyrogenic C with maximum elec. conductivity (EC) of 4.85 S/cm. Nitrobenzene was simultaneously reduced in liquid and sorbed phases by Shewanella oneidensis strain MR-1 in the presence of pyrogenic C. Pyrogenic C did not affect aqueous nitrobenzene reduction; reduction of sorbed nitrobenzene was much slower than that of the aqueous species. Enhancing the pyrogenic C oxygenated functional moiety content by HNO3 oxidation elevated bio-reduction rates of aqueous and sorbed species. Anthraquinone groups were deemed the most likely oxygenated functional redox compounds based on voltammetric curve tests and spectroscopic anal. Pyrogenic C reactivity for mediating sorbed nitrobenzene reduction was pos. correlated with its EC, which was demonstrated to be related to condensed aromatic structures. This work elucidated the mechanism for pyrogenic C-mediated biotransformation of nitrobenzene and helped properly evaluate the pyrogenic C role in biogeochem. redox processes occurring in nature. In the experiment, the researchers used ABTS Diammonium(cas: 30931-67-0Name: ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Name: ABTS Diammonium

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

In 2006,Jung, Frederic H.; Pasquet, Georges; Van der Brempt, Christine Lambert; Lohmann, Jean-Jacques M.; Warin, Nicolas; Renaud, Fabrice; Germain, Herve; De Savi, Chris; Roberts, Nicola; Johnson, Trevor; Dousson, Cyril; Hill, George B.; Mortlock, Andrew A.; Heron, Nicola; Wilkinson, Robert W.; Wedge, Stephen R.; Heaton, Simon P.; Odedra, Rajesh; Keen, Nicholas J.; Green, Stephen; Brown, Elaine; Thompson, Katherine; Brightwell, Stephen published 《Discovery of Novel and Potent Thiazoloquinazolines as Selective Aurora A and B Kinase Inhibitors》.Journal of Medicinal Chemistry published the findings.Application of 3034-22-8 The information in the text is summarized as follows:

The synthesis of a novel series of quinazolines substituted at C4 by five-membered ring aminoheterocycles is reported. Their in vitro structure-activity relationships vs. Aurora A and B serine-threonine kinases is discussed. Our results demonstrate that quinazolines with a substituted aminothiazole at C4 possess potent Aurora A and B inhibitory activity and excellent selectivity against a panel of various serine-threonine and tyrosine kinases, as exemplified by N-(3-fluorophenyl)-2-[2-[[7-[3-[4-(hydroxymethyl)piperidin-1-yl]propoxy]-6-methoxy-quinazolinyl]amino]-1,3-thiazol-5-yl]acetamide (I). It was found also that the position and nature of the substituent on the thiazole play key roles in cellular potency. Compounds with an acetanilide substituent at C5′ have the greatest cellular activity. The importance of the C5′ position for substitution has been rationalized by ab initio MO calculations Results show that the planar conformation with the sulfur of the thiazole next to the quinazoline N-3 is strongly favored over the other possible planar conformation. I is a potent suppressor of the expression of phospho-histone H3 in tumor cells in vitro as well as in vivo, where I, administered as its phosphate prodrug suppresses the expression of phospho-histone H3 in s.c. implanted tumors in nude mice. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Application of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Application of 3034-22-8

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica