Month: October 2022

In 2016,Li, Hongshuang; Wang, Xinran; Duan, Guiyun; Xia, Chengcai; Xiao, Yuliang; Li, Furong; Ge, Yanqing; You, Guirong; Han, Junfen; Fu, Xiaopan; Tan, Shanhui; Wang, Rongwei published 《Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives》.Chemical Research in Chinese Universities published the findings.Computed Properties of C3H3BrN2S The information in the text is summarized as follows:

In this paper, we described the synthesis of 2-aminothiazole sublibrary containing Me, bromo, Ph or butylidene at 4- or/and 5-position of its core. All target compounds were evaluated for their antitumor activities against human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compounds screened, 4,5,6,7-tetrahydrobenzo[d]thiazole(26b) exhibited the most potent antitumor activities with IC50 values of 4.89 and 4.03 μmol/L against the two tested cell lines, resp. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated. In the experiment, the researchers used 5-Bromothiazol-2-amine(cas: 3034-22-8Computed Properties of C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) 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.Computed Properties of C3H3BrN2S

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

Related Products of 3034-22-8In 2006 ,《Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Das, Jagabandhu; Furch, Joseph A.; Liu, Chunjian; Moquin, Robert V.; Lin, James; Spergel, Steven H.; McIntyre, Kim W.; Shuster, David J.; O’Day, Kathleen D.; Penhallow, Becky; Hung, Chen-Yi; Doweyko, Arthur M.; Kamath, Amrita; Zhang, Hongjian; Marathe, Punit; Kanner, Steven B.; Lin, Tai-An; Dodd, John H.; Barrish, Joel C.; Wityak, John. The article contains the following contents:

A series of structurally novel aminothiazole-based inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound I is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Related Products of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Related Products of 3034-22-8

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

《Zeolite/Chitosan/Gelatin Films: Preparation, Supercritical CO2 Processing, Characterization, and Bioactivity》 was written by Pajnik, Jelena; Dikic, Jelena; Milovanovic, Stoja; Milosevic, Milena; Jevtic, Sanja; Lukic, Ivana. Computed Properties of C18H24N6O6S4 And the article was included in Macromolecular Materials and Engineering on August 31 ,2022. The article conveys some information:

Chitosan/gelatin and chitosan/gelatin/zeolite films prepared by solvent casting method are impregnated with a mixture of thymol and carvacrol using a green solvent, supercritical carbon dioxide at 35°C and 30 MPa, during 18 h. Proposed method enables preparation of biocompatible and biodegradable blends with strong antioxidant and antibacterial activity, whereby amounts of loaded thymol/carvacrol (TC) mixture are in the range from 3.3% to 6%. After initial burst release, both types of films exhibit gradual release of bioactive compounds, with around 72% and 96% of impregnated TC mixture released in water and phosphate buffered saline solution (pH 7.4) during tested period of 10 days, resp. Results of water vapor transmission rate (>76 g m-2 day-1) confirm that prepared composites are suitable for wound dressing application. Thermal anal. shows superior properties of prepared TC loaded films compared to control samples. In addition, mech. and structural properties, as well as solubility and swelling behavior of the obtained films are investigated in detail.ABTS Diammonium(cas: 30931-67-0Computed Properties of C18H24N6O6S4) was used in this study.

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.Computed Properties of C18H24N6O6S4

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

HPLC of Formula: 30931-67-0On October 31, 2020 ,《Enzymatic depolymerization of industrial lignins by laccase-mediator systems in 1,4-dioxane/water》 appeared in Biotechnology and Applied Biochemistry. The author of the article were Dillies, Justine; Vivien, Celine; Chevalier, Mickael; Rulence, Alexandre; Chataigne, Gabrielle; Flahaut, Christophe; Senez, Vincent; Froidevaux, Renato. The article conveys some information:

Lignin is the second most abundant polymer after cellulose in lignocellulosic biomass. Its aromatic composition and recalcitrant nature make its valorization a major challenge for obtaining low mol. weight aromatics compounds with high value-added from the enzymic depolymerization of industrial lignins. The oxidation reaction of lignin polymer using laccases alone remains inefficient. Therefore, researches are focused on the use of a laccase-mediator system (LMS) to facilitate enzymic depolymerization Until today, the LMS system was studied using water-soluble lignin only (com. lignins, modified lignins, or lignin model compounds). This work reports a study of three LMS systems to depolymerize the three major industrial lignins (organosolv lignin, Kraft lignin, and sodium lignosulfonate). We show that an enzymic depolymerization of these lignins can be achieved by LMS using laccase from Trametes versicolor, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt as mediator and a cosolvent (25% of 1,4-dioxane) to enhance the solubilization of lignins. In the part of experimental materials, we found many familiar compounds, such as ABTS Diammonium(cas: 30931-67-0HPLC of Formula: 30931-67-0)

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.HPLC of Formula: 30931-67-0

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

Application of 95-24-9On November 15, 2019 ,《Pyrazolo-benzothiazole hybrids: synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model》 appeared in European Journal of Medicinal Chemistry. The author of the article were Reddy, Velma Ganga; Reddy, T. Srinivasa; Jadala, Chetna; Reddy, M. Soumya; Sultana, Faria; Akunuri, Ravikumar; Bhargava, Suresh K.; Wlodkowic, Donald; Srihari, P.; Kamal, Ahmed. The article conveys some information:

A series of new pyrazolo-benzothiazole hybrids I [R1 = H, MeO, F, Cl; R2 = H, Me, MeO, F, Cl] was synthesized and screened for their anticancer activity against several cancer cell lines [colon (HT-29), prostate (PC-3), lung (A549), glioblastoma (U87MG)] and normal human embryonic kidney cell line (Hek-293T). Compounds I [R1 = H, R2 = F, Cl; R1 = F, R2 = F, Cl; R1 = Cl, R2 = F, Cl; R1 = MeO, R2 = F, Cl] displayed significant anticancer activity against all tested cancer cell lines and compound I [R1 = F, R2 = Cl] showed most potent activity among the series with IC50 values in the range 3.17-6.77 μM, even better than reference drug axitinib (4.88-21.7 μM). Compound I [R1 = F, R2 = Cl] also showed the strongest growth inhibition in 3D multicellular spheroids of PC-3 and U87MG cells. The mechanism of cellular toxicity in PC-3 cells was found to be cell cycle arrest and apoptosis induction through depolarisation of mitochondrial membrane potential, increased ROS production and subsequent DNA damage. Further, compound I [R1 = F, R2 = Cl] displayed significant in vitro (VEGFR-2 inhibition) and in vivo [transgenic zebrafish Tg(flila:EGFP) model] antiangiogenic properties. Overall, these results provided strong evidence that compound I [R1 = F, R2 = Cl] could be considered for a lead candidate in anticancer and antiangiogenic drug discovery. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Application of 95-24-9)

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.Application of 95-24-9Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

《Benzothiazolyl ureas are low micromolar and uncompetitive inhibitors of 17β-HSD10 with implications to Alzheimer’s disease treatment》 was published in International Journal of Molecular Sciences in 2020. These research results belong to Schmidt, Monika; Benek, Ondrej; Vinklarova, Lucie; Hrabinova, Martina; Zemanova, Lucie; Chribek, Matej; Kralova, Vendula; Hroch, Lukas; Dolezal, Rafael; Lycka, Antonin; Prchal, Lukas; Jun, Daniel; Aitken, Laura; Gunn-Moore, Frank; Kuca, Kamil; Musilek, Kamil. Computed Properties of C7H5ClN2S The article mentions the following:

Human 17β-hydroxysteroid dehydrogenase type 10 is a multifunctional protein involved in many enzymic and structural processes within mitochondria. This enzyme was suggested to be involved in several neurol. diseases, e.g., mental retardation, Parkinson’s disease, or Alzheimer’s disease, in which it was shown to interact with the amyloid-beta peptide. We prepared approx. 60 new compounds based on a benzothiazolyl scaffold and evaluated their inhibitory ability and mechanism of action. The most potent inhibitors contained 3-chloro and 4-hydroxy substitution on the Ph ring moiety, a small substituent at position 6 on the benzothiazole moiety, and the two moieties were connected via a urea linker (4at, 4bb, and 4bg). These compounds exhibited IC50 values of 1-2μ and showed an uncompetitive mechanism of action with respect to the substrate, acetoacetyl-CoA. These uncompetitive benzothiazolyl inhibitors of 17β-hydroxysteroid dehydrogenase type 10 are promising compounds for potential drugs for neurodegenerative diseases that warrant further research and development. The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Computed Properties of C7H5ClN2S)

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.Computed Properties of C7H5ClN2SThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

《Blue Light-Gated Reversible Silver Nanozyme Reaction Networks that Achieve Life-like Adaptivity》 was written by Jiang, Zhengxing; Li, Hua; Deng, Yuequan; He, Yi. Synthetic Route of C18H24N6O6S4 And the article was included in ACS Sustainable Chemistry & Engineering on April 6 ,2020. The article conveys some information:

Life is preserved by complex enzymic reaction systems. Inspired by life, here the authors report on the first example to fabricate blue light-gated reversible silver nanozyme reaction networks that achieve life-like adaptivity. Upon blue light excitation, silver nanoparticles (AgNPs) display oxidase-like activity in the presence of Cl- as a cofactor. The addition of Cl- promotes the separation between hot holes and electrons that are generated by excited-state surface plasmon of AgNPs, inducing the generation of highly reactive hydroxyl and superoxide anion radicals. They oxidize colorless 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)diammonium salt (ABTS) to yield green ABTS radicals (ABTS•+). It is shown that ABTS•+ is able to be reduced by AgNPs to regenerate ABTS when the blue light is turned off, and the reaction system returns to its initial state, which is the typical feature of the artificial adaptive system. The dynamic process of the adaptive system is tunable by changing the concentrations of AgNPs and Cl-, and it possesses excellent recyclable performance, which can be repeated at least six times. Overall, the silver nanozyme reaction networks are capable of responding to blue light stimuli and renewing by recycling to the initial state without blue light irradiation Inspired by enzymic reaction systems, blue light-gated reversible silver nanozyme reaction networks that achieve life-like adaptivity are successfully constructed. After reading the article, we found that the author used ABTS Diammonium(cas: 30931-67-0Synthetic Route of C18H24N6O6S4)

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.Synthetic Route of C18H24N6O6S4

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

In 2015,Angewandte Chemie, International Edition included an article by Adams, Luke A.; Sharma, Pooja; Mohanty, Biswaranjan; Ilyichova, Olga V.; Mulcair, Mark D.; Williams, Martin L.; Gleeson, Ellen C.; Totsika, Makrina; Doak, Bradley C.; Caria, Sofia; Rimmer, Kieran; Horne, James; Shouldice, Stephen R.; Vazirani, Mansha; Headey, Stephen J.; Plumb, Brent R.; Martin, Jennifer L.; Heras, Begona; Simpson, Jamie S.; Scanlon, Martin J.. Related Products of 144060-98-0. The article was titled 《Application of Fragment-Based Screening to the Design of Inhibitors of Escherichia coli DsbA》. The information in the text is summarized as follows:

The thiol-disulfide oxidoreductase enzyme DsbA catalyzes the formation of disulfide bonds in the periplasm of Gram-neg. bacteria. DsbA substrates include proteins involved in bacterial virulence. In the absence of DsbA, many of these proteins do not fold correctly, which renders the bacteria avirulent. Thus DsbA is a critical mediator of virulence and inhibitors may act as antivirulence agents. Biophys. screening has been employed to identify fragments that bind to DsbA from Escherichia coli. Elaboration of one of these fragments produced compounds that inhibit DsbA activity in vitro. In cell-based assays, the compounds inhibit bacterial motility, but have no effect on growth in liquid culture, which is consistent with selective inhibition of DsbA. Crystal structures of inhibitors bound to DsbA indicate that they bind adjacent to the active site. Together, the data suggest that DsbA may be amenable to the development of novel antibacterial compounds that act by inhibiting bacterial virulence.4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Related Products of 144060-98-0) was used in this study.

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Related Products of 144060-98-0

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

In 2021,Chemical Communications (Cambridge, United Kingdom) included an article by Wu, Yue; Guo, Peng; Chen, Long; Duan, Weijie; Yang, Zengzhuan; Wang, Tao; Chen, Ting; Xiong, Fei. HPLC of Formula: 95-24-9. The article was titled 《Iron-catalyzed tandem oxidative coupling and acetal hydrolysis reaction to prepare formylated benzothiazoles and isoquinolines》. The information in the text is summarized as follows:

The direct formylation of benzothiazoles and isoquinolines was reported. The reaction features a novel iron-catalyzed Minisci-type oxidative coupling process using com. available 1,3-dioxolane as a formylated reagent followed by acetal hydrolysis without a separation process. The reaction was performed under exceedingly mild reaction conditions and exhibited broad functional group tolerance. The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9HPLC of Formula: 95-24-9)

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.HPLC of Formula: 95-24-9The 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 2008,Frechette, Sylvie; Leit, Silvana; Woo, Soon Hyung; Lapointe, Guillaume; Jeannotte, Guillaume; Moradei, Oscar; Paquin, Isabelle; Bouchain, Giliane; Raeppel, Stephane; Gaudette, Frederic; Zhou, Nancy; Vaisburg, Arkadii; Fournel, Marielle; Yan, Pu Theresa; Trachy-Bourget, Marie-Claude; Kalita, Ann; Robert, Marie-France; Lu, Aihua; Rahil, Jubrail; MacLeod, A. Robert; Besterman, Jeffrey M.; Li, Zuomei; Delorme, Daniel published 《4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Name: 5-Bromothiazol-2-amine The information in the text is summarized as follows:

The synthesis and biol. evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21WAF1/Cip1, and inhibit proliferation of human cancer cells. In addition, certain compounds of this class were active in several human tumor xenograft models in vivo. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) 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.Name: 5-Bromothiazol-2-amine

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