Category: 3034-22-8

Quality Control of 5-Bromothiazol-2-amineIn 2013 ,《Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Decor, Anne; Grand-Maitre, Chantal; Hucke, Oliver; O’Meara, Jeff; Kuhn, Cyrille; -Forget, Lea Constantineau; Brochu, Christian; Malenfant, Eric; Bertrand-Laperle, Megan; Bordeleau, Josee; Ghiro, Elise; Pesant, Marc; Fazal, Gulrez; Gorys, Vida; Little, Michael; Boucher, Colette; Bordeleau, Sylvain; Turcotte, Pascal; Guo, Tim; Garneau, Michel; Spickler, Catherine; Gauthier, Annick. The article contains the following contents:

Herein the design, synthesis and biol. evaluation of antiviral compounds acting against human rhinovirus (HRV) are described. A series of aminothiazoles I [X = CH, N; R1 = H, Me; R2 = F3CCH2CHMe, cis-4-methoxycyclohexyl, benzyl(4-pyridylcarbonyl)aminomethyl, etc.] demonstrated pan-activity against the HRV genotypes screened and productive structure-activity relationships. A comprehensive investigational library was designed and performed allowing the identification of potent compounds with lower mol. weight and improved ADME profile. The compounds I [X = N; R1 = Me; R2 = F3CCH2CHMe (both enantiomers), F3CCH2CMe2] showed good exposures in CD-1 mice. The mechanism of action was discovered to be a host target: the lipid kinase phosphatidylinositol 4-kinase III beta (PI4KIIIss). The identification of the pan-HRV active compound I (X = N; R1 = Me; R2 = F3CCH2CMe2) combined with a structurally distinct literature compound T-00127-HEV1 allowed the assessment of target related tolerability of inhibiting this kinase for a short period of time in order to prevent HRV replication. In the experiment, the researchers used 5-Bromothiazol-2-amine(cas: 3034-22-8Quality Control of 5-Bromothiazol-2-amine)

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.Quality Control of 5-Bromothiazol-2-amine

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

In 2018,Wang, Beilei; Wu, Jiaxin; Wu, Yun; Chen, Cheng; Zou, Fengming; Wang, Aoli; Wu, Hong; Hu, Zhenquan; Jiang, Zongru; Liu, Qingwang; Wang, Wei; Zhang, Yicong; Liu, Feiyang; Zhao, Ming; Hu, Jie; Huang, Tao; Ge, Juan; Wang, Li; Ren, Tao; Wang, Yuxin; Liu, Jing; Liu, Qingsong published 《Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor》.European Journal of Medicinal Chemistry published the findings.Formula: C3H3BrN2S The information in the text is summarized as follows:

Through a structure-guided rational drug design approach, we have discovered a highly selective inhibitor compound 40 (JSH-150), which exhibited an IC50 of 1 nM against CDK9 kinase in the biochem. assay and achieved around 300-10000-fold selectivity over other CDK kinase family members. In addition, it also displayed high selectivity over other 468 kinases/mutants (KINOMEscan S score(1) = 0.01). Compound 40 displayed potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines. It could dose-dependently inhibit the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrest the cell cycle and induce the apoptosis in the leukemia cells. In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of 40 could almost completely suppress the tumor progression. The high selectivity and good in vivo PK/PD profile suggested that 40 would be a good pharmacol. tool to study CDK9-mediated physiol. and pathol. as well as a potential drug candidate for leukemia and other cancers. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Formula: C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Formula: C3H3BrN2S

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

In 2010,Kitas, Eric; Mohr, Peter; Kuhn, Bernd; Hebeisen, Paul; Wessel, Hans Peter; Haap, Wolfgang; Ruf, Armin; Benz, Joerg; Joseph, Catherine; Huber, Walter; Sanchez, Ruben Alvarez; Paehler, Axel; Benardeau, Agnes; Gubler, Marcel; Schott, Brigitte; Tozzo, Effie published 《Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of Type-2 diabetes》.Bioorganic & Medicinal Chemistry Letters published the findings.Formula: C3H3BrN2S The information in the text is summarized as follows:

Sulfonylureido thiazoles were identified from a HTS campaign and optimized through a combination of structure-activity studies, x-ray crystallog. and mol. modeling to yield potent inhibitors of fructose-1,6-bisphosphatase. Compound 12 showed favorable ADME properties, for example, F = 70%, and a robust 32% glucose reduction in the acute db/db mouse model for Type-2 diabetes. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8Formula: C3H3BrN2S)

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.Formula: C3H3BrN2S

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

In 2010,Lin, Shuqun; Wrobleski, Stephen T.; Hynes, John Jr.; Pitt, Sidney; Zhang, Rosemary; Fan, Yi; Doweyko, Arthur M.; Kish, Kevin F.; Sack, John S.; Malley, Mary F.; Kiefer, Susan E.; Newitt, John A.; McKinnon, Murray; Trzaskos, James; Barrish, Joel C.; Dodd, John H.; Schieven, Gary L.; Leftheris, Katerina published 《Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C3H3BrN2S The information in the text is summarized as follows:

The design, synthesis, and structure-activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of I as a potent p38α inhibitor that utilizes a unique nitrogen-sulfur intramol. nonbonding interaction to stabilize the conformation required for binding to the p38α active site. X-ray crystallog. studies that confirm the proposed binding mode of this class of inhibitors in p38α and provide evidence for the proposed intramol. nitrogen-sulfur interaction are discussed. In addition to this study using 5-Bromothiazol-2-amine, there are many other studies that have used 5-Bromothiazol-2-amine(cas: 3034-22-8COA of Formula: C3H3BrN2S) was used in this study.

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.COA of Formula: C3H3BrN2S

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

SDS of cas: 3034-22-8In 2011 ,《Synthesis and application of a new thiazolylazo reagent for cloud point extraction and determination of cobalt in pharmaceutical preparations》 was published in Journal of AOAC International. The article was written by Yamaki, Regina Terumi; Nunes, Luana Sena; Rodrigues de Oliveira, Hygor; Araujo, Andre S.; Bezerra, Marcos Almeida; Lemos, Valfredo Azevedo. The article contains the following contents:

The synthesis and characterization of the reagent 2-(5-bromothiazolylazo)-4-chlorophenol (I) and its application in the development of a preconcentration procedure for cobalt determination using flame at. absorption spectrometry after cloud point extraction is presented. This procedure is based on cobalt complexing and entrapment of the metal chelates into micelles of a surfactant-rich phase of Triton X-114. The preconcentration procedure was optimized by using a response surface methodol. through the application of the Box-Behnken matrix. Under optimum conditions, the procedure determined the presence of cobalt with an LOD of 2.8 μg/L and LOQ of 9.3 μg/L. The enrichment factor obtained was 25. The precision was evaluated as the RSD, which was 5.5% for 10 μg/L cobalt and 6.9% for 30 μg/L. The accuracy of the procedure was assessed by comparing the results with those found using inductively coupled plasma-optical emission spectrometry. After validation, the procedure was applied to the determination of cobalt in pharmaceutical preparation samples containing cobalamin (vitamin B12). After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8SDS of cas: 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.SDS of cas: 3034-22-8

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

Application of 3034-22-8In 2017 ,《In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Vale, Nuno; Correia-Branco, Ana; Patricio, Barbara; Duarte, Diana; Martel, Fatima. The article contains the following contents:

The investment in cancer research is critical to find more and better treatments, but essentially to save lives. This paper describes the synthesis and characterization of bromothiazole derivatives with amino acids, e.g., I, and with core of nitazoxanide, an FDA-approved antiprotozoal drug. Using a human adenocarcinoma-derived cell line (the Caco-2 cell line), the antiproliferative (3H-thymidine incorporation) and cytotoxic (extracellular lactate dehydrogenase activity) effect of these derivatives, were investigated. All the derivatives caused a concentration-dependent decrease in cell proliferation and viability. At their highest concentration, all compounds were able to reduce 3H-thymidine incorporation by more than 80%, corresponding to a more marked antiproliferative effect than butyrate. As to their cytotoxic effect, it was comparable to that of butyrate. The ability of bromo substituent in thiazole ring with sequences of amino acids in inducing cell death and apoptosis in Caco-2 cells (and other cell lines) is now being studied. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8Application of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Application of 3034-22-8

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

In 2004,Quelever, Gilles; Burlet, Stephane; Garino, Cedrik; Pietrancosta, Nicolas; Laras, Younes; Kraus, Jean-Louis published 《Simple Coupling Reaction between Amino Acids and Weakly Nucleophilic Heteroaromatic Amines》.Journal of Combinatorial Chemistry published the findings.HPLC of Formula: 3034-22-8 The information in the text is summarized as follows:

Solution-phase amidation of amino acid Boc-Ala-OH by substituted, weakly nucleophilic heterocyclic aromatic amines was studied in presence of coupling reagents using a parallel synthesis procedure. Coupling agents POCl3/pyridine, BOP, DCC/HOBt, and HBTU were examined for this reaction. Thus, Boc-Ala-NHAr [Ar = CH2C6H4NO2-4, CH2Ph, CH2C6H11, 4-(4-nitrophenyl)-2-thiazolyl, 5-bromo-2-thiazolyl, 2-thiazolyl, 5-nitro-2-thiazolyl] were prepared in moderate to high yields. The results showed that when bulky, weakly nucleophilic, heterocyclic aromatic amines are to be coupled, POCl3 in pyridine could be used as a coupling agent in solution-phase automated synthesis for obtaining racemization-free products in reasonable good yields. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8HPLC of Formula: 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.HPLC of Formula: 3034-22-8

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

In 2011,Hebeisen, Paul; Haap, Wolfgang; Kuhn, Bernd; Mohr, Peter; Wessel, Hans Peter; Zutter, Ulrich; Kirchner, Stephan; Ruf, Armin; Benz, Joerg; Joseph, Catherine; Alvarez-Sanchez, Ruben; Gubler, Marcel; Schott, Brigitte; Benardeau, Agnes; Tozzo, Effie; Kitas, Eric published 《Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase》.Bioorganic & Medicinal Chemistry Letters published the findings.Product Details of 3034-22-8 The information in the text is summarized as follows:

A novel sulfonylureido pyridine series exemplified by compound 19 (I) yielded potent inhibitors of FBPase showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes. Our inhibitors occupy the allosteric binding site and also extend into the dyad interface region of tetrameric FBPase. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8Product Details of 3034-22-8)

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.Product Details of 3034-22-8

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

In 2011,Thomas, Mathew; Huang, Wei-Sheng; Wen, David; Zhu, Xiaotian; Wang, Yihan; Metcalf, Chester A.; Liu, Shuangying; Chen, Ingrid; Romero, Jan; Zou, Dong; Sundaramoorthi, Raji; Li, Feng; Qi, Jiwei; Cai, Lisi; Zhou, Tianjun; Commodore, Lois; Xu, Qihong; Keats, Jeff; Wang, Frank; Wardwell, Scott; Ning, Yaoyu; Snodgrass, Joseph T.; Broudy, Marc I.; Russian, Karin; Iuliucci, John; Rivera, Victor M.; Sawyer, Tomi K.; Dalgarno, David C.; Clackson, Tim; Shakespeare, William C. published 《Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant》.Bioorganic & Medicinal Chemistry Letters published the findings.Related Products of 3034-22-8 The information in the text is summarized as follows:

Ponatinib (AP24534) was previously identified as a pan-BCR-ABL inhibitor that potently inhibits the T315I gatekeeper mutant, and has advanced into clin. development for the treatment of refractory or resistant CML. In this study, we explored a novel series of five and six membered monocycles as alternate hinge-binding templates to replace the 6,5-fused imidazopyridazine core of ponatinib. Like ponatinib, these monocycles are tethered to pendant toluanilides via an ethynyl linker. Several compounds in this series displayed excellent in vitro potency against both native BCR-ABL and the T315I mutant. Notably, a subset of inhibitors exhibited desirable PK and were orally active in a mouse model of T315I-driven CML. In the experiment, the researchers 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. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Related Products of 3034-22-8

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

In 2009,Uto, Yoshikazu; Ogata, Tsuneaki; Kiyotsuka, Yohei; Miyazawa, Yuriko; Ueno, Yuko; Kurata, Hitoshi; Deguchi, Tsuneo; Yamada, Makiko; Watanabe, Nobuaki; Takagi, Toshiyuki; Wakimoto, Satoko; Okuyama, Ryo; Konishi, Masahiro; Kurikawa, Nobuya; Kono, Keita; Osumi, Jun published 《Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part II: Identification of 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide and its biological evaluation》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 3034-22-8 The information in the text is summarized as follows:

The continuing investigation of SAR studies of 3-(2-hydroxyethoxy)-N-(5-benzylthiazol-2-yl)benzamides as stearoyl-CoA desaturase-1 (SCD-1) inhibitors was reported. A prior hit-to-lead effort resulted in the identification of I (R = OMe) as a potent and orally efficacious SCD-1 inhibitor. Further optimization of the structural motif resulted in the identification of I (R = NHEt) with sub-nanomolar IC50 in both murine and human SCD-1 inhibitory assays. This compound demonstrated a dose-dependent decrease in the plasma desaturation index in C57BL/6J mice on a non-fat diet after 7 days of oral administration. In addition to this study using 5-Bromothiazol-2-amine, there are many other studies that have used 5-Bromothiazol-2-amine(cas: 3034-22-8Application of 3034-22-8) was used in this study.

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.Application of 3034-22-8

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