Day: October 14, 2022

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

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

Reference of 2-Bromo-6-fluorobenzothiazoleOn October 9, 2003 ,《Design and synthesis of pyrrolidine-5,5′-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability》 was published in Journal of Medicinal Chemistry. The article was written by Borthwick, Alan D.; Davies, Dave E.; Ertl, Peter F.; Exall, Anne M.; Haley, Terry M.; Hart, Graham J.; Jackson, Deborah L.; Parry, Nigel R.; Patikis, Angela; Trivedi, Naimisha; Weingarten, Gordon G.; Woolven, James M.. The article contains the following contents:

A series of chiral, (S)-proline-α-methylpyrrolidine-5,5-trans-lactam serine protease inhibitors has been developed as antivirals of human cytomegalovirus (HCMV). The SAR of the functionality on the proline nitrogen has shown that derivatives of para-substituted Ph ureas > para-substituted Ph sulfonamides > para-substituted Ph carboxamide for activity against HCMV δAla protease, producing para-substituted Ph ureas with single figure nM potency (Ki) against the viral enzyme. The SAR of the functionality on the lactam nitrogen has defined the steric and electronic requirements for high human plasma stability while retaining good activity against HCMV protease. The combination of high potency against HCMV δAla protease and high human plasma stability has produced compounds with significant in vitro antiviral activity against human cytomegalovirus with the 6-hydroxymethyl benzothiazole derivative 72 being equivalent in potency to ganciclovir. The parent benzothiazole 56 had good pharmacokinetics in dogs with 29% bioavailability and good brain and ocular penetration in guinea pigs. The experimental part of the paper was very detailed, including the reaction process of 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Reference of 2-Bromo-6-fluorobenzothiazole)

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.Reference of 2-Bromo-6-fluorobenzothiazoleTheir 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

Recommanded Product: ABTS DiammoniumOn March 4, 2020, Gaikwad, Adwait; Hlushko, Hanna; Karimineghlani, Parvin; Selin, Victor; Sukhishvili, Svetlana A. published an article in ACS Applied Materials & Interfaces. The article was 《Hydrogen-Bonded, Mechanically Strong Nanofibers with Tunable Antioxidant Activity》. The article mentions the following:

We report on mech. strong, water-insoluble hydrogen-bonded nanofiber mats composed of a hydrophilic polymer and a natural polyphenol that exhibit prolonged antioxidant activity. The high performance of fibrous mats resulted from the formation of a network of hydrogen bonds between a low-mol.-weight polyphenol (tannic acid, TA) and a water-soluble polymer (polyvinylpyrrolidone, PVP) and could be precisely controlled by the TA-to-PVP ratio. Dramatic enhancement (5- to 10-fold) in tensile strength, toughness, and Young’s moduli of the PVP/TA fiber mats (as compared to those of pristine PVP fibers) was achieved at the maximum d. of hydrogen bonds, which occurred at ∼0.2-0.4 M fractions of TA. The formation of hydrogen bonds was confirmed by an increase in the glass-transition temperature of the polymer after binding with TA. When exposed to water, the fibers exhibited composition- and pH-dependent stabilities, with the TA-enriched fibers fully preserving their integrity in acidic and neutral media. Importantly, the fiber mats exhibited strong antioxidant activity with dual (burst and prolonged) activity profiles, which could be controlled via fiber composition, a feature useful for controlling radical-scavenging rates in environmental and biol. applications. In addition to this study using ABTS Diammonium, there are many other studies that have used ABTS Diammonium(cas: 30931-67-0Recommanded Product: ABTS Diammonium) was used in this study.

ABTS Diammonium(cas: 30931-67-0) 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).Recommanded Product: ABTS Diammonium

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

Reference of 6-Morpholinobenzo[d]thiazol-2-amineOn October 30, 2014 ,《Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents》 was published in European Journal of Medicinal Chemistry. The article was written by Ma, Junjie; Chen, Dong; Lu, Kuan; Wang, Lihui; Han, Xiaoqi; Zhao, Yanfang; Gong, Ping. The article contains the following contents:

A series of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety were designed and synthesized and their cytotoxic activities against five cancer cell lines (NCI-H226, SK-N-SH, HT29, MKN45, and MDA-MB-231) were screened in vitro. Most of them showed moderate to excellent activity against all the tested cell lines. Two compounds (procaspase-3 EC50 = 1.42 μM and procaspase-3 EC50 = 0.25 μM) exhibited excellent antitumor activity with IC50 values ranging from 0.14 μM to 0.98 μM against all cancer cell lines, which were 1.8-8.7 times more active than the first procaspase activating compound (PAC-1) (procaspase-3 EC50 = 4.08 μM). The structure-activity relationship analyses indicated that the introduction of a lipophilic group (a benzyloxy or heteroaryloxy group) at the 4-position of the 2-hydroxyphenyl ring was beneficial to antitumor activity, and the presence of substituents containing nitrogen that are pos. charged at physiol. pH could also improve antitumor activity. It was also confirmed that the steric effect of the 4-position substituent of the benzyloxy group had a significant influence on cytotoxic activity.6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2Reference of 6-Morpholinobenzo[d]thiazol-2-amine) was used in this study.

6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Reference of 6-Morpholinobenzo[d]thiazol-2-amineTheir 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

Recommanded Product: 95-24-9On March 15, 2021, Al-Janabi, Ahmed S. M.; Elzupir, Amin O.; Yousef, Tarek A. published an article in Journal of Molecular Structure. The article was 《Synthesis, anti-bacterial evaluation, DFT study and molecular docking as a potential 3-chymotrypsin-like protease (3CLpro) of SARS-CoV-2 inhibitors of a novel Schiff bases》. The article mentions the following:

New Schiff bases (L1H) I (I), (L2H) II (II), (L3H) III (III) were synthesized by reaction of 2-benzoylpyridine with different amines (2-amino-6-chlorobenzothiazole, isonicotinohydrazide and N1-(naphthalen-1-yl)ethane-1,2-diamine) and characterized by 1H-NMR, 13C-NMR, IR mass spectroscopy and elemental anal. The compounds (I), (II) and (III) were assayed by the disk diffusion method for anti-bacterial against five pathogenic bacteria species (Staphylococcus aureus, Micrococcus luteus, Staphylococcus pyogenes, Bacillus subtilis, and E. coli). All prepared Schiff bases (I), (II) and (III) showed good activity compared to pos. control (streptomycin). Moreover the L3H showed the highest activity against S. aureus, and M. luteus than the other compounds and streptomycin. In addnl. mol. docking studies with 3-chymotrypsin-like protease (3CLpro), the essential enzyme for SARS-CoV-2 proliferation. The rest of compounds have shown promising results as 3CLpro inhibitors interacting with the active sites of the enzymes. Finally, DFT’s estimated electrostatic mol. potential results were used to illustrate the mol. docking findings. The DFT calculations showed that L3H has the highest dipole moment and electrophilicity index. Interestingly, L2H of the largest energy gap ΔE = 2.49 eV, there are several hydrophilic interactions that could facilitate the binding with the receptors. All of these parameters could be shared to significantly affect the protein sites of binding affinity with different extent. In the experiment, the researchers used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 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.Recommanded Product: 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

Agarwal, Charu; Hofmann, Tamas; Pasztory, Zoltan published their research in Chemical Engineering and Processing on February 28 ,2021. The article was titled 《Low-frequency, green sonoextraction of antioxidants from tree barks of Hungarian woodlands for potential food applications》.Reference of ABTS Diammonium The article contains the following contents:

The present work evaluates and compares the antioxidant capacities of bioactive constituents in the barks of ten common wood species from Hungary (Quercus rubra, Prunus serotina, Quercus robur, Betula pendula, Fraxinus excelsior, Robinia pseudoacacia, Carpinus betulus, Picea abies, Alnus glutinosa, Pinus sylvestris). Low-frequency ultrasound was used for intensification of extraction from the bark to obtain extracts rich in polyphenolic antioxidants with potential applications in the food industry. The extractions were carried out in different aqueous organic solvents- ethanol 80% and acetone 80% at optimized conditions. The overall antioxidant capacity of the extracts was estimated by the combined evaluation of Folin-Ciocalteu total phenol content (TPC), 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and ferric reducing ability of plasma (FRAP) assays using a scoring system. Aqueous ethanol had better extraction efficiency than aqueous acetone as a solvent medium. Of all the investigated species, Quercus robur showed the maximum antioxidant capacity with TPC of 105.88 ± 17.75 mg GAE/g dw, DPPH (IC50) of 1.90 ± 0.10μg/mL, ABTS of 437.09 ± 36.22 mg TE/g dw and FRAP of 102.62 ± 8.69 mg AAE/g dw. The polyphenolic characterization of Quercus robur, Robinia pseudoacacia and Fraxinus excelsior was done by liquid chromatog./tandem mass spectrometry. In the part of experimental materials, we found many familiar compounds, such as ABTS Diammonium(cas: 30931-67-0Reference of ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Reference of ABTS Diammonium

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

In 2019,SAR and QSAR in Environmental Research included an article by Geronikaki, A.; Petrou, A.; Kartsev, V.; Eleftheriou, P.; Boga, R.; Bartolo, B.; Crespan, E.; Franco, G.; Maga, G.. Quality Control of 6-Chlorobenzothiazol-2-ylamine. The article was titled 《Molecular docking, design, synthesis and biological evaluation of novel 2,3-aryl-thiazolidin-4-ones as potent NNRTIs》. The information in the text is summarized as follows:

A series of thiazolidinone derivatives I [R1 = 6-Cl, 6-cyano, 6-(adamant-1-yl), 6-CF3, 4-Me-6-(adamant-1-yl), R2 = 4-F, 4-NO2, 2-F-6-Cl, 2,6-Cl2, 2,6-F2] and II [R3 = 4-(pyridin-2-yl)thiazol-2-yl, 5-ethyl-4-methylthiazol-2-yl] was designed based on a butterfly mimicking scaffold consisting of a substituted benzothiazolyl moiety connected with a substituted Ph ring via a thiazolidinone moiety. The most promising derivatives were selected using mol. docking anal. and PASS prediction program, synthesized and evaluated for HIV-1 RT inhibition. Five out of fifteen tested compounds exhibited good inhibitory action. It was observed that the presence of Cl or CN substituents at position 6 of the benzothiazole ring in combination with two fluoro atoms at the ortho-positions or a hydrogen acceptor substituent at the 4-position of the Ph ring were favorable for the HIV RT inhibitory activity. In addition to this study using 6-Chlorobenzothiazol-2-ylamine, there are many other studies that have used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Quality Control of 6-Chlorobenzothiazol-2-ylamine) 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.Quality Control of 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

Xia, Huan; Zhong, Xue; Li, Zhixian; Jiang, Yanbin published an article in Journal of Colloid and Interface Science. The title of the article was 《Palladium-mediated hybrid biocatalysts with enhanced enzymatic catalytic performance via allosteric effects》.Synthetic Route of C18H24N6O6S4 The author mentioned the following in the article:

High activity and stability of immobilized enzymes have been constant pursuits and critical challenges for decades. Herein, Cytochrome c (peroxidase, Cyt c) and its corresponding enzyme mimic (Pd nanoparticles) were combined and successfully embedded into a zeolitic imidazolate framework-8 (ZIF-8) to enhance the enzymic catalytic performance using a biomimetic mineralization approach. Owing to allosteric effects of Cyt c-Pd complexes, the as-synthesized Cyt c-Pd@ZIF-8 composites exhibit an increased turnover number (approx. 2.4-fold for kcat) and an enhanced catalytic efficiency (approx. 2.3-fold for kcat/KM) compared to free Cyt c; also the shielding effect of ZIF-8 endows enzyme with improved resistance against harsh conditions (e.g. high temperatures and organic solvents). The strategy, which integrates enzyme with its enzyme mimic derived from transition metal nanoparticles to enhance enzymic catalytic performances, may provide a versatile and facile technique for designing highly efficient and multi-functional bio-catalysts. 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. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Synthetic Route of C18H24N6O6S4

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