Month: October 2022

Name: 5-Bromothiazol-2-amineIn 2014 ,《Development of radamide analogs as Grp94 inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Muth, Aaron; Crowley, Vincent; Khandelwal, Anuj; Mishra, Sanket; Zhao, Jinbo; Hall, Jessica; Blagg, Brian S. J.. The article conveys some information:

Hsp90 isoform-selective inhibition is highly desired as it can potentially avoid the toxic side-effects of pan-inhibition. The current study developed selective inhibitors of one such isoform, Grp94, predicated on the chimeric and pan-Hsp90 inhibitor, radamide (RDA). Replacement of the quinone moiety of RDA with a Ph ring (2) was found to be better suited for Grp94 inhibition as it can fully interact with a unique hydrophobic pocket present in Grp94. An extensive SAR for this scaffold showed that substitutions at the 2- and 4-positions (8 and 27, resp.) manifested excellent Grp94 affinity and selectivity. Introduction of heteroatoms into the ring also proved beneficial, with a 2-pyridine derivative (38) exhibiting the highest Grp94 affinity (Kd = 820 nM). Subsequent cell-based assays showed that these Grp94 inhibitors inhibit migration of the metastatic breast cancer cell line, MDA-MB-231, as well as exhibit an anti-proliferative affect against the multiple myeloma cell line, RPMI 8226. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Name: 5-Bromothiazol-2-amine

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

Recommanded Product: 5-Bromothiazol-2-amineIn 2002 ,《Synthesis and Structure-Activity Relationships of Novel 7-Substituted 1,4-Dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic Acids as Antitumor Agents. Part 1》 was published in Journal of Medicinal Chemistry. The article was written by Tomita, Kyoji; Tsuzuki, Yasunori; Shibamori, Koh-ichiro; Tashima, Masanori; Kajikawa, Fumie; Sato, Yuji; Kashimoto, Shigeki; Chiba, Katsumi; Hino, Katsuhiko. The article contains the following contents:

Title compounds, e.g. I (R = H2NCH2CH2NH, 1-pyrrolidinyl, 3-hydroxy-1-pyrrolidinyl), possess moderate cytotoxic activity. Structure-activity relationships of title compounds were investigated by changing substituents at N-1 and C-7 positions and the core ring structure itself and evaluated the synthesized compounds against several murine and human tumor cell lines. The 2-thiazolyl group at the N-1 position of the naphthyridine structure is the best substituent for antitumor activity and regarding core ring structure, the naphthyridine derivative is the most active followed by pyridopyrimidine analog. At the C-7 position, aminopyrrolidine derivatives are more effective than other amines or thioether derivatives I (R = 3-amino-4-methoxy-1-pyrrolidinyl, 3-amino-3-methyl-1-pyrrolidinyl, 3-aminopyrrolidinyl) were determined to be effective in vitro and in vivo antitumor assays, and their activity was comparable to that of etoposide.5-Bromothiazol-2-amine(cas: 3034-22-8Recommanded Product: 5-Bromothiazol-2-amine) 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.Recommanded Product: 5-Bromothiazol-2-amine

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

COA of Formula: C3H3BrN2SIn 2017 ,《Synthesis of Brominated Thiazoles via Sequential Bromination-Debromination Methods》 was published in Journal of Organic Chemistry. The article was written by Uzelac, Eric J.; Rasmussen, Seth C.. The article contains the following contents:

The synthesis of the full family of bromothiazoles has been revisited in order to update and optimize their production The species reported include 2-bromothiazole, 4-bromothiazole, 5-bromothiazole, 2,4-dibromothiazole, 2,5-dibromothiazole, 4,5-dibromothiazole, and 2,4,5-tribromothiazole, the majority of which are produced via sequential bromination and debromination steps. This complete family can now be produced without the use of elemental bromine, and the presented methods have allowed the phys. and NMR spectroscopic characterization of the full family to be reported for the first time. In the experimental materials used by the author, we found 5-Bromothiazol-2-amine(cas: 3034-22-8COA of Formula: C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) 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).COA of Formula: C3H3BrN2S

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

《Commercialized Sesame Oil Analysis: Quality Characterization and Oxidative Stability of Blended Sesame Oil》 was written by Chau, Chi-Fai; Ciou, Jhih-Ying; Wu, Chung-Li. Recommanded Product: 30931-67-0 And the article was included in ACS Food Science & Technology on August 20 ,2021. The article conveys some information:

Sesame oil is a high quality edible oil in Asia with unique flavor and aroma. However, sesame oil is more expensive than soybean oil; therefore, both sesame and soybean oil are blended to reduce costs. In this study, we performed quality characterization anal. of sesame oil (SeO) and sesame oil blended with soybean oil (B-SeO). In our results, fatty acid composition was not significantly different; however, acid, anisidine, peroxide, and total oxidation values of B-SeO were lower than SeO; B-SeO was found to meet CODEX quality standards for cold-pressed oil; 1,1-diphenyl-2-trinitrophenylhydrazine, 2,2-diazo-bis(3-ethyl-benzothiazole-6-sulfonic acid) diammonium salt scavenging capacity, and ferric reducing antioxidant power values of the SeO and B-SeO were in the following ranges 23.72-42.66%, 26.4-29.62%, and 0.44-0.57%, resp.; by following the Arrhenius equation, activation energies for oxidative stability of the two products ranged between 95.51 and 120.34 kJ/mol; antioxidant activities of these oil products were correlated with Maillard reaction products. In conclusion, it was determined that blending sesame oil with soybean oil improved the quality characterization and increased the applications and uses of sesame oil products. In the experiment, the researchers used ABTS Diammonium(cas: 30931-67-0Recommanded Product: 30931-67-0)

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.Recommanded Product: 30931-67-0

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

COA of Formula: C18H24N6O6S4On October 31, 2020 ,《Synthesis of selenium-containing galactomannan-stabilized nanocomposites with particle size-sensitive antiradical activity》 appeared in Russian Chemical Bulletin. The author of the article were Lesnichaya, M. V.; Sapozhnikov, A. N.; Sukhov, B. G.. The article conveys some information:

Water-soluble hybrid nanocomposites were synthesized for the first time with the use of industrial crystalline selenium (gray powder selenium) activated in a hydrazine hydrate-alkali base-recovery system. The obtained nanocomposites consist of the selenium nanoparticles 13.0-24.0 nm in size stabilized by biocompatible natural polysaccharide galactomannan. The structures of the nanocomposites were characterized by a complex of physicochem. methods (X-ray diffraction anal., transmission electron microscopy, and IR spectroscopy). The pronounced antioxidant activity of the prepared nanocomposites against free radicals of 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt was found, and its value correlates with the particle size of selenium. The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0COA of Formula: C18H24N6O6S4)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.COA of Formula: C18H24N6O6S4

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

Recommanded Product: ABTS DiammoniumOn March 31, 2019, Ates, Fadime; Sahin, Selin; Ilbay, Zeynep; Kirbaslar, S. I. published an article in Waste and Biomass Valorization. The article was 《A Green Valorisation Approach Using Microwaves and Supercritical CO2 for High-Added Value Ingredients from Mandarin (Citrus deliciosa Tenore) Leaf Waste》. The article mentions the following:

The present study aims to increase the efficiency of a resource from waste to health by valorization of it through cleaner, eco-friendly and less energy-consuming tech. processes such as microwave-asissted (MAE) and supercritical fluid (SFE) extractions On the other hand, optimization of the processes have been applied utilizing multivariate statistic technique such as Response surface Methodol. (RSM) in order to consider any possible interaction between variables with less number of experiments as well as to model a response affected by several variables. The outcome of the present study indicates that the optimum conditions for MAE were 275 W of microwave power together with 2 g mandarin leaf for 45 s; regarding SFE, 50 °C, 200 bar and 0.39 mL/min was found as the optimal condition to obtain the maximum yields of each dependent variable such as total phenolic material (TPM) and total flavonoid material (TFM), resp. Addnl., antioxidant activity values measured by several methods such as cupric ion reducing antioxidant capacity (CUPRAC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) were correlated pos. with both TPM and TFM in the leaf extracts Furthermore, scanning electron microscope (SEM) images indicated cell wall disruption in all the treatment groups compared to untreated samples. In the experiment, the researchers used ABTS Diammonium(cas: 30931-67-0Recommanded Product: ABTS Diammonium)

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

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

In 2020,Catalysis Science & Technology included an article by Koohgard, Mehdi; Hosseinpour, Zeinab; Sarvestani, Abdollah Masoudi; Hosseini-Sarvari, Mona. Reference of 6-Chlorobenzothiazol-2-ylamine. The article was titled 《ARS-TiO2 photocatalyzed direct functionalization of sp2 C-H bonds toward thiocyanation and cyclization reactions under visible light》. The information in the text is summarized as follows:

An ARS-TiO2 photocatalyst has been prepared by a simple method through stirring a mixture of ARS and TiO2 at room temperature in the dark to extend the photocatalytic response of titanium dioxide toward the visible light spectrum. The synergic effect of ARS and TiO2 in the photocatalyst system has catalyzed direct C-H functionalization of sp2 C-H bonds toward thiocyanation and cyclization reactions. Several aromatic and heteroaromatic scaffolds (2-phenylamino-thiazoles I (R = H, 2-Cl, 4-Ph, etc.), phenols R1OH (R1 = Ph, 3-ethylphenyl, 2-formylphenyl, etc.), anilines R2C6H4N(R3)(R4) (R2 = 2-Me, 3-Cl, 3-OMe, etc.; R3 = H, Me, Et, Ph; R4 = H, Me, Et), indoles II (R5 = H, Me; R6 = H, Me; R7 = H, 5-MeO, 6-methoxycarbonyl, 5-Br, 5-Me) and pyrroles such as 1H-pyrrole and 1-methyl-1H-pyrrole) were treated with the ammonium thiocyanate at room temperature Thiocyanation of phenol and synthesis of 2-aminobenzothiazole derivatives III (R8 = Me, I, prop-1-en-2-yl, etc.) under visible light are presented.6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Reference 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.Reference 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

The author of 《Copper-catalyzed one-pot coupling reactions of aldehydes (ketones), tosylhydrazide and 2-amino(benzo)thiazoles: An efficient strategy for the synthesis of N-alkylated (benzo)thiazoles》 were Xie, Zengyang; Chen, Ruijiao; Ma, Mingfang; Kong, Lingdong; Liu, Jun; Wang, Cunde. And the article was published in Applied Organometallic Chemistry in 2019. Computed Properties of C7H5ClN2S The author mentioned the following in the article:

An efficient and practical C-N bond formation methodol. for the synthesis of N-(alkyl)benzothiazoles I [R = H, 4-Me, 6-Br, etc.; R1 = n-Pr, Ph, 4-MeOC6H4, etc.] and N-(alkyl)thiazoles II [R2 = H, Me; R3 = Ph, 2-MeC6H4, 2-naphthyl, etc.; R2R3 = (CH2)5; R4 = H, 4-Me, 5-Me] was developed via Cu-catalyzed one-pot two-step cross-coupling of 2-aminobenzothiazoles/2-aminothiazoles and aldehydes/ketones with tosylhydrazide. This cross-coupling reaction proceeded smoothly and tolerated a broad range of functional groups. A variety of functionalized benzothiazoles/thiazoles were obtained in moderate to high yields. Notably, gram-scale synthesis of fanetizole (anti-inflammatory drug) was also realized through this protocol. In the experimental materials used by the author, we found 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 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 2018,Liu, Juan-Juan; Lu, Yan-Ju; Zhao, Zhen-Dong; Xu, Shi-Chao; Bi, Liang-Wu published 《Synthesis and Cytotoxic Activity of Amides from Isopimaric Acid》.Chemistry of Natural Compounds published the findings.Name: 5-Bromothiazol-2-amine The information in the text is summarized as follows:

The amide derivatives were synthesized from isopimaric acid and characterized by spectroscopy. These amides were examined in vitro for their cytotoxic activity against four cancer cell lines. The majority of the screened compounds displayed better inhibitory activity than isopimaric acid, and many amides displayed promising cytotoxic activity against hepatocarcinoma (HepG-2), breast carcinoma (MDA-MB-231), and prostate adenocarcinoma (PC-3). The substituent type, number, and position in the benzene and heterocyclic rings have an important influence on cytotoxicity against the three tested cancer cell lines. In the experimental materials used by the author, we found 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Name: 5-Bromothiazol-2-amine

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

COA of Formula: C7H5ClN2SOn November 27, 2019 ,《Chagas Disease Drug Discovery: Multiparametric Lead Optimization against Trypanosoma cruzi in Acylaminobenzothiazole Series》 appeared in Journal of Medicinal Chemistry. The author of the article were Fleau, Charlotte; Padilla, Angel; Miguel-Siles, Juan; Quesada-Campos, Maria T.; Saiz-Nicolas, Isabel; Cotillo, Ignacio; Cantizani Perez, Juan; Tarleton, Rick L.; Marco, Maria; Courtemanche, Gilles. The article conveys some information:

Acylaminobenzothiazole hits were identified as potential inhibitors of T. cruzi replication, a parasite responsible for Chagas Disease. We selected compound 1, N-(6-chlorobenzo[d]thiazol-2-yl)cyclopropanecarboxamide, for lead optimization, aiming to improve in parallel its anti-T. cruzi activity (IC50 = 0.630μM) and its human metabolic stability (human clearance = 9.57mL/min/g). A total of 39 analogs of 1 were synthesized and tested in vitro. We established a multiparametric structure activity relationship, allowing optimization of both anti-parasite activity, physicochem. parameters and ADME properties. We identified compound 50, N-(5-Fluoro-6-(trifluoromethyl)benzothiazol-2-yl)cyclopropanecarboxamide, as an advanced lead with an improved anti-T. cruzi activity in vitro (IC50 = 0.079μM), an enhanced metabolic stability (Human Clearance = 0.413mL/min/g) and opportunity for oral route of administration. After tolerability assessment, compound 50 demonstrated a promising in vivo efficacy. In the experiment, the researchers used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9COA of Formula: 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.COA of Formula: 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