Month: October 2022

Ghavidel Hajiagha, N.; Mahmoudi, A.; Sazegar, M. Reza; Pouramini, Mostafa M. published an article on January 15 ,2019. The article was titled 《Synthesis of cobalt-modified MSN as a model enzyme: Evaluation of the peroxidatic performance》, and you may find the article in Microporous and Mesoporous Materials.Safety of ABTS Diammonium The information in the text is summarized as follows:

The cobalt incorporated mesoporous silica nanomaterials (Co-MSN) with different ratios of Si/Co in the framework were synthesized. The as-obtained products were characterized by x-ray diffraction anal. (XRD), FTIR spectroscopy (FTIR), x-ray fluorescence (XRF), field emission SEM (FESEM), transmission electron microscope (TEM), N2 adsorption/desorption (BET) and UV-visible spectroscopic techniques. The effect of the various content of Co incorporated into the framework on the catalytic activity was studied. The Co-MSN samples exhibited an excellent catalytic activity toward the reduction of hydrogen peroxide (H2O2) and the oxidation of 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) as a chromogenic substrate and followed Michaelis-Menten kinetics. It means that they have intrinsic peroxidase-like activity. The Co-MSN catalyst with Si/Co=75 (as the optimum ratio), has the higher affinity to ABTS and H2O2 and higher catalytic efficiency. These features made this nanocatalyst suitable to apply for the determination of H2O2 and glucose. The linear range for detecting H2O2 was from 22.5μM to 0.2mM with a detection limit of 6.7μM. Coupled with glucose oxidase, the Co-MSN(75) was successfully used for the determination of glucose with the linear range of 11.6μM-0.1mM and a detection limit of 3.5μM. In addition to this study using ABTS Diammonium, there are many other studies that have used ABTS Diammonium(cas: 30931-67-0Safety of ABTS Diammonium) was used in this study.

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Safety of ABTS Diammonium

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

In 2014,Khanfar, Mohammad A.; Quinti, Luisa; Wang, Hua; Choi, Soo Hyuk; Kazantsev, Aleksey G.; Silverman, Richard B. published 《Development and characterization of 3-(arylsulfamoyl)benzamides as potent and selective SIRT2 inhibitors》.European Journal of Medicinal Chemistry published the findings.Synthetic Route of C3H3BrN2S The information in the text is summarized as follows:

Inhibitors of sirtuin-2 deacetylase (SIRT2) have been shown to be protective in various models of Huntington’s disease (HD) by decreasing polyglutamine aggregation, a hallmark of HD pathol. The present study was directed at optimizing the potency of SIRT2 inhibitors containing the neuroprotective sulfobenzoic acid scaffold and improving their pharmacol. To achieve that goal, 176 analogs were designed, synthesized, and tested in deacetylation assays against the activities of major human sirtuins SIRT1-3. This screen yielded 15 compounds with enhanced potency for SIRT2 inhibition and 11 compounds having SIRT2 inhibition equal to reference compound AK-1. The newly synthesized compounds also demonstrated higher SIRT2 selectivity over SIRT1 and SIRT3. These candidates were subjected to a dose-response bioactivity assay, measuring an increase in α-tubulin K40 acetylation in two neuronal cell lines, which yielded five compounds bioactive in both cell lines and eight compounds bioactive in at least one of the cell lines tested. These bioactive compounds were subsequently tested in a tertiary polyglutamine aggregation assay, which identified five inhibitors. ADME properties of the bioactive SIRT2 inhibitors (e.g., I) were assessed, which revealed a significant improvement of the pharmacol. properties of the new entities, reaching closer to the goal of a clin.-viable candidate. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Synthetic Route of C3H3BrN2S)

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.Synthetic Route of C3H3BrN2S

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

In 2016,Gogliotti, Rocco D.; Blobaum, Anna L.; Morrison, Ryan M.; Daniels, J. Scott; Salovich, James M.; Cheung, Yiu-Yin; Rodriguez, Alice L.; Loch, Matthew T.; Conn, P. Jeffrey; Lindsley, Craig W.; Niswender, Colleen M.; Hopkins, Corey R. published 《Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)》.Bioorganic & Medicinal Chemistry Letters published the findings.Reference of 5-Bromothiazol-2-amine The information in the text is summarized as follows:

Herein the authors report the synthesis and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as novel pos. allosteric modulators of mGlu4. The authors detail the authors’ work towards finding Ph replacements for the core scaffold of previously reported Ph sulfonamides and Ph sulfone compounds The authors’ efforts culminated in the identification of N-(1-((3,4-dimethylphenyl)sulfonyl)-1H-pyrrol-3-yl)picolinamide as a potent PAM of mGlu4. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Reference of 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Reference of 5-Bromothiazol-2-amine

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

《Design, synthesis, and biological evaluation of [1,2,4]triazolo[4,3-a] pyrazine derivatives as novel dual c-Met/VEGFR-2 inhibitors》 was published in Frontiers in Chemistry (Lausanne, Switzerland) in 2022. These research results belong to Liu, Xiaobo; Li, Yuzhen; Zhang, Qian; Pan, Qingshan; Zheng, Pengwu; Dai, Xinyang; Bai, Zhaoshi; Zhu, Wufu. HPLC of Formula: 144060-98-0 The article mentions the following:

In this study, a series of novel [1,2,4]triazolo[4,3-a]pyrazine derivatives, I (R = 4-methyl-2-phenyl-1,3-thiazol-5-yl, 4-(4-methyl-1,3-thiazol-2-yl)pyridine, 3-(thiophen-2-yl)-1H-pyrazol-5-yl, etc.; R1 = H, Me; X = H, F) evaluated for their inhibitory activities toward c-Met/VEGFR-2 kinases and antiproliferative activities against tested three cell lines in vitro was designed and synthesized. Most of the compounds I showed satisfactory activity compared with lead compound foretinib. Among them, the most promising compound I (R = 1-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrazol-4-yl, R1 = Me; X = F) (II) exhibited excellent antiproliferative activities against A549, MCF-7, and Hela cancer cell lines with IC50 values of 0.98 ± 0.08, 1.05 ± 0.17, and 1.28 ± 0.25μM, resp., as well as excellent kinase inhibitory activities (c-Met IC50 = 26.00 nM and VEGFR-2 IC50 = 2.6μM). Moreover, compound II inhibited the growth of A549 cells in G0/G1 phase in a dose-dependent manner, and induced the late apoptosis of A549 cells. Its intervention on intracellular c-Met signaling of A549 was verified by the result of Western blot. Fluorescence quant. PCR showed that compound 17l inhibited the growth of A549 cells by inhibiting the expression of c-Met and VEGFR-2, and its hemolytic toxicity was low. Mol. docking and mol. dynamics simulation indicated that compound II could bind to c-Met and VEGFR-2 protein, which was similar to that of foretinib. In the experiment, the researchers used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0HPLC of Formula: 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.HPLC of Formula: 144060-98-0

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

《N-thiophenylethyl-2,2-dichloro-1-cyclopropanecarboxamides: modification of the amide part of carpropamid and examination of fungicidal activity》 was published in Journal of Pesticide Science (Tokyo, Japan) in 2009. These research results belong to Kagabu, Shinzo; Shimizu, Maiko; Mori, Masaru; Kurahashi, Yoshio; Yamaguchi, Isamu. Quality Control of 2-(2-Chlorothiazol-5-yl)acetonitrile The article mentions the following:

The synthetic route for a halo-substituted thiophenylethyl variant of blasticide carpropamid is described. First, halo-substituted acetylthiophene was homologated to thiophenylacetic acid using Pb(OAc)4 and BF3OEt2, followed by reduction to CH2CH2OH with NaBH4/I2 or BH3Me2S, and then to the azide via the tosylate. The azide was transformed to the amine using triphenylphosphine, which was then allowed to react with the corresponding acyl chloride to yield the final amide product. Fungicidal tests of 50 related products for gray mold and downy mildew on cucumber, and leaf rust and powdery mildew on wheat were conducted in 500 mg/l on pot. Many compounds showed efficacy to control these plant diseases. It should be noted that several blasticide-oriented compounds displayed high control effectiveness on downy mildew. In the experiment, the researchers used 2-(2-Chlorothiazol-5-yl)acetonitrile(cas: 865660-15-7Quality Control of 2-(2-Chlorothiazol-5-yl)acetonitrile)

2-(2-Chlorothiazol-5-yl)acetonitrile(cas: 865660-15-7) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Quality Control of 2-(2-Chlorothiazol-5-yl)acetonitrile

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

《Organocatalytic asymmetric [4+2] cyclization of 2-benzothiazolimines with azlactones: access to chiral benzothiazolopyrimidine derivatives》 was published in Chemical Communications (Cambridge, United Kingdom) in 2020. These research results belong to Ni, Qijian; Wang, Xuyang; Xu, Fangfang; Chen, Xiaoyun; Song, Xiaoxiao. Application of 95-24-9 The article mentions the following:

An organocatalytic asym. domino Mannich/cyclization reaction between 2-benzothiazolimines I (R = H, 6-OMe, 5-Br, etc.; R1 = Ph, 4-MeC6H4, 2-thienyl, etc.) with azlactones II (R2 = Me, Bn, 4-FC6H4CH2, etc.; R3 = Ph, 4-MeC6H4, 1-naphthyl, etc.) has been successfully developed. With the bifunctional squaramide catalyst, this formal [4+2] cyclization occurs with good to high yields and excellent stereoselectivities (up to 99% ee, >20 : 1 dr), providing an efficient and mild access to chiral benzothiazolopyrimidines III (R = H, 6-OMe, 5-Br, etc.; R1 = Ph, 4-MeC6H4, 2-thienyl, etc.; R2 = Me, Bn, 4-FC6H4CH2, etc.; R3 = Ph, 4-MeC6H4, 1-naphthyl, etc.) bearing adjacent tertiary and quaternary stereogenic centers. The results came from multiple reactions, including the reaction of 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

《Phytochemical composition and biological activity of Neurada procumbens L. growing in southern Algeria》 was published in Journal of Food Processing and Preservation in 2020. These research results belong to Chelalba, Imane; Benchikha, Naima; Begaa, Samir; Messaoudi, Mohammed; Debbeche, Hanane; Rebiai, Abdelkrim; Youssef, Fadia S.. Quality Control of ABTS Diammonium The article mentions the following:

Neurada procumbens L. (Neuradaceae) is one of the most popular plants in the province of El-Oued in south-eastern Algeria. This study aimed to determine the antioxidant effectiveness of the 80% methanol extract of the aerial parts of the plant via the study of three-way antioxidant activity namely, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), Catalase activity (CAT), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assays in addition to examining its inhibitory capacity on the proliferation of hepatic (HepG2) and colon cancer (HCT116) cells. Chem. profiling of the major constituents of its extract was tentatively done using LC-MS in addition to quant. determination of phenols, flavonoids, and chem. mineral elements by Inductively coupled plasma-optical emission spectrometry technique (ICP-OES). Practical applications : UHPLC/MS profiling resulted in the tentative identification of 14 compounds including fatty acids, flavones, flavonoids and sesquiterpenes. ICP-OES technique showed that Algerian N. procumben represents a potential source for essential macronutrient like Na, Fe, Ca, and K, it is also a rich source of phenolic compounds evidenced by its high total phenol content (56.23 mg GAE/g extract) and high total flavonoid content (30.10 mg RE/g extract). It also revealed a significant antioxidant potential in DPPH, CAT, and ABTS assays with EC50 equals to 75.84 mg TE/g extract, 136.55 mg eq. AG/g and 92.06 mg TE/g extract, resp., with no cytotoxic effect on hepatic and colon cancer cells revealing its relative safety. Thus, it can be concluded that N. procumbens L., acts as a promising source of antioxidants owing to its richness with phenolic compounds The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0Quality Control of ABTS Diammonium)

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).Quality Control of ABTS Diammonium

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

Related Products of 152937-04-7On September 15, 2012 ,《Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Malmstroem, Jonas; Viklund, Jenny; Slivo, Can; Costa, Ana; Maudet, Mickael; Sandelin, Catrin; Hiller, Goesta; Olsson, Lise-Lotte; Aagaard, Anna; Geschwindner, Stefan; Xue, Yafeng; Vasaenge, Mervi. The article contains the following contents:

4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (I) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand I with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water mol. The results came from multiple reactions, including the reaction of 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Related Products of 152937-04-7)

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.Related Products of 152937-04-7Their 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

Related Products of 95-24-9On October 31, 2021 ,《Design, Synthesis and Biological Evaluation of a Novel Series of Thiadiazole- Based Anticancer Agents as Potent Angiogenesis Inhibitors》 appeared in Anti-Cancer Agents in Medicinal Chemistry. The author of the article were Altug-Tasa, Burcugul; Kaya-Cavusoglu, Betul; Koparal, Ayse T.; Turan, Gulhan; Koparal, Ali S.; Kaplancikli, Zafer A.. The article conveys some information:

Thiadiazole has attracted a great deal of interest as a versatile heterocycle for the discovery and development of potent anticancer agents. Thiadiazole derivatives exert potent antitumor activity against a variety of human cancer cell lines through various mechanisms. The goal of this work was to design and synthesize thiadiazole-based anticancer agents with anti-angiogenic activity. N-aryl-2-[(5-(aryl)amino-1,3,4-thiadiazol-2-yl)thio]acetamides (4a-r) were synthesized via the reaction of 5-(aryl)amino-1,3,4-thiadiazole-2(3H)-thiones with N-(aryl)-2-chloroacetamides in the presence of potassium carbonate. The compounds were investigated for their cytotoxic effects on three cancer (A549, HepG2, SH-SY5Y), two normal (HUVEC and 3T3-L1) cell lines using MTT and WST-1 assays. In order to examine whether the compounds have anti-angiogenic effects or not, HUVECs were cultured on matrigel matrix to create a vascular-like tube formation. Compounds 4d, 4m and 4n were more effective on A549 human lung adenocarcinoma cells than cisplatin. The IC50 values of compounds 4d, 4m and 4n for A549 cell line were found to be 7.82 ± 0.4, 12.5 ± 0.22, 10.1 ± 0.52 μM, resp. when compared with cisplatin (IC50= 20 ± 0.51 μM), while their IC50 values for HUVEC cell line were determined as 138.7 ± 0.84, 78 ± 0.44, 177.6 ± 0.2 μM, resp. after 48 h of the treatment. The concentrations (10-20-50 μM) of compounds 4d, 4e, 4l, 4m, 4n, 4q and 4r were found to inhibit vascular like tube formation. According to their anticancer and anti-angiogenic effects, compounds 4d, 4m and 4n may be potential anticancer agents for further in vivo studies. The experimental process involved the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Related Products 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.Related Products of 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

Davidsson, Oejvind; Nilsson, Kristina; Braanalt, Jonas; Andersson, Terese; Berggren, Kristina; Chen, Yantao; Fjellstroem, Ola; Graden, Henrik; Gustafsson, Linda; Hermansson, Nils-Olov; Jansen, Frank; Johannesson, Petra; Ohlsson, Bengt; Tyrchan, Christian; Wellner, Annika; Wellner, Eric; Oelwegaard-Halvarsson, Maria published an article on February 15 ,2020. The article was titled 《Identification of novel GPR81 agonist lead series for target biology evaluation》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Recommanded Product: 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine The information in the text is summarized as follows:

GPR81 is a novel drug target that is implicated in the control of glucose and lipid metabolism The lack of potent GPR81 modulators suitable for in vivo studies has limited the pharmacol. characterization of this lactate sensing receptor. We performed a high throughput screen (HTS) and identified a GPR81 agonist chem. series containing a central acyl urea scaffold linker. During SAR exploration two addnl. new series were evolved, one containing cyclic acyl urea bioisosteres and another a central amide bond. These three series provide different selectivity and physicochem. properties suitable for in-vivo studies. In the experiment, the researchers used many compounds, for example, 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine(cas: 97817-23-7Recommanded Product: 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine)

4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine(cas: 97817-23-7) 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: 4,5,6,7-Tetrahydro-thiazolo[5,4-c]pyridin-2-ylamine

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