Author: tianli

In 2020,Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry included an article by Acharya, Prachi T.; Jethava, Divya J.; Vasava, Mahesh S.; Bhavsar, Zeel A.; Bhoi, Manoj N.; Rajani, Dhanji P.; Patel, Hitesh D.. Formula: C7H5ClN2S. The article was titled 《Synthesis, docking study and biological evaluation of novel N-(1,3-benzothiazol-2-yl)-2-(pyridin-3-ylformohydrazido)acetamide derivatives》. The information in the text is summarized as follows:

A series of N-(1,3-benzothiazol-2-yl)-2-(pyridin-3-ylformohydrazido)acetamide derivatives I (R = H, OMe, OEt, OH, Cl, F; X = H, N) have been synthesized by facile and efficient conventional method. Mol. docking revealed that synthesized derivatives and target proteins are actively involved in the binding pattern and had a significant correlation with biol. activity. Mol. dynamics studies have also been performed and ADME parameters for the synthesized compounds determined Biol. evaluation of all synthesized compounds have been carried out in vitro for their antibacterial, antituberculosis and antifungal efficacy against various bacterial and fungal strains and H37Rv. The different studies indicate that newly synthesized compounds possess moderate to good biol. activities.6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Formula: C7H5ClN2S) 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.Formula: 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

Meng, Shuaiqi; Guo, Jia; Nie, Kaili; Schwaneberg, Ulrich; Tan, Tianwei; Xu, Haijun; Liu, Luo published an article on February 28 ,2019. The article was titled 《High throughput screening method for engineering P450 towards terminal hydroxylation of fatty acids》, and you may find the article in Journal of Biobased Materials and Bioenergy.Safety of ABTS Diammonium The information in the text is summarized as follows:

Terminal ω-hydroxy fatty acids are important industrial precursors for the synthesis of polyhydroxy fatty acids, nylons, and lactones. The cytochrome P 450 monooxygenases are able to catalyze hydroxylation of fatty acids for synthesis of terminal ω-hydroxy fatty acids. Directed evolution is the promising strategy to engineer the P 450 and shift its regioselectivity towards the terminal position. In this article, a high throughput screening method to detect terminal ω-hydroxy fatty acids for identifying P 450 variants with selectivity for terminal oxidation was developed and validated. A ω-hydroxy fatty acids specific fatty alc. oxidase (FAO) from Candida tropicalis was applied to quant. detect the products. The formation of hydrogen peroxide during the process of oxidation of ω-hydroxy fatty acids is coupled with horse radish peroxidase (HRP) for color reaction with the chromogenic substrate of 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid; ABTS) in 96 multi-well plates. The FAO-ABTS system was successfully applied to the detect the P 450 BM3 mutant capable of catalyzing the terminal ω-hydroxylation of pentadecanoic acid and palmitic acid. The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0Safety 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).Safety of ABTS Diammonium

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

《Site-Selective Thiolation of (Multi)halogenated Heteroarenes》 was written by Sandfort, Frederik; Knecht, Tobias; Pinkert, Tobias; Daniliuc, Constantin G.; Glorius, Frank. Recommanded Product: 3034-22-8 And the article was included in Journal of the American Chemical Society in 2020. The article conveys some information:

A general and simple strategy for the site-selective thiolation of various pharmaceutically relevant electron-rich heteroarenes with thiols is reported. This mild and reliable photocatalytic protocol enables C-S coupling at the most electron-rich position of the (multi)halogenated substrates, complementing established methodologies. Exptl. and computational studies suggest a radical chain mechanism with the key step being a homolytic aromatic substitution of the heteroaryl halide by an electrophilic thiyl radical, highlighting an underdeveloped reactivity mode. In the part of experimental materials, we found many familiar compounds, such as 5-Bromothiazol-2-amine(cas: 3034-22-8Recommanded Product: 3034-22-8)

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

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

《Effect of simultaneous dual-frequency ultrasound aided ethanolic pretreatment on drying kinetics, bioactive compounds, antioxidant activity, and physicochemical properties of apple slices using pulsed vacuum dryer》 was published in Journal of Food Process Engineering in 2020. These research results belong to Amanor-Atiemoh, Robert; Zhou, Cunshan; Mujumdar, Arun; Osae, Richard; Taiye Mustapha, Abdullateef; Wahia, Hafida; Sampson, Gilbert; Amoa-Owusu, Abigail; Ma, Haile. Reference of ABTS Diammonium The article mentions the following:

This work aims at investigating effect of different pretreatments and varied temperature on the drying kinetics, bioactive compounds, antioxidant activity, microstructure and functional group of apple slices using pulsed vacuum dryer. Pretreated apple slices (Ethanol, US + W, and US + E) dried at varied temperature (60, 70, and 80°C) were analyzed to determine total phenolic content (TPC), total flavonoid content (TFC), 1,1-diphenyl-2-picrylhydrazyl (DPPH+), 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid color, microstructure and FT-IR spectroscopy. The findings revealed that US + E pretreatment significantly decreased drying time. US + E pretreatment retained TPC, TFC, DPPH+ and ABTS+ than Ethanol, US + W, and control and was further corroborated by the observed peaks as revealed by the FT-IR spectroscopy. However, drying often leads to a reduction in quality parameters as well as degradation of nutritional components of the apple. Novel pretreatment techniques like ultrasonic aided ethanolic pretreatment preceding to apple drying provides an added advantage over conventional drying methods in that it reduces dehydration time as a result of faster moisture removal, lowers energy consumption, improves process efficiency leading to industrial competiveness and it also preserves the nutritional and sensorial parameters of dried apple slices. In addition to this study using ABTS Diammonium, there are many other studies that have used ABTS Diammonium(cas: 30931-67-0Reference of ABTS Diammonium) was used in this study.

ABTS Diammonium(cas: 30931-67-0) 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.Reference of ABTS Diammonium

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

《Facile preparation of dihydro-1,4-benzothiazine derivatives via oxidative ring-expansion of 2-aminobenzothiazoles with olefins》 was published in Chemical Communications (Cambridge, United Kingdom) in 2022. These research results belong to Sun, Qing; Bao, Xiaoguang. SDS of cas: 95-24-9 The article mentions the following:

A concise and efficient approach to prepare dihydro-1,4-benzothiazine derivatives I (R1 = H, 7-Br, 5,7-difluoro, 5-OMe, etc.; R2 = Ph, naphthalen-2-yl, ethyloxidanyl, etc.; R3 = H, Me, Ph), Et 9-cyano-3,3a,9,9a-tetrahydro-2H-benzo[b]furo[2,3-e][1,4]thiazine-6-carboxylate and Et 10-cyano-4b,10,10a,11-tetrahydrobenzo[b]indeno[2,1-e][1,4]thiazine-7-carboxylate is described via oxidative ring-expansion of 2-aminobenzothiazoles II with olefins R2CH=CHR3 under metal-free conditions. This protocol is applicable for a wide range of readily accessible 2-aminobenzothiazoles II and olefins with moderate-to-good yields. The [4+2] heteroannulation between the intermediacy of oxidative ring-opening of 2-aminobenzothiazoles II and olefins is suggested to rationalize the formation of the product. In the part of experimental materials, we found many familiar compounds, such as 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9SDS of cas: 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.SDS of cas: 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

Name: ABTS DiammoniumOn November 30, 2019 ,《The multicopper oxidase of Mycobacterium tuberculosis (MmcO) exhibits ferroxidase activity and scavenges reactive oxygen species in activated THP-1 cells》 appeared in International Journal of Medical Microbiology. The author of the article were Kinkar, Eyad; Kinkar, Ayat; Saleh, Mazen. The article conveys some information:

The MmcO protein of Mycobacterium tuberculosis is a membrane-associated multicopper oxidase. Its natural substrate(s) and its role in pathogenesis are not well characterized. A recent report proposes that MmcO contributes to copper resistance in M. tuberculosis during infection. We have expressed and reconstituted the active enzyme from inclusion bodies in E. coli. MmcO exhibits maximal activity against the exptl. substrate 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) or ABTS, at pH 4. The enzyme also exhibits ferroxidase activity at pH 4. Most notable was the finding that MmcO is able to scavenge the reactive oxygen species (ROS) generated by the xanthine/xanthine oxidase enzyme system. This ROS scavenging activity of MmcO was also evident against ROS generated by THP-1 cells. We propose that MmcO protects M. tuberculosis during infection against ROS attack in addition to providing copper resistance to the pathogen. The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0Name: ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Name: ABTS Diammonium

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

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