Tag: 200-300

Vantourout, Julien C.; Mason, Andrew M.; Yuen, Josephine; Simpson, Graham L.; Evindar, Ghotas; Kuai, Letian; Hobbs, Michael; Edgar, Emma; Needle, Saul; Bai, Xiaopeng; Wilson, Steve; Scott-Stevens, Paul; Traylen, William; Lambert, Kim; Young, Neil; Bunally, Shenaz; Summerfield, Scott G.; Snell, Richard; Lad, Rakesh; Shi, Eric; Skinner, Steven; Shewchuk, Lisa; Watson, Allan J. B.; Chung, Chun-wa; Pal, Sandeep; Holt, Dennis A.; Kallander, Lara S.; Prendergast, Joanne; Rivera, Katrina; Washburn, David G.; Harpel, Mark R.; Arico-Muendel, Christopher; Isidro-Llobet, Albert published their research in Bioconjugate Chemistry in 2021. The article was titled 《In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders》.Quality Control of Benzyl 2-bromoacetate The article contains the following contents:

Reducing the required frequence of drug dosing can improve the adherence of patients to chronic treatments. Hence, drugs with longer in vivo half-lives are highly desirable. One of the most promising approaches to extend the in vivo half-life of drugs is conjugation to human serum albumin (HSA). In this work, we describe the use of AlbuBinder 1, a small-mol. noncovalent HSA binder, to extend the in vivo half-life and pharmacol. of small-mol. BMP1/TLL inhibitors in humanized mice (HSA KI/KI). A series of conjugates of AlbuBinder 1 with BMP1/TLL inhibitors were prepared In particular, conjugate c showed good solubility and a half-life extension of >20-fold vs. the parent mol. in the HSA KI/KI mice, reaching half-lives of >48 h with maintained maximal inhibition of plasma BMP1/TLL. The same conjugate showed a half-life of only 3 h in the wild-type mice, suggesting that the half-life extension was principally due to specific interactions with HSA. It is envisioned that conjugation to AlbuBinder 1 should be applicable to a wide range of small mol. or peptide drugs with short half-lives. In this context, AlbuBinders represent a viable alternative to existing half-life extension technologies. The results came from multiple reactions, including the reaction of Benzyl 2-bromoacetate(cas: 5437-45-6Quality Control of Benzyl 2-bromoacetate)

Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is a synthetic chemical produced for industry from benzyl alcohol and acetic acid, but is also naturally present in the essential oils of many plants, including jasmine and ylang ylang.Quality Control of Benzyl 2-bromoacetate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《A Fluorescent Compound from the Exuviae of the Scorpion, Liocheles australasiae》 was written by Yoshimoto, Yusuke; Tanaka, Masato; Miyashita, Masahiro; Abdel-Wahab, Mohammed; Megaly, Alhussin M. A.; Nakagawa, Yoshiaki; Miyagawa, Hisashi. Name: 1,6-Dibromohexane And the article was included in Journal of Natural Products in 2020. The article conveys some information:

Most scorpions fluoresce under UV light. To date, two types of fluorescent compounds have been identified in scorpions, but it has been assumed that other unknown compounds may be responsible for the fluorescence. In this study, we isolated a fluorescent compound from the exuviae of the scorpion Liocheles australasiae identified as a macrocyclic diphthalate ester with a mol. mass of 496.2 Da. The same compound was also detected in extracts from four other scorpion species. This suggests that this compound is shared by multiple scorpion species, although its contribution to the cuticle fluorescence may be relatively small. The experimental part of the paper was very detailed, including the reaction process of 1,6-Dibromohexane(cas: 629-03-8Name: 1,6-Dibromohexane)

1,6-Dibromohexane(cas: 629-03-8) is generally used to introduce C6 spacer in the molecular architecture. Some of the examples are: synthesis of solvent processable and conductive polyfluorene ionomers for alkaline fuel cell applications; synthesis of cross-linkable regioregular poly(3-(5-hexenyl)thiophene) (P3HNT) for stabilizing the film morphology in polymer photovoltaic cells.Name: 1,6-Dibromohexane

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Multiple Enhancement Effects of Crown Ether in Tröger’s Base Polymers on the Performance of Anion Exchange Membranes》 was published in ACS Applied Materials & Interfaces in 2020. These research results belong to Yang, Qian; Cai, Yuan Yuan; Zhu, Zhao Yu; Sun, Li Xuan; Choo, Yvonne Shuen Lann; Zhang, Qiu Gen; Zhu, Ai Mei; Liu, Qing Lin. Recommanded Product: 1,6-Dibromohexane The article mentions the following:

The development of anion exchange membranes (AEMs) is hindered by the trade-off of ionic conductivity, alk. stability, and mech. property. Troger’s base polymers (Tb-polymers) are recognized as promising membrane materials to overcome these obstacles. Herein, the AEMs made from Tb-poly(crown ether)s (Tb-PCEs) show good comprehensive performance. The influence of crown ether on the conductivity and alk. stability of AEMs has been investigated in detail. The formation of hydronium ion-crown ether complexes and an obvious microphase separated structure formed by the existence of crown ether can enhance the conductivity of the AEMs. The maximum ionic conductivity of 141.5 mS cm-1 is achieved from the Tb-PCEs based AEM (Tb-PCEs-1) at 80 oC under 100% humidity. The ion-dipole interaction of the Na+ with crown ether can protect the quaternary ammonium from the attack of OH- to improve the alk. stability of AEMs. After 480 h alk. treatment, the ionic conductivity of Tb-PCEs-1 only decreases by 6%. The single cell fabricated by the Tb-PCEs-1 shows a peak power d. of 0.202 W cm-2 at 80 oC. The prominent physicochem. properties are attributed to the well-developed microstructure of the Tb-PCEs, as revealed by TEM, AFM and SAXS observations. In addition to this study using 1,6-Dibromohexane, there are many other studies that have used 1,6-Dibromohexane(cas: 629-03-8Recommanded Product: 1,6-Dibromohexane) was used in this study.

1,6-Dibromohexane(cas: 629-03-8) is generally used to introduce C6 spacer in the molecular architecture. Some of the examples are: synthesis of pyrrolo-tetrathiafulvalene molecular bridge (6PTTF6) to study redox switching behavior of single molecules; synthesis of water-soluble thermoresponsive polylactides.Recommanded Product: 1,6-Dibromohexane

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Shifted Selectivity in Protonation Enables the Mild Deuteration of Arenes Through Catalytic Amounts of Bronsted Acids in Deuterated Methanol》 was published in Journal of Organic Chemistry in 2020. These research results belong to Fischer, Oliver; Hubert, Anja; Heinrich, Markus R.. Quality Control of 1-Bromo-3,4,5-trimethoxybenzene The article mentions the following:

Taking advantage of the “”differentiating effect”” of the solvent methanol, deuterations of electron-rich aromatic systems can be carried out under mild acid catalysis and thus under far milder conditions than known so far. The exceptional functional group tolerance observed under the optimized conditions, which even includes highly acid-labile groups, results from a hitherto unexploited shifted selectivity in protonation, and enabled simple and straightforward access to complex deuterium-labeled compounds In the experiment, the researchers used many compounds, for example, 1-Bromo-3,4,5-trimethoxybenzene(cas: 2675-79-8Quality Control of 1-Bromo-3,4,5-trimethoxybenzene)

1-Bromo-3,4,5-trimethoxybenzene(cas: 2675-79-8) is an important raw material and intermediate used in organic synthesis, pharmaceuticals, agrochemicals and dyestuff.Quality Control of 1-Bromo-3,4,5-trimethoxybenzene1-Bromo-3,4,5-trimethoxybenzene can be used to synthesize N,N′-diarylated indolo[3,2-b]carbazole derivatives, which can find applications in electrophotography.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Synthesis and Crystal Structure of Chalcone Derivatives and Their Effect on α-Glucosidase》 was published in Journal of Chemical Crystallography in 2020. These research results belong to Lin, Ping; Yin, Zhong-Ping; Wang, Meng; Liu, Jia; Yuan, En; Peng, Da-Yong; Nie, Xu-Liang; Shang-Guan, Xin-Chen. Application of 629-03-8 The article mentions the following:

Five trans-chalcone derivatives I [n = 2, 3, 4, 5, 6] were synthesized and characterized by 1H NMR, HRMS. The crystalline structures of compounds I [n = 5, 6] were further characterized by X-ray crystal diffraction. Among the five compounds, I [n = 2, 3] showed inhibitory activity on α-glucosidase, but I [n = 5, 6] increased the activity of α-glucosidase. In addition to this study using 1,6-Dibromohexane, there are many other studies that have used 1,6-Dibromohexane(cas: 629-03-8Application of 629-03-8) was used in this study.

1,6-Dibromohexane(cas: 629-03-8) is generally used to introduce C6 spacer in the molecular architecture. Some of the examples are: synthesis of solvent processable and conductive polyfluorene ionomers for alkaline fuel cell applications; synthesis of cross-linkable regioregular poly(3-(5-hexenyl)thiophene) (P3HNT) for stabilizing the film morphology in polymer photovoltaic cells.Application of 629-03-8

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《A Bithiophene-Promoted ppm Levels of Palladium-Catalyzed Regioselective Hydrosilylation of Terminal Allenes》 was published in Advanced Synthesis & Catalysis in 2020. These research results belong to Chen, Jun-Jia; Zeng, Jia-Hao; Yang, Ying; Liu, Zhi-Kai; Jiang, Ya-Nan; Li, Miao-Ran; Chen, Li; Zhan, Zhuang-Ping. Computed Properties of C4H2Br2S The article mentions the following:

A bithiophene-alkyne-based compound was synthesized and 1st used as a ligand for the selective hydrosilylation of allenes with primary and secondary phenylsilanes. It shows high selectivity towards the production of branched allylsilanes with a wide range of allenes. It is worth mentioning that the catalytic loading of the Pd can be reduced to 500 ppm. This work opens a new front of using bidentate thiophene ligand as a reaction promoter in transition-metal-catalyzed organic reaction. The experimental process involved the reaction of 2,5-Dibromothiophene(cas: 3141-27-3Computed Properties of C4H2Br2S)

2,5-Dibromothiophene(cas: 3141-27-3) , is mainly used as pharmaceutical intermediate and synthesis intermediate. 2,5-Dibromothiophene may be used in the preparation of soluble α,ω-diformyl-a-oligothiophenes.Computed Properties of C4H2Br2S

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Visible- and UV-Light-Induced Decarboxylative Radical Reactions of Benzoic Acids Using Organic Photoredox Catalysts》 was published in Journal of Organic Chemistry in 2020. These research results belong to Kubosaki, Suzuka; Takeuchi, Haruka; Iwata, Yutaka; Tanaka, Yosuke; Osaka, Kazuyuki; Yamawaki, Mugen; Morita, Toshio; Yoshimi, Yasuharu. Application of 586-76-5 The article mentions the following:

Photoinduced decarboxylative radical reactions of benzoic acids with electron-deficient alkenes, diborane, and acetonitrile under organic photoredox catalysis conditions and mild heating afforded adducts, arylboronate esters, and the reduction product, resp. The reaction is thought to involve single-electron transfer promoted the generation of aryl radicals via decarboxylation. A diverse range of benzoic acids were found to be suitable substrates for this photoreaction. Only two-mol. organic photoredox system can work well for the direct photoinduced decarboxylation of benzoic acids. In the experiment, the researchers used many compounds, for example, 4-Bromobenzoic acid(cas: 586-76-5Application of 586-76-5)

4-Bromobenzoic acid(cas: 586-76-5) has been used in bromine-specific detection of the metabolites of 2-,3-and 4-bromobenzoic acid in the urine and bile of rats by inductively coupled plasma mass spectrometry.Application of 586-76-5 It was used to study the metabolic fate of 2-,3-and 4-bromo benzoic acids in rat hepatocytes incubation using high temperature liquid chromatography.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Driving Quick and Large Amplitude Contraction of Viologen-Incorporated Poly-L-Lysine-Based Hydrogel by Reduction》 was written by Wang, Bo; Tahara, Hironobu; Sagara, Takamasa. Related Products of 17696-11-6This research focused onviologen functionalized polylysine hydrogel reduction induced contraction; actuation; contraction and re-expansion; hydrogel; redox; viologen. The article conveys some information:

A glutaraldehyde-crosslinked poly-L-lysine-based hydrogel with pendant viologens was synthesized with various [viologen unit]/[Lys unit] ratios. The hydrogel with the ratio of 25% had (i) a water content of 95.8%, (ii) unbound viologen unit was absent, and (iii) lyophilized gel showing porous structure was rewettable. The hydrogel in contact with a gold, glassy carbon, pyrolytic graphite, or ITO electrode was electroactive, showing voltammetric responses involving diffusion process. Occurrence of electron transfer between viologen sites was verified by ESR measurements. The electroreflectance spectrum indicated significant dimerization of one-electron-reduced forms, viologen radical cations. Reduction of the hydrogel by dithionite showed a 93% volume decrease, being near to the water content, at 100 s and finally 97% contraction at 380 s. The initial rate of contraction was 0.02 s-1, and the swelling weight ratio was > 17. The contraction rate was much faster than that observed when adding of redox-inactive salts in the outer medium. Recovery by reoxidation was relatively sluggish even when O2-saturated water was used. The quick and large-amplitude contraction with removal of water from the gel body should be the consequence of permeability of reductant, interchain π-stacking of one-electron-reduced forms (viologen monoradical monocation), desolvation of viologen upon reduction, electron hopping between viologen units and its acceleration with contraction, and effective osmotic pressure difference. The experimental process involved the reaction of 8-Bromooctanoic acid(cas: 17696-11-6Related Products of 17696-11-6)

8-Bromooctanoic acid(cas: 17696-11-6) acid is used in the synthesis of 8-(N-Methyl-4,4′-bipyridinyl)- octanoic acid. 8-Mercaptooctanoic acid was prepared from 8-bromooctanoic acid.Related Products of 17696-11-6

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthetic Route of C9H9BrO2In 2020 ,《Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells》 was published in Journal of Medicinal Chemistry. The article was written by Pan, Zhaoping; Li, Xiang; Wang, Yujia; Jiang, Qinglin; Jiang, Li; Zhang, Min; Zhang, Nan; Wu, Fengbo; Liu, Bo; He, Gu. The article contains the following contents:

Bromodomain-containing protein 4 (BRD4) and histone deacetylases (HDAC) are both attractive epigenetic targets in cancer and other chronic diseases. Based on the integrated fragment-based drug design, synthesis, and in vitro and in vivo evaluations, a series of novel thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives are discovered as selective BRD4-HDAC dual inhibitors. Compound 17c is the most potent inhibitor for BRD4 and HDAC with IC50 values at nanomolar levels, as well as the expression level of c-Myc, and increases the acetylation of histone H3. Moreover, 17c presents inhibitory effects on the proliferation of colorectal carcinoma (CRC) cells via inducing autophagic cell death. It also has a good pharmacokinetic profile in rats and oral bioavailability of 40.5%. In the HCT-116 xenograft in vivo models, 17c displays potent inhibitory efficiency on tumor growth by inducing autophagic cell death and suppressing IL6-JAK-STAT signaling pathways. Our results suggest that the BRD4-HDAC dual inhibition might be an attractive therapeutic strategy for CRC. The results came from multiple reactions, including the reaction of Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Synthetic Route of C9H9BrO2)

Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Synthetic Route of C9H9BrO2 The most pervasive is the naturally produced bromomethane.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Recommanded Product: 3141-27-3In 2022 ,《Synthesis, molecular docking, and biological evaluation of 5-alkyl(aryl)-2-isobutylthiazole derivatives as α-amylase, α-glucosidase, and protein kinase inhibitors》 was published in Applied Organometallic Chemistry. The article was written by Khan, Siraj; Bugday, Nesrin; Rehman, Asim Ur; Haq, Ihsan Ul; Yasar, Sedat; Ozdemir, Ismail. The article contains the following contents:

A series of 18 biol. active C5-arylated-2-isobutylthiazoles (aryl = Ph, 4-MeCOC6H4, 4-methyl-1-naphthyl, 5-formyl-2-furyl, etc.) was synthesized from 2-isobutylthiazole and the corresponding aryl bromides via C-H bond activation using Pd-NHC complexes [Pd(μ-Cl)Cl(NHC)]2 [NHC = 1,3-bis(2,6-dimethylphenyl)imidazolylidene] and [LCl2Pd-NHC] (L = PPh3, pyridine, 3-formylpyridine). All Pd-NHC complexes were prepared and characterized by 1H NMR, 13C NMR and FTIR spectroscopy, quadrupole-time of flight-liquid chromatog./mass spectroscopy (Q-TOF-LC/MS), gas chromatog.-mass spectrometry (GCMS), and m.p. techniques. The physicochem. properties, pharmacokinetics and drug-likeness of the thiazole products were calculated by SwissADME. PkCSM database was used to calculated the toxicity profile. Almost all the compounds showed no to low toxicity. All the products were addnl. assessed in vitro for their antidiabetic potential using α-amylase and α-glucosidase inhibitory activities. Except for 7 compounds, the prepared thiazoles showed good α-glucosidase inhibitory potential (IC50 7.17 ± 0.201 to 74.08 ± 0.244μg/mL) when compared with acarbose standard (IC50 16.59 ± 0.135μg/mL). All compounds had moderate to good inhibitory potential against the α-amylase enzyme, with IC50 values ranging from 12.00 ± 0.289 to 76.15 ± 0.477μg/mL. The protein kinase inhibition potential was determined for the first time, and 7 compounds showed activity with the zone of inhibition in the range of 9 ± 1.3 to 19 ± 1.5 mm. The ligands and active site binding interactions of α-glucosidase, α-amylase, and protein kinase enzymes were also studied using mol. modeling. In the experiment, the researchers used many compounds, for example, 2,5-Dibromothiophene(cas: 3141-27-3Recommanded Product: 3141-27-3)

2,5-Dibromothiophene(cas: 3141-27-3) , is mainly used as pharmaceutical intermediate and synthesis intermediate. 2,5-Dibromothiophene polymerizes by debromination with magnesium catalyzed by nickel compounds to form poly(2,5- thienylene) .Recommanded Product: 3141-27-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary