Tag: 200-300

Synthesis and evaluation of novel 1,2,3-triazole-based acetylcholinesterase inhibitors with neuroprotective activity was written by Li, Jia-Cheng;Zhang, Juan;Rodrigues, Mosar Correa;Ding, De-Jun;Longo, Joao Paulo Figueiro;Azevedo, Ricardo Bentes;Muehlmann, Luis Alexandre;Jiang, Cheng-Shi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Application of 61150-57-0 This article mentions the following:

A series of new 1,2,3-triazole derivatives were synthesized and evaluated for anticholinesterase and neuroprotective activities. Some synthetic derivatives, especially compound I, exhibited improved acetylcholinesterase (AChE) inhibitory activity by comparison with the hit, high selectivity toward AChE over butyrylcholinesterase (BuChE), and suitable in vitro neuroprotective effect against amyloid-β_25-35 (Aβ_25-35)-induced neurotoxicity in SH-SY5Y cells. Furthermore, these mols. have desired physicochem. properties in the range of CNS drugs and showed no cytotoxicity against two normal cells, including human keratinocytes HaCaT and murine fibroblasts NIH-3T3. The preliminary bioassay results and docking study indicated that compound I might be a promising lead compound with dual action for the treatment of Alzheimer’s disease. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0Application of 61150-57-0).

2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Application of 61150-57-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Iridium-Catalyzed Borylation of Secondary Benzylic C-H Bonds Directed by a Hydrosilane was written by Cho, Seung Hwan;Hartwig, John F.. And the article was included in Journal of the American Chemical Society in 2013.Product Details of 61150-57-0 This article mentions the following:

Most functionalizations of C-H bonds by main-group reagents occur at aryl or Me groups. The authors describe a highly regioselective borylation of secondary benzylic C-H bonds catalyzed by an Ir precursor and 3,4,7,8-tetramethyl-1,10-phenanthroline as the ligand. The reaction is directed to the benzylic position by a hydrosilyl substituent. This hydrosilyl directing group is readily deprotected or transformed to other functional groups after the borylation reaction, providing access to a diverse set of secondary benzylboronate esters by C-H borylation chem. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0Product Details of 61150-57-0).

2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Product Details of 61150-57-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Determination of aromaticity indices of thiophene and furan by nuclear magnetic resonance spectroscopic analysis of their phenyl esters was written by Lee, Chang Kiu;Yu, Ji Sook;Lee, Hye-Jin. And the article was included in Journal of Heterocyclic Chemistry in 2002.Computed Properties of C8H7BrO2 This article mentions the following:

A series of m- and p-substituted Ph benzoates, 2-thienoates, and 2-furoates were prepared and their ¹H and ¹³C NMR spectroscopic characteristics were examined In general, good correlations were observed between the chem. shift values of protons and carbons of the acyl aromatic rings and the Hammett σ. Plots of the chem. shift values of the carbonyl carbons of the benzoates against those of the 2-thienoates and 2-furoates gave an excellent correlation and the values of the slopes are 0.85 and 0.75, resp., in DMSO-d₆ and 0.90 and 0.78, resp., in chloroform-d. The values could be considered as a set of aromaticity indexes. In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Computed Properties of C8H7BrO2).

3-Bromophenyl acetate (cas: 35065-86-2) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Computed Properties of C8H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of UK-78282 was written by Liang, Xizhou;Da, Shijun;Li, Ying. And the article was included in Zhongguo Yiyao Gongye Zazhi in 2005.Related Products of 57293-19-3 This article mentions the following:

UK-78282 [i.e., 4-[(diphenylmethoxy)methyl]-1-[3-(4-methoxyphenyl)propyl]piperidine] a novel potassium channel blocker (no data), was synthesized from 4-methoxycinnamic acid by reduction and bromination to give 3-(4-methoxyphenyl)-1-bromopropane, which subjected to condensation with Et piperidine-4-carboxylate followed by reduction and etherification by diphenylmethanol. The overall yield was 58%. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Related Products of 57293-19-3).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Related Products of 57293-19-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Regio- and Stereoselective Alkylboration of Endocyclic Olefins Enabled by Nickel Catalysis was written by Ding, Chao;Ren, Yaoyu;Sun, Caocao;Long, Jiao;Yin, Guoyin. And the article was included in Journal of the American Chemical Society in 2021.Category: bromides-buliding-blocks This article mentions the following:

Whereas there is a significant interest in the rapid construction of diversely substituted saturated heterocycles, direct and modular access is currently limited to the mono-, 2,3-, or 3,4-substitution pattern. This Communication describes the straightforward and modular construction of 2,4-substituted saturated heterocycles from readily available materials in a highly stereo- and regioselective manner, which sets the stage for numerous readily accessible drug motifs. The strategy relies on chain walking catalysis. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Category: bromides-buliding-blocks).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Receptor agonists of macrophage migration inhibitory factor was written by Jorgensen, William L.;Gandavadi, Sunilkumar;Du, Xin;Hare, Alissa A.;Trofimov, Alexander;Leng, Lin;Bucala, Richard. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Category: bromides-buliding-blocks This article mentions the following:

The cytokine MIF is involved in inflammation and cell proliferation via pathways initiated by its binding to the transmembrane receptor CD74. MIF also promotes AMPK activation with potential benefits for response to myocardial infarction and ischemia-reperfusion. Structure-based mol. design has led to the discovery of not only antagonists, but also the first agonists of MIF-CD74 binding. The compounds contain a triazole core that is readily assembled via Cu-catalyzed click chem. The agonist and antagonist behaviors were confirmed via study of MIF-dependent ERK1/2 phosphorylation in human fibroblasts. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Category: bromides-buliding-blocks).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential ¹⁸F-radioligands for 5-HT_2A receptor imaging with PET was written by Herth, Matthias M.;Kramer, Vasko;Piel, Markus;Palner, Mikael;Riss, Patrick J.;Knudsen, Gitte M.;Roesch, Frank. And the article was included in Bioorganic & Medicinal Chemistry in 2009.Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene This article mentions the following:

Radiolabeled piperidine derivatives such as [¹¹C]MDL 100907 and [¹⁸F]altanserin have played an important role in diagnosing malfunction in the serotonergic neurotransmission. A variety of novel piperidine MDL 100907 derivatives, possible to label with ¹⁸F-fluorine, were synthesized to improve mol. imaging properties of [¹¹C]MDL 100907. Their in vitro affinities to a broad spectrum of neuroreceptors and their lipophilicities were determined and compared to the clin. used reference compounds MDL 100907 and altanserin. The novel compounds MA-1 (53) and (R)-MH.MZ (56) show K _i-values in the nanomolar range towards the 5-HT_2A receptor and insignificant binding to other 5-HT receptor subtypes or receptors. Interestingly, compounds MA-1 (53), MH.MZ (55) and (R)-MH.MZ (56) provide a receptor selectivity profile similar to MDL 100907. These compounds could possibly be preferable antagonistic ¹⁸F-tracers for visualization of the 5-HT_2A receptor status. Medium affine compounds (VK-1 (32), (51), (52), (54)) were synthesized and have K _i values between 30 and 120 nM. All promising compounds show log P values between 2 and 3, i.e., within the range of those for the established radiotracers altanserin and MDL 100907. The novel compounds MA-1 (53) and (R)-MH.MZ (56) thus appear to be promising high affine and selective tracers of ¹⁸F-labeled analogs for 5-HT_2A imaging with PET. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression was written by Gacias, Mar;Gerona-Navarro, Guillermo;Plotnikov, Alexander N.;Zhang, Guangtao;Zeng, Lei;Kaur, Jasbir;Moy, Gregory;Rusinova, Elena;Rodriguez, Yoel;Matikainen, Bridget;Vincek, Adam;Joshua, Jennifer;Casaccia, Patrizia;Zhou, Ming-Ming. And the article was included in Chemistry & Biology (Oxford, United Kingdom) in 2014.COA of Formula: C13H14BrNO2 This article mentions the following:

Lysine acetylation regulates gene expression through modulating protein-protein interactions in chromatin. Chem. inhibition of acetyl-lysine binding bromodomains of the major chromatin regulators BET (bromodomain and extraterminal domain) proteins has been shown to effectively block cell proliferation in cancer and inflammation. However, whether selective inhibition of individual BET bromodomains has distinctive functional consequences remains only partially understood. In this study, we show that selective chem. inhibition of the first bromodomain of BET proteins using our small-mol. inhibitor, Olinone, accelerated the progression of mouse primary oligodendrocyte progenitors toward differentiation, whereas inhibition of both bromodomains of BET proteins hindered differentiation. This effect was target specific, as it was not detected in cells treated with inactive analogs and independent of any effect on proliferation. Therefore, selective chem. modulation of individual bromodomains, rather than use of broad-based inhibitors, may enhance regenerative strategies in disorders characterized by myelin loss such as aging and neurodegeneration. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4COA of Formula: C13H14BrNO2).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. COA of Formula: C13H14BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HT_1A weak partial agonistic activity showing the antidepressant-like effect was written by Yoshinaga, Hidefumi;Masumoto, Shuji;Koyama, Koji;Kinomura, Naoya;Matsumoto, Yuji;Kato, Taro;Baba, Satoko;Matsumoto, Kenji;Horisawa, Tomoko;Oki, Hitomi;Yabuuchi, Kazuki;Kodo, Toru. And the article was included in Bioorganic & Medicinal Chemistry in 2017.Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene This article mentions the following:

We report the discovery of a novel benzylpiperidine derivative with serotonin transporter (SERT) inhibitory activity and 5-HT_1A receptor weak partial agonistic activity showing the antidepressant-like effect. The 3-methoxyphenyl group and the phenethyl group of compound 1, which has weak SERT binding activity, but potent 5-HT_1A binding activity, were optimized, leading to compound 35 with potent and balanced dual SERT and 5-HT_1A binding activity, but also potent CYP2D6 inhibitory activity. Replacement of the methoxy group in the left part of compound 35 with a larger alkoxy group, such as ethoxy, isopropoxy or methoxy-ethoxy group ameliorated CYP2D6 inhibition, giving SMP-304 as a candidate. SMP-304 with serotonin uptake inhibitory activity and 5-HT_1A weak partial agonistic activity, which could work as a 5-HT_1A antagonist, displayed faster onset of antidepressant-like effect than a representative SSRI paroxetine in an animal model. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Recommanded Product: 1-(2-Bromoethyl)-4-methoxybenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synergistic Photo-Copper-Catalyzed Hydroxylation of (Hetero)aryl Halides with Molecular Oxygen was written by Zhang, Xin;Wu, Ge;Gao, Wenxia;Ding, Jinchang;Huang, Xiaobo;Liu, Miaochang;Wu, Huayue. And the article was included in Organic Letters in 2018.Safety of Methyl 4-bromo-2-fluorobenzoate This article mentions the following:

Photoredox-mediated copper-catalyzed hydroxylation of (hetero)aryl halides (including chlorides, bromides and iodides) with O₂ at room temperature has been developed. Preliminary mechanistic studies indicate no arylcopper intermediate and that aryl radicals are involved in this procedure. ¹⁸O-labeling experiments confirm the hydroxyl oxygen atom originated from mol. oxygen. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Safety of Methyl 4-bromo-2-fluorobenzoate).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Safety of Methyl 4-bromo-2-fluorobenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary