Category: 954-81-4

Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with 閻?amyloid anti-aggregation properties and beneficial effects on memory in vivo was written by Wieckowska, Anna;Wieckowski, Krzysztof;Bajda, Marek;Brus, Boris;Salat, Kinga;Czerwinska, Paulina;Gobec, Stanislav;Filipek, Barbara;Malawska, Barbara. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Reference of 954-81-4 This article mentions the following:

Due to the complex nature of Alzheimer’s disease, multi-target-directed ligand approaches are one of the most promising strategies in the search for effective treatments. Acetylcholinesterase, butyrylcholinesterase and 閻?amyloid are the predominant biol. targets in the search for new anti-Alzheimer’s agents. Our aim was to combine both anticholinesterase and 閻?amyloid anti-aggregation activities in one mol., and to determine the therapeutic potential in vivo. We designed and synthesized 28 new compounds as derivatives of donepezil that contain the N-benzylpiperidine moiety combined with the phthalimide or indole moieties. Most of these test compounds showed micromolar activities against cholinesterases and aggregation of 閻?amyloid, combined with pos. results in blood-brain barrier permeability assays. The most promising compound 23 (2-(8-(1-(3-chlorobenzyl)piperidin-4-ylamino)octyl)isoindoline-1,3-dione) is an inhibitor of butyrylcholinesterase (IC₅₀ = 0.72 婵炴挾鎷? that has 閻?amyloid anti-aggregation activity (72.5% inhibition at 10 婵炴挾鎷? and can cross the blood-brain barrier. Moreover, in an animal model of memory impairment induced by scopolamine, the activity of 23 was comparable to that of donepezil. The selected compound 23 is an excellent lead structure in the further search for new anti-Alzheimer’s agents. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Reference of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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闁艰京鐗梤omine bond is electrophilic in nature. 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.Reference of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, synthesis, and in vitro evaluation of an activity-based protein profiling (ABPP) probe targeting agmatine deiminases was written by Thomson, Andrew;O’Connor, Sean;Knuckley, Bryan;Causey, Corey P.. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Related Products of 954-81-4 This article mentions the following:

Agmatine deiminases (AgDs) belong to a family of enzymes known as guanidinium group modifying enzymes (GMEs). Many pathogenic bacteria encode an AgD that participates in the catabolism of agmatine (decarboxylated arginine). This catabolism may confer a competitive survival advantage, by virtue of energy production and increased acid tolerance, making this sub-family of enzymes a potential therapeutic target that warrants further study. Herein we report the development of an activity-based protein profiling (ABPP) probe that selectively targets the AgD from Streptococcus mutans. Due to the selectivity and covalent nature of the modification, this probe could prove to be a valuable tool for the study of other AgD family members. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Related Products of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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闁艰京鐗梤omine bond is electrophilic in nature. 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.Related Products of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A Potent and Highly Selective Inhibitor of Human 濞?1,3-Fucosyltransferase via Click Chemistry was written by Lee, Lac V.;Mitchell, Michael L.;Huang, Shih-Jung;Fokin, Valery V.;Sharpless, K. Barry;Wong, Chi-Huey. And the article was included in Journal of the American Chemical Society in 2003.Name: N-(5-Bromopentyl)phthalimide This article mentions the following:

Potent inhibitors of fucosyltransferases, and glycosyltransferases in general, have been elusive due to the inherent barriers surrounding the family of glycosyl transfer reactions. The problems of weak substrate affinity and low catalytic proficiency of fucosyltransferase was offset by recruiting addnl. binding features, in this case hydrophobic interactions, to produce a high affinity inhibitor, 24, with K_i = 62 nM. The mol. was identified from a GDP-triazole library of 85 compounds, which was produced by the Cu(I)-catalyzed [2+3] cycloaddition reaction between azide and acetylene reactants, followed by in situ screening without product isolation. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Name: N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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). 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.Name: N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Development of Phthalimide-Donepezil Hybrids as Potent Multitarget- Directed Ligands for the Treatment of Alzheimer’s Disease was written by Yu, Lintao;Shi, Jian;Cheng, Xinfeng;Wang, Keren;Liu, Shuang;Liu, Wenmin;Sang, Zhipei. And the article was included in Letters in Drug Design & Discovery in 2020.COA of Formula: C13H14BrNO2 This article mentions the following:

Due to the complex etiol. of AD, multi-target-directed ligands (MTDLs), combining two or more distinct pharmacol. moieties, have been developed in both symptomatic and disease-modifying efficiencies and are considered as an effective way for the treatment of AD. To test their biol. activities, including AChE/BChE inhibitory activity and MAOA/ MAO-B inhibitory activity. In addition, mol. modeling studies were performed to afford insight into the binding mode. The results displayed that compound 4c showed the best AChE inhibitory activity with an IC₅₀ value of 4.2 I1/4M, which was supported by the kinetic study and docking study. Compound 4c was also a selective MAO-B inhibitor (IC₅₀ = 8.2 I1/4M). Moreover, compound 4c could cross the blood-brain barrier in vitro. Compound 4c deserved to further study as a potential multifunctional agent for the treatment of Alzheimeraeuros disease. 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. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon闂佺偨鍎茶ぐ绲﹐mine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.COA of Formula: C13H14BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer’s disease was written by Sang, Zhipei;Wang, Keren;Wang, Huifang;Yu, Lintao;Wang, Huijuan;Ma, Qianwen;Ye, Mengyao;Han, Xue;Liu, Wenmin. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Application of 954-81-4 This article mentions the following:

A series of phthalimide-alkylamine derivs, e.g., I, were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer’s disease (AD). The results showed that compound I could be regarded as a balanced multi-targets active mol. It exhibited potent and balanced inhibitory activities against ChE and MAO-B (huAChE, huBuChE, and huMAO-B with IC₅₀ values of 1.2 婵炴挾鎷? 3.8 婵炴挾鎷?and 2.6 婵炴挾鎷? resp.) with low selectivity. Both kinetic anal. of AChE inhibition and mol. modeling study suggested that I binds simultaneously to the catalytic active site and peripheral anionic site of AChE. Interestingly, compound I abided by Lipinski’s rule of five. Furthermore, our investigation proved that I indicated weak cytotoxicity, and it could cross the blood-brain barrier (BBB) in vitro. The results suggest that compound I, an interesting multi-targeted active mol., offers an attractive starting point for further lead optimization in the drug-discovery process against Alzheimer’s disease. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Application of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Application of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The synthesis of oxa-analogs and homologs of naturally occurring polyamines was written by Lin, P. Kong Thoo;Kuksa, V. A.;Maguire, N. M.. And the article was included in Synthesis in 1998.Formula: C13H14BrNO2 This article mentions the following:

A number of polyamine oxa-analogs were synthesized. Spermidine oxa-analogs and homologs were made from N-(aminooxypropyl)phthalimide which was obtained either by deprotection of the corresponding Fmoc-protected compound or from the reaction between 3-Br(CH₂)₃NH₂ and N-hydroxyphthalimide, both reactions involving an unusual rearrangement mechanism. Sulfonated derivatives, upon Mitsunobu condensation with N-protected 3-HO(CH₂)₃NH₂ or N-alkylation with N-(bromoalkyl)phthalimides, afforded the fully protected spermidine and spermine oxa-analogs and homologs. Subsequent sequential deprotection gave spermidine analogs. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Formula: C13H14BrNO2).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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). 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.Formula: C13H14BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Catalytic asymmetric reductive hydroalkylation of enamides and enecarbamates to chiral aliphatic amines was written by Wang, Jia-Wang;Li, Yan;Nie, Wan;Chang, Zhe;Yu, Zi-An;Zhao, Yi-Fan;Lu, Xi;Fu, Yao. And the article was included in Nature Communications in 2021.Electric Literature of C13H14BrNO2 This article mentions the following:

A mild and general nickel-catalyzed asym. reductive hydroalkylation effectively converted to enamides and enecarbamates into drug-like 濞?branched chiral amines was reported. This reaction involved the regio- and stereoselective hydrometallation of an enamide or enecarbamate to generated a catalytic amount of enantioenriched alkylnickel intermediate, followed by C-C bond formation via alkyl electrophiles. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Electric Literature of C13H14BrNO2).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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. 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.Electric Literature of C13H14BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Orthosteric-allosteric dual inhibitors of PfHT1 as selective antimalarial agents was written by Huang, Jian;Yuan, Yafei;Zhao, Na;Pu, Debing;Tang, Qingxuan;Zhang, Shuo;Luo, Shuchen;Yang, Xikang;Wang, Nan;Xiao, Yu;Zhang, Tuan;Liu, Zhuoyi;Sakata-Kato, Tomoyo;Jiang, Xin;Kato, Nobutaka;Yan, Nieng;Yin, Hang. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2021.Recommanded Product: N-(5-Bromopentyl)phthalimide This article mentions the following:

Artemisinin-resistant malaria parasites have emerged and have been spreading, posing a significant public health challenge. Antimalarial drugs with novel mechanisms of action are therefore urgently needed. In this report, we exploit a ‘selective starvation’ strategy by inhibiting Plasmodium falciparum hexose transporter 1 (PfHT1), the sole hexose transporter in P. falciparum, over human glucose transporter 1 (hGLUT1), providing an alternative approach to fight against multidrug-resistant malaria parasites. The crystal structure of hGLUT3, which shares 80% sequence similarity with hGLUT1, was resolved in complex with C3361, a moderate PfHT1-specific inhibitor, at 2.3-闁?resolution Structural comparison between the present hGLUT3-C3361 and our previously reported PfHT1-C3361 confirmed the unique inhibitor binding-induced pocket in PfHT1. We then designed small mols. to simultaneously block the orthosteric and allosteric pockets of PfHT1. Through extensive structure-activity relationship studies, the TH-PF series was identified to selectively inhibit PfHT1 over hGLUT1 and potent against multiple strains of the blood-stage P. falciparum. Our findings shed light on the next-generation chemotherapeutics with a paradigm-shifting structure-based design strategy to simultaneously target the orthosteric and allosteric sites of a transporter. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Recommanded Product: N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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. 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.Recommanded Product: N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Pyridylbenzimidazole-Based Gold(III) Complexes: Lysozyme Metalation, DNA Binding Studies, and Biological Activity was written by Mansour, Ahmed M.;Shehab, Ola R.. And the article was included in European Journal of Inorganic Chemistry in 2019.Related Products of 954-81-4 This article mentions the following:

The lysozyme binding affinity of new Au(III) complexes, bearing pyridylbenzimidazole ligands, was studied by ESI-MS and UV/visible. Metalation of lysozyme happened mainly by {Au}ⁿ⁺, {AuCl}^0/n+ and {AuCl₂}^n+/-. The appendage sulfonate group of pyridylbenzimidazole ligand system played a role in determining the products of interaction of HEWL with Au(III) complexes. The hydrophilic sulfonate group inhibited the ligand cleavage via the participation in several coulombic and H-bond interactions giving several AuLⁿ⁺ containing adduct peaks (L = 1-[(pyridin-2-yl) benzimidazole]-propyl-sulfonic acid). The stability of the complexes in presence of ascorbic acid was examined by UV/visible and ¹³C NMR. To recognize if His15 side-chain is the metalation site of HEWL, the interactions between the complexes and imidazole, as a simple model of histidine, were studied by ¹H and ¹³C NMR. The DNA binding studies of the complexes are reported. For this class of Au(III) complexes, it is preferred to decorate the pyridylbenzimidazole system with Et group rather than sulfonate and phthalimido group to have a complex with interesting antifungal activity against Candida albicans and Cryptococcus neoformans var. grubii. Au(III) complex, having sulfonate group, is noncytotoxic to non-malignant cells (human embryonic kidney cells (HEK293)), shows negligible Hb release and is safe to the normal cells if applicable. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Related Products of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Related Products of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Nanostructures from Self-Assembling Triazine Tertiary Amine N-Oxide Amphiphiles was written by Beecham, Matthew P.;Clarkson, Guy J.;Hall, Gareth;Marsh, Andrew. And the article was included in ChemPhysChem in 2013.Reference of 954-81-4 This article mentions the following:

A set of amphiphilic tertiary amine N-oxides has been prepared and their self-assembly was observed in aqueous solution by tensiometry, dynamic, and static light scattering. X-ray crystallog. anal. of parent amines and sulfoxide congeners indicated the formation of hydrogen-bonded dimers as the primary assembly unit for formation of vesicles in preference to the compact micelles typical of lauryl dimethylamine N-oxide (LDAO). 6-Benzyloxy-N,N’-bis(5-diethylaminopentylamine oxide)[1,3,5]triazine-2,4-diamine formed a 1 娓璵 vesicle observed to entrap fluorescein. The [1,3,5]triazine core thus allowed for the variation of the new self-assembled structures from nano- to micrometer length scales. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Reference of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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.Reference of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary