Tag: M.W=250-300

Prinz, Michaela published the artcile1,4-Substituted 4-(1H)-pyridylene-hydrazone-type inhibitors of AChE, BuChE, and amyloid-β aggregation crossing the blood-brain barrier, Product Details of C7H5Br2F, the publication is European Journal of Pharmaceutical Sciences (2013), 49(4), 603-613, database is CAplus and MEDLINE.

Given the fundamentally multifactorial character of Alzheimer’s disease (AD), addressing more than one target for disease modification or therapy is expected to be highly advantageous. Here, following the cholinergic hypothesis, we aimed to inhibit both acetyl- and butyrylcholinesterase (AChE and BuChE) in order to increase the concentration of acetylcholine in the synaptic cleft. In addition, the formation of the amyloid β fibrils should be inhibited and already preformed fibrils should be destroyed. Based on a recently identified AChE inhibitor with a 1,4-substituted 4-(1H)-pyridylene-hydrazone skeleton, a substance library has been generated and tested for inhibition of AChE, BuChE, and fibril formation. Blood-brain barrier mobility was ensured by a transwell assay. Whereas the p-nitrosubstituted compound 18C shows an anti-AChE activity in the nanomolar range of concentration (IC₅₀ = 90 nM), the bisnaphthyl substituted compound 20L was found to be the best overall inhibitor of AChE/BuChE and enhances the fibril destruction.

European Journal of Pharmaceutical Sciences published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Product Details of C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Zhu, Shaojuan published the artcileIn vitro and in vivo evaluation of antioxidant activity of ARIs: benzothiadiazine and pyridothiadiazine derivatives, Application of 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Journal of Chemical and Pharmaceutical Research (2014), 6(5), 173-179, 7 pp., database is CAplus.

Increased oxidant stress plays an important role in the chronic complications of diabetes. This study aimed to examine if our previously synthesized aldose reductase inhibitors (ARIs), benzothiadiazine 1,1-dioxide derivatives and the structural analogs pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide derivatives, have the potent as antioxidants. Several assays have been used to estimate antioxidant capacities including DPPH, MDA and sorbitol assays. Effect of concentration, PH and sunlight on DPPH scavenging activity were determined, and results showed benzothiadiazine 1,1-dioxide derivatives (compound 7a, 7b, 7c) at both concentration of 10-5 M and 10-4 M had notable scavenging activity against DPPH, significantly higher than that of pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide derivatives(compound 7’a, 7’b, 7’c). The PH demonstrated no effect on the activity and sunlight was essential for the activity. The brain MDA levels (MDA, an index of lipid peroxidation) for compounds 7a, 7b, 7c significantly decreased comparing with the neg. control, the brain homogenate sample induced by oxidant system Fe(III) ascorbic acid. Oral administration of compound 7’a, 7’b and 7’c to groups of STZ-induced rats for 5 days decreased the level of sciatic nerve sorbitol, The inhibition of sorbitol level in the range of 24%-35% for 7’a, 7’b and 7’c, showing some difference with the in vitro study.

Journal of Chemical and Pharmaceutical Research published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C18H20N2O12, Application of 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Gao, Xingming published the artcileA fluorescent bisboronic acid compound that selectively labels cells expressing oligosaccharide Lewis X, Computed Properties of 166821-88-1, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(12), 2501-2504, database is CAplus and MEDLINE.

Two fluorescent diboronic acid compounds with a dipeptide linker were synthesized as potential sensors for cell surface saccharide Lewis X (Le^X). Compound 6a (I) with a dipeptide (H-Asp-Ala-) as the linker was found to selectively label CHOFUT4 cells, which express Le^x, at micromolar concentrations, while non-Le^x-expressing control cells were not labeled.

Bioorganic & Medicinal Chemistry Letters published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C12H16BBrO2, Computed Properties of 166821-88-1.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Leenders, Ruben published the artcileNovel SAR for quinazoline inhibitors of EHMT1 and EHMT2, Application In Synthesis of 1256955-36-8, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(17), 2516-2524, database is CAplus and MEDLINE.

Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitor compounds I [R = COOH, CONH₂, (5-prop-2-ynylpyrrolidin-2-one)-3-yl etc.] and II [R¹ = OMe, F, OCF₃ ; R² = aminopropynyl,(5-prop-2-ynylpyrrolidin-2-one)-3-yl etc.] were elaborated. New and active alternatives were presented for the ubiquitous substitution patterns found in literature for the linker to the lysine mimicking region and the lysine mimic itself.

Bioorganic & Medicinal Chemistry Letters published new progress about 1256955-36-8. 1256955-36-8 belongs to bromides-buliding-blocks, auxiliary class Bromide,Amine,Benzene,Ester,Ether, name is Methyl 2-amino-4-bromo-5-methoxybenzoate, and the molecular formula is C9H10BrNO3, Application In Synthesis of 1256955-36-8.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Cakmak, Osman published the artcileBromination of naphthalene. Preparation of 1,3-dibromonaphthalene, Quality Control of 52358-73-3, the publication is Journal of Chemical Research, Synopses (1999), 366-367, database is CAplus.

Photobromination of naphthalene with mol. bromine gives only one stereoisomer, 1α,2β,3α,4β-tetrabromo-1,2,3,4-tetrahydronaphthalene (I) in 90% yield; dehydrobromination of I results in the formation of 1,3-dibromonaphthalene in 88% yield.

Journal of Chemical Research, Synopses published new progress about 52358-73-3. 52358-73-3 belongs to bromides-buliding-blocks, auxiliary class Bromide,Naphthalene, name is 1,3-Dibromonaphthalene, and the molecular formula is C10H6Br2, Quality Control of 52358-73-3.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Craig, Sandra published the artcileSynthesis and evaluation of aryl boronic acids as fluorescent artificial receptors for biological carbohydrates, Synthetic Route of 166821-88-1, the publication is Bioorganic Chemistry (2012), 137-142, database is CAplus and MEDLINE.

Carbohydrates in various forms play a vital role in numerous critical biol. processes. The detection of such saccharides can give insight into the progression of such diseases such as cancer. Boronic acids react with 1,2 and 1,3 diols of saccharides in non-aqueous or basic aqueous media. Herein, we describe the design, synthesis and evaluation of three bisboronic acid fluorescent probes, each having about ten linear steps in its synthesis. Among these compounds that were evaluated, 9b was shown to selectively label HepG2, liver carcinoma cell line within a concentration range of 0.5-10 μM in comparison to COS-7, a normal fibroblast cell line.

Bioorganic Chemistry published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C12H16BBrO2, Synthetic Route of 166821-88-1.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Hou, Jin published the artcileEvaluation of Novel N-(piperidine-4-yl)benzamide Derivatives as Potential Cell Cycle Inhibitors in HepG2 Cells, Formula: C7H5Br2F, the publication is Chemical Biology & Drug Design (2015), 86(2), 223-231, database is CAplus and MEDLINE.

In this study, a series of novel N-(piperidine-4-yl)benzamide derivatives was designed, synthesized, and evaluated for antitumor activity. Some compounds were found to have potent antitumor activity. In particular, compound 47 (N-(1-(2,6-difluorobenzyl)piperidine-4-yl)-4phenoxybenzamide) showed the most potent biol. activity against HepG2 cells, with an IC₅₀ value of 0.25 μM. Western blot anal. demonstrated that compound 47 inhibited the expression of cyclin B1 and p-Rb and enhanced the expression of p21, p53, Rb, and phospho-adenosine monophosphate-activated protein kinase (p-AMPK). Further, cell cycle arrest was observed by flow cytometry (FCM). In summary, compound 47 was screened to have potential activity for the treatment of hepatocarcinoma via the induction of cell cycle arrest by a p53/p21-dependent pathway.

Chemical Biology & Drug Design published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Sun, Xin published the artcileMetal-Free Hypervalent-Iodine-Promoted C3 Difluorination and C2 Oxidation of N-Substituted Indoles, Category: bromides-buliding-blocks, the publication is Asian Journal of Organic Chemistry (2017), 6(6), 690-693, database is CAplus.

A metal-free, highly regioselective C3 difluorination and C2 oxidation of N-substituted indoles I (R¹ = 5-Br, 7-Cl, 3,6-F₂, etc.; R² = Bn, 4-ClC₆H₄CH₂, 2,3,5-F₃C₆H₂CH₂, etc.) with the aid of in situ generated PhIF₂ in the presence of two types of fluorinating agents such as Pyr·HF and Et₃N·HF was reported. This reaction provided 3,3-difluoro-2-oxindoles II with yields up to 64% under mild reaction conditions. A mechanism for this reaction was proposed.

Asian Journal of Organic Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H10BNO4S, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Ya-Wei published the artcile^tBuOK-Promoted Cyclization of Imines with Aryl Halides, Synthetic Route of 76283-09-5, the publication is Organic Letters (2020), 22(11), 4553-4556, database is CAplus and MEDLINE.

A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramol. coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.

Organic Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Synthetic Route of 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Liu, Shunjie published the artcileMolecular Motion in Aggregates: Manipulating TICT for Boosting Photothermal Theranostics, HPLC of Formula: 303734-52-3, the publication is Journal of the American Chemical Society (2019), 141(13), 5359-5368, database is CAplus and MEDLINE.

Planar donor and acceptor (D-A) conjugated structures are generally believed to be the standard for architecting highly efficient photothermal theranostic agents, in order to restrict intramol. motions in aggregates (nanoparticles). However, other channels of extra nonradiative decay may be blocked. Now this challenge is addressed by proposing an “abnormal” strategy based on mol. motion in aggregates. Mol. rotors and bulky alkyl chains are grafted to the central D-A core to lower intermol. interaction. The enhanced mol. motion favors the formation of a dark twisted intramol. charge transfer state, whose nonradiative decay enhances the photothermal properties. Result shows that small-mol. NIRb14 with long alkyl chains branched at the second carbon exhibits enhanced photothermal properties compared with NIRb6, with short branched chains, and much higher than NIR6, with short linear chains, and the com. gold nanorods. Both in vitro and in vivo experiments demonstrate that NIRb14 nanoparticles can be used as nanoagents for photoacoustic imaging-guided photothermal therapy. Moreover, charge reversal poly(β-amino ester) makes NIRb14 specifically accumulate at tumor sites. This study thus provides an excited mol. motion approach toward efficient phototheranostic agents.

Journal of the American Chemical Society published new progress about 303734-52-3. 303734-52-3 belongs to bromides-buliding-blocks, auxiliary class Thiophene,Bromide, name is 2-Bromo-3-(2-ethylhexyl)thiophene, and the molecular formula is C12H19BrS, HPLC of Formula: 303734-52-3.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary