Tag: 200-300

Novel Selective PDE4 Inhibitors. 3. In Vivo Antiinflammatory Activity of a New Series of N-Substituted cis-Tetra- and cis-Hexahydrophthalazinones was written by Van der Mey, Margaretha;Boss, Hildegard;Hatzelmann, Armin;Van der Laan, Ivonne J.;Sterk, Geert J.;Timmerman, Hendrik. And the article was included in Journal of Medicinal Chemistry in 2002.Formula: C8H7BrO2 This article mentions the following:

The synthesis and biol. activities of a series of N-substituted cis-4a,5,6,7,8,8a-hexa- and cis-4a,5,8,8a-tetrahydro-2H-phthalazin-1-ones I [XY = (CH₂)₂, HC:CH; R = Me, cyclopentyl, allyl, PhCOCH₂, etc.] are described. It was found that compounds bearing a cycloalkyl group at the 2-position exhibit the highest PDE4 inhibitory activities (pIC₅₀ = 8.6-9.4). The N-cycloheptyl- and N-adamantanyltetrahydrophthalazinones I (XY = HC:CH; R = cycloheptyl, 2-adamantyl) and II [R¹ = R² = Me, R¹R² = (CH₂)₄] show high in vivo antiinflammatory activities after oral application. Addnl., some phthalazinones were found to exhibit potent suppression of LPS-induced TNF浼?release and show moderate potency against fMLP-stimulated production of ROS. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Formula: C8H7BrO2).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) 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. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. 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.Formula: C8H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Intramolecular Charge-Transfer Interaction in a New Dyad Based on C₆₀ and Bis(4′-tert-butylbiphenyl-4-yl)aniline (BBA) Donor was written by Ohno, Toshinobu;Moriwaki, Kazuyuki;Miyata, Toshiyuki. And the article was included in Journal of Organic Chemistry in 2001.Synthetic Route of C16H17Br This article mentions the following:

A novel methanofullerene dyad based on C₆₀ and bis(4′-tert-butylbiphenyl-4-yl)aniline (BBA) has been prepared and characterized. Cyclic voltammetry (CV) and UV-vis spectra of the C₆₀-BBA methanofullerene dyad, 61-phenyl-1,2-methanofullerene[60], 1,2-methanofullerene[60], and BBA were measured and analyzed. CV measurements showed that a reversible oxidation wave of the C₆₀-BBA methanofullerene dyad was pos. shifted by 40 mV compared to that of BBA. More remarkably, comparing UV-vis spectra of the C₆₀-BBA methanofullerene dyad and 1,2-methanofullerene[60] shows a large increase in intensity for a broad band at 500 nm in the dyad despite the lack of an absorbance at >400 nm for BBA. These results indicate the presence of charge-transfer interactions in the C₆₀-BBA methanofullerene dyad between the fullerene moiety and diarylaniline moieties. In the experiment, the researchers used many compounds, for example, 4-Bromo-4′-tert-butylbiphenyl (cas: 162258-89-1Synthetic Route of C16H17Br).

4-Bromo-4′-tert-butylbiphenyl (cas: 162258-89-1) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon閳ユ彽romine 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.Synthetic Route of C16H17Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On the Scope of Trimethylaluminum-Promoted 1,2-Additions of ArZnX Reagents to Aldehydes was written by Glynn, Daniel;Shannon, Jonathan;Woodward, Simon. And the article was included in Chemistry – A European Journal in 2010.Recommanded Product: 35065-86-2 This article mentions the following:

A practical asym. 1,2-addition of functionalized arylzinc halides to aromatic and aliphatic aldehydes is described by the use of aminoalc. catalysis in the presence of AlMe₃. The process is simple to carry out, uses only com. available reagents/ligands and provides moderate to good (80-96 % ee) enantioselectivities for a wide range of substrates. Either com. ArZnX reagents or those prepared in situ from low cost aryl bromides can be used. In the latter case electrophilic functional groups are tolerated (CO₂Et, CN). The reaction relies on rapid exchange between ArZnX and AlMe₃ to generate mixed organometallic species that lead to the formation of a key intermediate that is distinctly different from the classic “anti” transition states of Noyori. NMR monitoring and related experiments have been used to probe the validity of the proposed selective transition state. In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Recommanded Product: 35065-86-2).

3-Bromophenyl acetate (cas: 35065-86-2) 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鑱砨romine bond is electrophilic in nature. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Recommanded Product: 35065-86-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of benzocarbacephem and benzocarbapemen derivatives by copper-promoted intramolecular aromatic substitution was written by Joyeau, Roger;Yadav, Lal D. S.;Wakselman, Michel. And the article was included in Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) in 1987.Product Details of 2178-24-7 This article mentions the following:

Copper-mediated cyclization of 4-[2-(o-bromophenyl)ethyl]azetidinones and 4-[o-bromophenyl)methyl]azetidinones gave benzocarbacephem and benzocarbapenem derivatives resp. Halogenation of the diastereoisomeric 2-hydroxybenzocarbacephem-4′-carboxylate (I, R = OH) afforded I (R=Cl) as racemic diastereoisomers or I (R = F) as a single racemic diastereoisomer. The free carboxylic acids of I (R = Cl, F) were inactivators of 灏?lactamases. In the experiment, the researchers used many compounds, for example, Ethyl (2-bromophenyl)acetate (cas: 2178-24-7Product Details of 2178-24-7).

Ethyl (2-bromophenyl)acetate (cas: 2178-24-7) 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.Product Details of 2178-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Rational Design of a Red Fluorescent Sensor for ALDH1A1 Displaying Enhanced Cellular Uptake and Reactivity was written by Bearrood, Thomas E.;Aguirre-Figueroa, Guadalupe;Chan, Jefferson. And the article was included in Bioconjugate Chemistry in 2020.SDS of cas: 107317-58-8 This article mentions the following:

High aldehyde dehydrogenase 1A1 (ALDH1A1) activity has emerged as a reliable marker for the identification of both normal and cancer stem cells. To facilitate the detection, mol. imaging, and sorting of stem cells, a green fluorescent probe based on the xanthene dye scaffold was recently developed. However, green dyes are less amenable to multicolor imaging because most com. reagents are also green. Overcoming this limitation will enable the simultaneous tracking of multiple stem cell markers. Herein, we report the development of a red congener, red-AlDeSense. Through chem. tuning we were able to achieve excellent isoform selectivity and chemostability, a good turn on response, and enhanced cellular uptake and reactivity. Importantly, red-AlDeSense represents one of only a few turn-on sensors in the red region that use the d-PeT quenching mechanism. By employing red-AlDeSense and a green anti-CD44 antibody, we were able to demonstrate staining of these two stem cell markers is independent of one another in A549 lung adenocarcinoma cells. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-3-(trifluoromethyl)benzoate (cas: 107317-58-8SDS of cas: 107317-58-8).

Methyl 4-bromo-3-(trifluoromethyl)benzoate (cas: 107317-58-8) 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. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. 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.SDS of cas: 107317-58-8

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

One-Pot Copper-Catalyzed Three-Component Reaction of Sulfonyl Azides, Alkynes and Allylamines To Access 2,3-Dihydro-1H-imidazo[1,2-a]indoles was written by Jin, Hongwei;Liu, Daohong;Zhou, Bingwei;Liu, Yunkui. And the article was included in Synthesis in 2020.Reference of 85118-24-7 This article mentions the following:

A copper-catalyzed multicomponent reaction of sulfonyl azides, alkynes and allylamines affording 2,3-dihydro-1H-imidazo-[1,2-a]indoles in moderate yields was reported. Four C-N bonds were constructed by way of azide-alkyne cycloaddition (CuAAC) and double Ullmann-type coupling reactions in a one-pot process. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Reference of 85118-24-7).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) 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. 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.Reference of 85118-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

New method of synthesis of polyene ketones with conjugated double bonds was written by Samokhvalov, G. I.;Miropol’skaya, M. A.;Preobrazhenskii, N. A.. And the article was included in Doklady Akademii Nauk SSSR in 1956.Recommanded Product: 827-24-7 This article mentions the following:

Alcs. of propargyl type react with diketene yielding esters of acetoacetic acid, whose Raman spectrum shows a triple bond line (2112 cm.^-1) indicating no reaction at the terminal link. Heating to 160-70° eliminates CO₂ and yields unsaturated ketones. Condensation of 6-methyl-2-heptenone with C₂H₂ in Na-liquid NH₃ gave 74% 3,7-dimethyloct-6-en-1-yn-3-ol, b₆ 83-4° n_D²⁰ 1.4622, d₂₀ 0.8861. This with diketene in the presence of a little Na gave 72% Me₂C:CHCH₂CH₂CMe(CCH)O₂CCH₂Ac, b_0.2 93-4°, n_D²⁰ 1.4665, d₂₀ 0.9879. This heated in N stream to 160-70° 3 hrs. gave 61% pseudoionone, b_0.1 90-2°, absolute maximum 290 mμ; 2,4-dinitrophenylhydrazone, m. 134-6°. Fractionation of the latter gave mainly the geometric isomer, m. 147.5-48°, and only traces of isomer, m. 119°. The isomer found in major amounts corresponds to the structure of geranial form of citral. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7Recommanded Product: 827-24-7).

2-Bromo-4-methyl-6-nitroaniline (cas: 827-24-7) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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.Recommanded Product: 827-24-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Combination of Methods for in Vitro Study of Antioxidant Properties of Chemical Compounds was written by Menshchikova, E. B.;Zenkov, N. K.;Kandalintseva, N. V.;Prosenko, A. E.. And the article was included in Bulletin of Experimental Biology and Medicine in 2008.HPLC of Formula: 57293-19-3 This article mentions the following:

We proposed a combination of methods to study antioxidant properties of compounds, including evaluation of the capacity of the test preparations to inhibit peroxidation of unsaturated lipids (in model systems with oxidation of Et oleate; aqueous emulsion medium) and low-d. lipoproteins (in the presence of transition metal ions), generation of superoxide anion radical (system of lucigenin, xanthine oxidase, and xanthine) and NO·/ONOO- (system of SIN-1 and lucigenin), and induction of respiratory burst in blood granulocytes (luminol-induced and lucigenin-induced reaction after zymosan stimulation). In vitro study showed that the antioxidant properties of synthetic watersol. phenols depend strongly on masking of the phenol OH group and nature of the ionogenic fragment in the p-Pr substituent. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3HPLC of Formula: 57293-19-3).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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.HPLC of Formula: 57293-19-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide was written by Kankanala, Jayakanth;Ribeiro, Carlos J. A.;Kiselev, Evgeny;Ravji, Azhar;Williams, Jessica;Xie, Jiashu;Aihara, Hideki;Pommier, Yves;Wang, Zhengqiang. And the article was included in Journal of Medicinal Chemistry in 2019.COA of Formula: C8H7BrO2 This article mentions the following:

Topoisomerase II (TOP2) poisons as anticancer drugs work by trapping TOP2 cleavage complexes (TOP2cc) to generate DNA damage. Repair of such damage by tyrosyl DNA phosphodiesterase 2 (TDP2) could render cancer cells resistant to TOP2 poisons. Inhibiting TDP2, thus, represents an attractive mechanism-based chemosensitization approach. Currently known TDP2 inhibitors lack cellular potency and/or permeability. We report herein two novel subtypes of the deazaflavin TDP2 inhibitor core. By introducing an addnl. Ph ring to the N-10 Ph ring (subtype 11) or to the N-3 site of the deazaflavin scaffold (subtype 12), we have generated novel analogs with considerably improved biochem. potency and/or permeability. Importantly, many analogs of both subtypes, particularly compounds 11a, 11e, 12a, 12b, and 12h, exhibited much stronger cancer cell sensitizing effect than the best previous analog 4a toward the treatment with etoposide, suggesting that these analogs could serve as effective cellular probes. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8COA of Formula: C8H7BrO2).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) 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. 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: C8H7BrO2

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