Tag: 200-300

Polyamide-Scorpion cyclam lexitropsins selectively bind AT-rich DNA independently of the nature of the coordinated metal was written by Lo, Anthony T. S.;Salam, Noeris K.;Hibbs, David E.;Rutledge, Peter J.;Todd, Matthew H.. And the article was included in PLoS One in 2011.HPLC of Formula: 1196-90-3 This article mentions the following:

Cyclam was attached to 1-, 2- and 3-pyrrole lexitropsins for the first time through a synthetically facile copper-catalyzed “click” reaction. The corresponding copper and zinc complexes were synthesized and characterized. The ligand and its complexes bound AT-rich DNA selectively over GC-rich DNA, and the thermodn. profile of the binding was evaluated by isothermal titration calorimetry. The metal, encapsulated in a scorpion azamacrocyclic complex, did not affect the binding, which was dominated by the organic tail. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate (cas: 1196-90-3HPLC of Formula: 1196-90-3).

Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate (cas: 1196-90-3) 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.HPLC of Formula: 1196-90-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Phenotypic Screening-Based Identification of 3,4-Disubstituted Piperidine Derivatives as Macrophage M2 Polarization Modulators: An Opportunity for Treating Multiple Sclerosis was written by Weng, Qinjie;Che, Jinxin;Zhang, Zhikang;Zheng, Jiahuan;Zhan, Wenhu;Lin, Sendong;Tian, Tian;Wang, Jincheng;Gai, Renhua;Hu, Yongzhou;Yang, Bo;He, Qiaojun;Dong, Xiaowu. And the article was included in Journal of Medicinal Chemistry in 2019.Reference of 179232-29-2 This article mentions the following:

Multiple sclerosis (MS) is a disease of the autoimmune-mediated disorder in the central nervous system, for which no effective therapeutic agent is currently available. The regulation of macrophage polarization toward M2 is a general benefit for treating MS. The gene biomarker-based phenotypic screening approach was developed, and 3,4-disubstituted piperidine derivative S-28 was identified as a lead compound modulating macrophage M2 polarization. Further SAR studies resulted in the discovery of the most potent modulator D11 that showed good oral bioavailability and significant in vivo therapeutic effects. Mechanistic studies demonstrated that the M2 polarization macrophages modulated by D11 mainly functioned through inhibiting the proliferation of T-cells and activating the phosphorylation of Stat3 and Akt. Therefore, the gene biomarker-based phenotypic screening was demonstrated as a promising tool for the discovery of novel macrophage M2 polarization modulators. Compound D11 may serve as a promising starting point for the development of therapeutics to treat MS. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Reference of 179232-29-2).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) 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. 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.Reference of 179232-29-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17 was written by Baqi, Younis;Pillaiyar, Thanigaimalai;Abdelrahman, Aliaa;Kaufmann, Olesja;Alshaibani, Samer;Rafehi, Muhammad;Ghasimi, Saman;Akkari, Rhalid;Ritter, Kirsten;Simon, Katharina;Spinrath, Andreas;Kostenis, Evi;Zhao, Qiang;Kose, Meryem;Namasivayam, Vigneshwaran;Muller, Christa E.. And the article was included in Journal of Medicinal Chemistry in 2018.Formula: C6H5BrClN This article mentions the following:

The orphan receptor GPR17 may be a novel drug target for inflammatory diseases. 3-(2-Carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid (MDL29,951, 1) was previously identified as a moderately potent GPR17 agonist. In the present study, we investigated the structure-activity relationships (SARs) of 1. Substitution of the indole 1-, 5-, or 7-position was detrimental. Only small substituents were tolerated in the 4-position while the 6-position accommodated large lipophilic residues. Among the most potent compounds were 3-(2-carboxyethyl)-1H-indole-2-carboxylic acid derivatives containing the following substituents: 6-phenoxy (26, PSB-1737, EC₅₀ 270 nM), 4-fluoro-6-bromo (33, PSB-18422, EC₅₀ 27.9 nM), 4-fluoro-6-iodo (35, PSB-18484, EC₅₀ 32.1 nM), and 4-chloro-6-hexyloxy (43, PSB-1767, EC₅₀ 67.0 nM). (3-(2-Carboxyethyl)-6-hexyloxy-1H-indole-2-carboxylic acid (39, PSB-17183, EC₅₀ 115 nM) behaved as a partial agonist. Selected potent compounds tested at human P2Y receptor subtypes showed high selectivity for GPR17. Docking into a homol. model of the human GPR17 and mol. dynamic simulation studies rationalized the observed SARs. In the experiment, the researchers used many compounds, for example, 3-Bromo-5-chlorophenylamine (cas: 96558-78-0Formula: C6H5BrClN).

3-Bromo-5-chlorophenylamine (cas: 96558-78-0) 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. 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: C6H5BrClN

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Antagonists of the human adenosine A_2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines was written by Gillespie, Roger J.;Cliffe, Ian A.;Dawson, Claire E.;Dourish, Colin T.;Gaur, Suneel;Jordan, Allan M.;Knight, Antony R.;Lerpiniere, Joanne;Misra, Anil;Pratt, Robert M.;Roffey, Jonathan;Stratton, Gemma C.;Upton, Rebecca;Weiss, Scott M.;Williamson, Douglas S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Recommanded Product: 3-(Bromomethyl)benzoic acid This article mentions the following:

A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A_2A antagonists is described. Many examples were highly selective against the human A₁ receptor sub-type and were active in an in vivo model of Parkinson’s disease. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Recommanded Product: 3-(Bromomethyl)benzoic acid).

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. 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: 3-(Bromomethyl)benzoic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

A carbon-13 NMR investigation of [5]metacyclophanes was written by Jenneskens, L. W.;De Kanter, F. J. J.;De Wolf, W. H.;Bickelhaupt, F.. And the article was included in Magnetic Resonance in Chemistry in 1986.COA of Formula: C8H8Br2 This article mentions the following:

¹³C NMR data of [5]metacyclophane, its 8,11-dihalosubstituted derivatives and of some model compounds are reported and discussed. A remarkable downfield shift is observed for the aromatic carbon between the bridging carbons; this is tentatively ascribed to long-range effects of the bridge and to the bending of the aromatic ring. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2COA of Formula: C8H8Br2).

2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2) 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.COA of Formula: C8H8Br2

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

Enantioselective semireduction of allenes was written by Chen, Zhiwei;Dong, Vy M.. And the article was included in Nature Communications in 2017.Electric Literature of C9H11BrO This article mentions the following:

Herein, Rh-catalyzed regio- and enantioselective semiredn. of allenes to generate chiral benzylic motifs is reported. Rh-hydride catalysis solves a synthetic challenge by affording the enantioselective reduction of allenes, thereby yielding access to motifs commonly used in medicinal chem. A designer Josiphos ligand promotes the generation of chiral benzylic isomers, when combined with a Hantzsch ester as the reductant. This semiredn. proceeds chemoselectively in the presence of other functional groups, which are typically reduced using conventional hydrogenations. Isotopic labeling studies support a mechanism where the hydride is delivered to the branched position of a Rh-allyl intermediate. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Electric Literature of C9H11BrO).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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.Electric Literature of C9H11BrO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters was written by Hernandez-Olmos, Victor;Heering, Jan;Planz, Viktoria;Liu, Ting;Kaps, Alexander;Rajkumar, Rinusha;Gramzow, Matthias;Kaiser, Astrid;Schubert-Zsilavecz, Manfred;Parnham, Michael J.;Windbergs, Maike;Steinhilber, Dieter;Proschak, Ewgenij. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 653-92-9 This article mentions the following:

The first potent leukotriene B4 (LTB4) receptor type 2 (BLT2) agonists, endogenous 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT), and synthetic CAY10583 (CAY) have been recently described to accelerate wound healing by enhanced keratinocyte migration and indirect stimulation of fibroblast activity in diabetic rats. CAY represents a very valuable starting point for the development of novel wound-healing promoters. In this work, the first structure-activity relationship study for CAY scaffold-based BLT2 agonists is presented. The newly prepared derivatives showed promising in vitro wound-healing activity. In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Product Details of 653-92-9).

Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) 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). 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.Product Details of 653-92-9

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Development of ¹⁸F-labeled radiotracers for PET imaging of the adenosine A₂A receptor: synthesis, radiolabeling and preliminary biological evaluation was written by Lai, Thu Hang;Schroder, Susann;Toussaint, Magali;Dukic-Stefanovic, Sladjana;Kranz, Mathias;Ludwig, Friedrich-Alexander;Fischer, Steffen;Steinbach, Jorg;Deuther-Conrad, Winnie;Brust, Peter;Moldovan, Rares-Petru. And the article was included in International Journal of Molecular Sciences in 2021.Related Products of 61150-57-0 This article mentions the following:

The adenosine A2A receptor (A2AR) represents a potential therapeutic target for neurodegenerative diseases. Aiming at the development of a positron emission tomog. (PET) radiotracer to monitor changes of receptor d. and/or occupancy during the A2AR-tailored therapy, authors designed a library of fluorinated analogs based on a recently published lead compound (PPY). Among those, the highly affine 4-fluorobenzyl derivate (K_i(hA_2AR) = 5.3 nM) and the 2-fluorobenzyl derivate (K_i(hA_2AR) = 2.1 nM) were chosen for ¹⁸F-labeling via an alc. enhanced copper-mediated procedure starting from the corresponding boronic acid pinacol ester precursors. Investigations of the metabolic stability of compound I (R = p-¹⁸F, o-¹⁸F) in CD-1 mice by radio-HPLC anal. revealed parent fractions of more than 76% of total activity in the brain. Specific binding of I (R = o-¹⁸F)on mice brain slices was demonstrated by in vitro autoradiog. In vivo PET/magnetic resonance imaging (MRI) studies in CD-1 mice revealed a reasonable high initial brain uptake for both radiotracers, followed by a fast clearance. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0Related Products of 61150-57-0).

2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0) 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. 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.Related Products of 61150-57-0

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