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N’Da, David D.; Smith, Peter J. published an article about the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5,SMILESS:C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3 ).Reference of 7-Chloro-4-(piperazin-1-yl)quinoline. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:837-52-5) through the article.

Quinoline-ferrocene hybrids containing various linkers were synthesized and evaluated for antimalarial and anticancer activities as well as cytotoxicity. The hybrids with rigid linkers are inactive, while those with flexible spacers showed activity against both the D10 and Dd2 strains of Plasmodium falciparum, and demonstrated a good selectivity towards these parasitic cells in comparison with emetine. The hybrid 16, featuring 3-aminopropyl methylamine linker, was the most antimalarial active compound, exhibiting a significantly better potency than chloroquine against the Dd2 strain (IC50 = 0.008 vs. 0.148 μM; 19-fold), and also is significantly more active than the equimolar chloroquine-ferrocene combination (IC50 = 3.7 vs. 41 ng/mL, 10-fold) against the Dd2 strain. Anticancer activity screening showed that all the antimalarial active hybrids also exhibited potent cytostatic (GI50 = 0.6-3.3 μM) and had good cytotoxic effects (LC50 = 6-8 μM) against all three cancer cell lines. The hybrid 11 possessing 1,4-butanediamine linker was distinctively the most antiproliferative of all. It is more cytostatic (GI50: 0.7 vs. 5.9 μM, 8-fold) and (LC50: 6.4 vs. 92.6 μM, 14-fold) more cytotoxic than etoposide against the TK10 (renal) cell line.

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Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Towards the development of 5-HT7 ligands combining serotonin-like and arylpiperazine moieties.

Many known 5-HT7 ligands contain either a serotonin-like or an arylpiperazine structure that, in published SAR studies, are generally supposed to bind the same receptor pocket. Conversely, the authors explored the hypothesis that two such moieties can coexist in the same ligand, binding to different pockets. The authors thus designed and synthesized a set of compounds including both a 5-hydroxyindol-3-ylethyl and a 1-arylpiperazine moieties connected by a short linker, e.g. I [R1 = HO, NH2, Cl, etc.; R2 = Ph, α-naphthyl, β-naphthyl, etc.; X = CH2, O, NH, etc.; Y = (CH2)n; n = 2, 3, 4, 5, 6]. The compounds were tested for their affinity for human 5-HT7 serotonin receptor. The authors further prepared a novel series of 5-HT7 ligands, where the 5-hydroxyindol-3-ylethyl moiety was bioisosterically replaced by a 3-hydroxyanilinoalkyl one. Among the newly synthesized compounds, potent ligands at the 5-HT7 receptor, behaving as antagonists in functional tests, were identified, even if they showed limited subtype selectivity. Docking studies within a model of the 5-HT7 receptor showed that the binding site can actually accommodate both moieties, with the serotonin-like one in the putative orthosteric site and the arylpiperazine one occupying an accessory pocket. The present results demonstrate that it is possible to devise and develop new 5-HT7 ligands merging two privileged structures in the same mol.

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COA of Formula: C13H14ClN3. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis and Antimycobacterial Evaluation of Piperazyl-alkyl-Ether Linked 7-Chloroquinoline-Chalcone/Ferrocenyl Chalcone Conjugates. Author is Singh, Amandeep; Viljoen, Albertus; Kremer, Laurent; Kumar, Vipan.

A series of piperazyl-alkyl-ether linked 7-chloroquinoline-chalcone/ferrocenyl chalcone conjugates were synthesized and evaluated for their anti-mycobacterial activities against the mc26230 strain of Mycobacterium tuberculosis and cytotoxicity against the Vero cell line. While all the compounds showed limited cytotoxicity, the ferrocenyl-chalcone conjugate with pentyl chain as spacer proved to be most potent among the series with a Min. Inhibitory Concentration (MIC) of 14 μg/mL.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 1219741-50-0, is researched, Molecular C9H8BrN, about Organic semiconductor photocatalyst can bifunctionalize arenes and heteroarenes, the main research direction is functionalized arene heteroarene preparation; arene heteroarene functionalization mesoporous graphitic carbon nitride photoredox catalyst.Safety of 6-Bromo-3-methyl-1H-indole.

In photoredox catalysis, an excited chromophore typically activates a single reactant either by oxidizing or reducing it. Ghosh et al. used a semiconductor catalyst to activate two reactants at once by quenching both an excited electron and the residual pos. hole (see the Perspective by Swift). As such, two different reactive carbon or halide fragments could be appended to sep. sites on an aryl ring. The catalyst also tolerated strong nucleophiles such as cyanide and could be recovered easily and reused.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 17696-11-6, is researched, Molecular C8H15BrO2, about A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring Nε-thioacetyl-lysine, the main research direction is cyclic peptide thioacetyllysine synthesis human sirtuin inhibitor structure activity; peptidomimetic solid phase peptide synthesis macrocyclization mol docking; Cyclic peptide; Inhibitor; N(ε)-thioacetyl-lysine; Sirtuin; Structure-activity relationship.Quality Control of 8-Bromooctanoic acid.

Past few years have seen an active pursuit of the inhibitors for the deacylation catalyzed by the seven human sirtuins (i.e. SIRT1-7) as valuable chem. biol./pharmacol. probes of this enzymic deacylation and lead compounds for developing novel therapeutics for human diseases. In the current study, we prepared eight monocyclic and one bicyclic analogs of a linear pentapeptide-based potent (sub-μM IC50’s) pan-SIRT1/2/3 inhibitor Zheng laboratory discovered recently that harbors the catalytic mechanism-based SIRT1/2/3 inhibitory warhead Nε-thioacetyl-lysine at its central position. We found that the bicyclic analog exhibited largely comparable SIRT1/2/3 inhibitory potencies to those of the parent linear pentapeptide, however, the former is proteolytically much more stable than the latter. Moreover, the bicyclic analog displayed very weak inhibition against SIRT5/6/7, was cell permeable, and exhibited an anti-proliferative effect on the human SK-MEL-2 melanoma cells. This bicyclic analog could be a lead for the future development of more potent and still selective pan-SIRT1/2/3 inhibitors whose use in studies on human sirtuin biol., pharmacol., and medicinal chem. could complement with the use of the potent inhibitors selective for a single human sirtuin.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4,4-Dipyridyl Disulfide, is researched, Molecular C10H8N2S2, CAS is 2645-22-9, about Synthesis of Sulfonimidamides from Sulfenamides via an Alkoxy-amino-λ6-sulfanenitrile Intermediate, the main research direction is sulfenamide hypervalent ammonium carbamate iodine oxidation imination; sulfonimidamide preparation; hypervalent iodine; reactive intermediates; sulfonimidamides; sulfur; synthetic methods.Recommanded Product: 2645-22-9.

Sulfonimidamides are intriguing new motifs for medicinal and agrochem., and provide attractive bioisosteres for sulfonamides. However, there remain few operationally simple methods for their preparation Here, the synthesis of NH-sulfonimidamides is achieved directly from sulfenamides, themselves readily formed in one step from amines and disulfides. A highly chemoselective and one-pot NH and O transfer is developed, mediated by PhIO in iPrOH, using ammonium carbamate as the NH source, and in the presence of 1 equiv of acetic acid. A wide range of functional groups are tolerated under the developed reaction conditions, which also enables the functionalization of the antidepressants desipramine and fluoxetine and the preparation of an aza analog of the drug probenecid. The reaction is shown to proceed via different and concurrent mechanistic pathways, including the formation of novel S N sulfanenitrile species as intermediates. Several alkoxy-amino-λ6-sulfanenitriles are prepared with different alcs., and shown to be alkylating agents to a range of nucleophiles.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Ananthan, Subramaniam; Saini, Surendra K.; Zhou, Guangyan; Hobrath, Judith V.; Padmalayam, Indira; Zhai, Ling; Bostwick, J. Robert; Antonio, Tamara; Reith, Maarten E. A.; McDowell, Shea; Cho, Eunie; McAleer, Leah; Taylor, Michelle; Luedtke, Robert R. researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).SDS of cas: 837-52-5.They published the article 《Design, Synthesis, and Structure-Activity Relationship Studies of a Series of [4-(4-Carboxamidobutyl)]-1-arylpiperazines: Insights into Structural Features Contributing to Dopamine D3 versus D2 Receptor Subtype Selectivity》 about this compound( cas:837-52-5 ) in Journal of Medicinal Chemistry. Keywords: aroylaminobutyl arylpiperazine preparation selective dopamine D3 receptor ligand; structure aroylaminobutyl arylpiperazine antagonism partial agonism dopamine D3 receptor; selectivity aroylaminobutyl arylpiperazine binding D3 D2 dopamine receptor; mol docking calculation aroylaminobutyl arylpiperazine bound dopamine D3 receptor; calculated lipophilicity aroylaminobutyl arylpiperazine. We’ll tell you more about this compound (cas:837-52-5).

(Aroylaminobutyl)arylpiperazines such as I were prepared as antagonists or partial agonists of the dopamine D3 receptor selective for D3 receptors over the related dopamine D2 receptors for potential use in treatment of drug addiction and schizophrenia. The calculated lipophilicities of and inhibition of dopamine D3 and D2 receptors by (aroylaminobutyl)arylpiperazines was determined, and the inhibition of mutant and chimeric D3 receptors by selected compounds and the activities of selected compounds in functional assays in human cells were determined Mol. docking calculations of the structures of selected compounds bound to dopamine D3 receptors were performed; the mol. docking studies and evaluation against a set of chimeric and mutant receptors suggest that interactions at the extracellular end of TM7 contribute to the selectivity of the ligands for dopamine D3 receptors over dopamine D2 receptors.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Organic Letters called Organocatalytic Formal (3+2) Cycloaddition toward Chiral Pyrrolo[1,2-a]indoles via Dynamic Kinetic Resolution of Allene Intermediates, Author is Bai, Jian-Fei; Zhao, Lulu; Wang, Fang; Yan, Fachao; Kano, Taichi; Maruoka, Keiji; Li, Yuehui, which mentions a compound: 1219741-50-0, SMILESS is CC1=CNC2=C1C=CC(Br)=C2, Molecular C9H8BrN, Application In Synthesis of 6-Bromo-3-methyl-1H-indole.

The chiral phosphoric acid catalyzed formal (3+2) cycloaddition of 3-substituted 1H-indoles and propargylic alcs. containing a functional directing group (p-NHAc or p-OH) was reported. A straightforward method to synthesize chiral pyrrolo[1,2-a]indole bearing a tetrasubstituted carbon stereocenter was represented. The reaction proceeded smoothly with a wide array of substrate tolerance to deliver various chiral pyrrolo[1,2-a]indoles in up to 93% yield and 98% ee. The utility of this method is highlighted by the diverse transformations of the products into various indole derivatives

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Formula: C8H15BrO2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Photoredox-catalyzed decarboxylative alkylation/cyclization of alkynylphosphine oxides: a metal- and oxidant-free method for accessing benzo[b]phosphole oxides.

By photoredox-catalysis, alkylation/aryl C-H cyclization of readily available alkynylphosphine oxides towards benzo[b]phospholes has been realized under metal- and oxidant-free conditions at room temperature This reaction readily incorporates various functionalized alkyl groups into the benzo[b]phosphole skeletons, representing a mild and versatile tool for the preparation of valuable phosphole compounds

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Quality Control of 7-Chloro-4-(piperazin-1-yl)quinoline. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about N-Propargylated isatin-Mannich mono- and bis-adducts: Synthesis and preliminary analysis of in vitro activity against Tritrichomonas foetus.

Cu(I)Cl promoted synthesis of N-propargylated-isatin Mannich mono- and bis-adducts, e.g. I [R = H, Me, Cl, etc.] with an extension towards the synthesis of N-propargylated-isatin-7-chloroquinoline conjugates was described. The synthesized scaffolds were evaluated for their in vitro activity against the veterinary protozoal pathogen Tritrichomonas fetus and cytotoxicity against human prostate cancer cell line. The preliminary evaluation data revealed the enhancement in the activity profiles with the introduction of 7-chloroquinoline ring with the most active conjugates I [R = H, Cl, Me] exhibiting IC50 of 22.2, 11.3 and 24.5 μM resp. against T. fetus and minimal toxicity against human prostate cell lines.

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