Category: 837-52-5

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.Kaur, Hardeep; Balzarini, Jan; de Kock, Carmen; Smith, Peter J.; Chibale, Kelly; Singh, Kamaljit researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).Electric Literature of C13H14ClN3.They published the article 《Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids》 about this compound( cas:837-52-5 ) in European Journal of Medicinal Chemistry. Keywords: cyanopyridine quinoline preparation SAR antiplasmodial activity; 4-Aminoquinoline; Antiplasmodial agents; Cytotoxic activity; Heme binding; Hybrid antimalarials; Pyrimidine. We’ll tell you more about this compound (cas:837-52-5).

A series of hybrids I [R1 = H, 3-NO2, 4-Me, etc, R2 = SMe, morpholinyl; R3 = -NH(CH2)3NH-, -NH(CH2)4NH-, -O(CH2)3NH-, etc.] comprising of 5-cyanopyrimidine and quinoline moiety were synthesized and tested for in vitro antiplasmodial activity against NF54 and Dd2 strains of Plasmodium falciparum. Hybrid bearing m-nitrophenyl substituent at C-4 of pyrimidine displayed the highest antiplasmodial activity [IC50 = 56 nM] against the CQR (Dd2) strain, which is four-fold greater than CQ.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Design, Synthesis, Biological Screening, and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes.Recommanded Product: 837-52-5.

Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. From a library of compounds synthesized, 1-(2-(4-(7-Chloro-4-quinolyl)piperazin-1-yl)acetyl)pyrrolidine (2g) was identified as a potential DPP-IV inhibitor exhibiting better inhibitory activity than P32/98, reference inhibitor. The in vivo studies carried out in STZ and db/db mice models indicated that the compound 2g showed moderate antihyperglycemic activity as compared to the marketed drug Sitagliptin. A two-week repeated dose study in db/db mice revealed that compound 2g significantly declined blood glucose levels with no evidence of hypoglycemia risk. Furthermore, it showed improvement in insulin resistance reversal and antidyslipidemic properties. Mol. docking studies established good binding affinity of compound 2g at the DPP-IV active site and are in favor of the observed biol. data. These data collectively suggest that compound 2g is a good lead mol. for further optimization studies.

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HPLC of Formula: 837-52-5. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis and biological evaluation of certain new cyclohexane-1-carboxamides as apoptosis inducers. Author is Abd-Allah, Walaa Hamada; Elshafie, Mohamed Fathy.

Series of 1-(N-phenyl-2-(heteroalicyclic-1-yl)acetamido)cyclohexane-1-carboxamide derivatives (5a-m) and 1-(phenyl(heteroalicyclic-1-ylmethyl)amino)cyclohexane-1-carboxamide (6a-f) were designed and synthesized with biol. interest through coupling of 1-(2-chloro-N-phenylacetamido)cyclohexane-1-carboxamide (4) and (phenylamino)cycloakanecarboxamide (2) with different amines. The structures of the target compounds were elucidated via IR, 1H and 13C NMR, MS, and microanal. Compounds 5a-m and 6a-f were evaluated for their in vitro antitumor activity against four different cancer cell lines, MCF-7, HepG2, A549, and Caco-2. Compound 5i exhibited a promising activity against breast cancer cell line (IC50 value = 3.25 μM) compared with doxorubicin (IC50 value = 6.77 μM). Results from apoptosis and cell cycle anal. for compound 5i revealed good antitumor activity against MCF-7 cancer cell line and potent inhibition.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 837-52-5, is researched, SMILESS is C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3, Molecular C13H14ClN3Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Optimization of 4-Aminoquinoline/Clotrimazole-Based Hybrid Antimalarials: Further Structure-Activity Relationships, in Vivo Studies, and Preliminary Toxicity Profiling, Author is Gemma, Sandra; Camodeca, Caterina; Sanna Coccone, Salvatore; Joshi, Bhupendra P.; Bernetti, Matteo; Moretti, Vittoria; Brogi, Simone; Bonache de Marcos, Maria Cruz; Savini, Luisa; Taramelli, Donatella; Basilico, Nicoletta; Parapini, Silvia; Rottmann, Matthias; Brun, Reto; Lamponi, Stefania; Caccia, Silvio; Guiso, Giovanna; Summers, Robert L.; E. Martin, Rowena; Saponara, Simona; Gorelli, Beatrice; Novellino, Ettore; Campiani, Giuseppe; Butini, Stefania, the main research direction is antimalarial aminoquinoline clotrimazole hybrid preparation toxicity pharmacokinetics modeling; structure activity antimalarial aminoquinoline clotrimazole hybrid preparation modeling.Computed Properties of C13H14ClN3.

Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development of a novel antimalarial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of clotrimazole-based antimalarials. Here we describe the optimization of this class of hybrid drug through in-depth structure-activity relation studies. Antiplasmodial properties and mode of action were characterized in vitro and in vivo, and interactions with the parasite’s ‘chloroquine resistance transporter’ were investigated in a Xenopus laevis oocyte expression system. These tests indicated that piperazine derivatives 4b and 4d may be suitable for coadministration with chloroquine against chloroquine-resistant parasites. The potential for metabolism of the drugs by cytochrome P 450 was determined in silico, and the lead compounds were tested for toxicity and mutagenicity. A preliminary pharmacokinetic anal. undertaken in mice indicated that compound 4b has an optimal half-life.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ) is researched.Related Products of 837-52-5.Maether, Marie-Pierre; Bernat, Virginie; Maturano, Marie; Andre-Barres, Christiane; Ladeira, Sonia; Valentin, Alexis; Vial, Henri; Payrastre, Corinne published the article 《Synthesis and antiplasmodial activity of streptocyanine/peroxide and streptocyanine/4-aminoquinoline hybrid dyes》 about this compound( cas:837-52-5 ) in Organic & Biomolecular Chemistry. Keywords: streptocyanine dye cyclic peroxide aminoquinoline antiplasmodial. Let’s learn more about this compound (cas:837-52-5).

Two series of streptocyanine dyes incorporating cyclic peroxide or 4-aminoquinoline moieties are prepared and X-ray diffraction structures for three compounds are determined All hybrid dyes show good antiplasmodial activity (0.06 to 0.66 μM) and are not or are slightly cytotoxic, except 10a.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum, published in 2007-01-01, which mentions a compound: 837-52-5, Name is 7-Chloro-4-(piperazin-1-yl)quinoline, Molecular C13H14ClN3, Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline.

A targeted series of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives were synthesized and evaluated in vitro against the malarial cysteine protease falcipain-2 and a chloroquine resistant strain (W2) of Plasmodium falciparum. A novel series of 4-aminoquinoline semicarbazones were the most effective inhibitors of falcipain-2 (most potent inhibitor had IC50 = 0.63 μM) while a bisquinoline semicarbazone compound 8f (I) was the most potent antimalarial compound with an IC50 of 0.07 μM against W2. Compound 8f also weakly inhibited falcipain-2, with an IC50 of 3.16 μM, although its principal antiparasitic activity did not appear to be due to inhibition of this enzyme.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety, the main research direction is oxadiazolylmethylpiperazinyl quinoline derivative preparation antituberculosis; Antitubercular activity; Bioavailability; Cytotoxicity; Oxadiazole; Quinoline.Reference of 7-Chloro-4-(piperazin-1-yl)quinoline.

Tuberculosis is the infectious disease caused by mycobacterium tuberculosis (Mtb), responsible for the utmost number of deaths annually across the world. Herein, twenty-one new substituted 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl-quinoline derivatives were designed and synthesized through multistep synthesis followed by in vitro evaluation of their antitubercular potential against Mtb WT H37Rv. The compound I was found to be promising with MIC value of 0.5 μg/mL and QD-19 to QD-21 were also remarkable with MIC value of 0.25 μg/mL. Addnl., we have carried out experiments to confirm the metabolic stability, cytotoxicity and pharmacokinetics of these compounds along with kill kinetics of QD-18. These compounds were found to be orally bioavailable and highly effective. Altogether, these results indicate that I and II (R = 2,3-Me2Ph, cyclopentyl, and 4-iPrPh) are promising lead compounds for the development of a novel chem. class of antitubercular drugs.

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Solomon, V. Raja; Pundir, Sheetal; Lee, Hoyun published the article 《Examination of novel 4-aminoquinoline derivatives designed and synthesized by a hybrid pharmacophore approach to enhance their anticancer activities》. Keywords: structure activity aminoquinoline antitumor; bortezomib monastrol aminoquinoline derivative anticancer breast cancer progression.They researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).Category: bromides-buliding-blocks. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:837-52-5) here.

In an attempt to develop effective and potentially safe anticancer agents, thirty-six 4-aminoquinoline-derived sulfonyl analogs I (R = CH3, 4-ClC6H4, p-tolyl, etc., X = Cl, CF3) and II were designed and synthesized using a hybrid pharmacophore approach. The cytotoxicity of these compounds was determined using three breast tumor cell lines (MDA-MB231, MDA-MB468 and MCF7) and two matching non-cancer breast epithelial cell lines (184B5 and MCF10A). Although most of the compounds were quite effective on the breast cancer cells, I [R = 2,4-(O2N)2C6H3, X = Cl] (III; VR23) emerged as potentially the most desirable one in this series of compounds Data from the NCI-60 cancer panel screening show that compound III is effective on a wide range of different cancers. Importantly, compound III needed up to 17.6-fold less doses to achieve the same IC50 against cancer than non-cancer cells (MDA-MB468 vs MCF10A), suggesting that it can potentially be less toxic to normal cells. Cancer cells formed multiple centrosomes in the presence of compound III, resulting in the cell cycle arrest at prometa-meta phase. This abnormality leads to eventual cell demise with sub-G1 DNA content typically shown with apoptotic cells. In addition, compound III also causes an increase in lysosomal volume in cancer but not in non-cancer cells, which may contribute at least in part to its preferential cancer cell-killing. The cancer cell-killing effect of compound III is highly potentiated when combined with either bortezomib or monastrol.

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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: 837-52-5, is researched, Molecular C13H14ClN3, about Antimalarials. 7-Chloro-4-(substituted amino)quinolines, the main research direction is quinoline antimalarial; chloroquinolines antimalarial.Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline.

Forty-one 7-chloro-4-(substituted amino)quinolines were prepared from 4,7-dichloroquinoline and tested for antimalarial activity against Plasmodium berghei in mice. Of 27 active compounds, 7-chloro-4-[(1-ethyl-3-piperidyl)-amine]quinoline (I) and 7-chloro-4-[[4-(benzyl-2-propynylamino]-2-butyl]amino]quinoline (II) were curative antimalarial agents at doses of 80 and 160 mg/kg, i.p.,resp.

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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, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids, Author is Lombard, Marli C.; N’Da, David D.; Breytenbach, Jaco C.; Smith, Peter J.; Lategan, Carmen A., which mentions a compound: 837-52-5, SMILESS is C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3, Molecular C13H14ClN3, Computed Properties of C13H14ClN3.

Dihydroartemisinin (DHA) was coupled to different aminoquinoline moieties forming hybrids, which were then treated with oxalic acid to form oxalate salts. Some of the compounds showed comparable potency in vitro to that of chloroquine (CQ) against the chloroquine sensitive (CQS) strain, and were found to be more potent against the chloroquine resistant CQR strain. Hybrid I and its oxalate salt were the most active against CQR strain, being 9- and 7-fold more active than CQ resp. (17.12 nM; 20.76 nM vs. 157.9 nM). An optimum chain length was identified having 2 or 3 Cs with or without an extra methylene substituent.

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