Category: 837-52-5

Guantai, Eric M.; Ncokazi, Kanyile; Egan, Timothy J.; Gut, Jiri; Rosenthal, Philip J.; Bhampidipati, Ravi; Kopinathan, Anitha; Smith, Peter J.; Chibale, Kelly 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 ).Computed Properties of C13H14ClN3. 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.

Analogs of the previously reported antimalarial hybrid compounds I (R1 = Me, 2,4-di-OMe-C6H3) were proposed with the aim of identifying compounds with improved solubility and retained antimalarial potency. In silico characterization predicted improved solubilities of the analogs, particularly at low pH; they retained acceptable predicted permeability properties but were predicted to be susceptible to hepatic metabolism These analogs were synthesized and found to exhibit notable in vitro antimalarial activity. Compounds II (R1 = 2,4-di-OMe-C6H3; R2 = OMe, H) were the most active of the analogs. In vitro metabolism studies indicated susceptibility of the analogs to hepatic metabolism There was also evidence of primary glucuronidation for analogs II (R1 = Me, 2,4-di-OMe-C6H3; R2 = OMe, H). Presumed cis-trans isomerism of I (R1 = Me) and III (R1 = Me, 2,4-di-OMe-C6H3) under in vitro metabolism assay conditions was also observed, with differences in the nature and rates of metabolism observed between isomers. Biochem. studies strongly suggested that inhibition of hemozoin formation is the primary mechanism of action of these analogs.

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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, European Journal of Medicinal Chemistry called Squaric acid/4-aminoquinoline conjugates: Novel potent antiplasmodial agents, Author is Ribeiro, Carlos J. A.; Kumar, S. Praveen; Gut, Jiri; Goncalves, Lidia M.; Rosenthal, Philip J.; Moreira, Rui; Santos, Maria M. M., the main research direction is squaric acid aminoquinoline conjugate preparation antiplasmodial SAR; 4-Aminoquinoline; Antiplasmodial activity; Hybrid; Malaria; Squaramide.Related Products of 837-52-5.

We report the synthesis and structure-activity relationship (SAR) anal. of a series of hybrid compounds containing a squaric moiety conjugated with heterocyclic moieties from well-known antimalarials. This novel series of compounds presents improved antiplasmodial activity compared with the squaric derivatives described in our previous work. Three compounds, I (n = 3, IC50 = 99 nM; n = 4, IC50 = 95 nM) and II (IC50 = 105 nM) had greater in vitro potency than chloroquine (IC50 = 140 nM) against chloroquine resistant Plasmodium falciparum. In addition, they were noncytotoxic against NIH 3T3 and Hek 293T cells.

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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 Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates, the main research direction is piperazinyl quinoline Candida fluconazole sensitivity.Recommanded Product: 837-52-5.

The effectiveness of the potent antifungal drug fluconazole is being compromised by the rise of drug-resistant fungal pathogens. While inhibition of Hsp90 or calcineurin can reverse drug resistance in Candida, such inhibitors also impair the homologous human host protein and fungal-selective chemosensitizers remain rare. The MLPCN library was screened to identify compounds that selectively reverse fluconazole resistance in a Candida albicans clin. isolate, while having no antifungal activity when administered as a single agent. A piperazinyl quinoline was identified as a new small-mol. probe (ML189) satisfying these criteria.

There is still a lot of research devoted to this compound(SMILES：C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3)Recommanded Product: 837-52-5, and with the development of science, more effects of this compound(837-52-5) can be discovered.

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Safety of 7-Chloro-4-(piperazin-1-yl)quinoline. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Development of a lateral flow dipstick for simultaneous and semi-quantitative analysis of dihydroartemisinin and piperaquine in an artemisinin combination therapy. Author is Ning, Xiangxue; Tan, Guiyu; Chen, Xiaojiao; Wang, Mian; Wang, Baomin; Cui, Liwang.

Dihydroartemisinin (DHA) and piperaquine (PPQ) are two drugs used in an artemisinin-based combination therapy (ACT). The circulation of counterfeit antimalarial drugs demands the development of simple, point-of-care (POC) tests for monitoring drug quality. Here we aimed to design an antibody-based lateral flow dipstick assay for simultaneous quality control of DHA and PPQ. To obtain a monoclonal antibody (mAb) for PPQ, one structural unit of the sym. PPQ mol. was used to derive a carboxylic acid for linkage to a carrier protein as immunogen. Screening of hybridoma cells identified an mAb 4D112B2 that reacted with the PPQ-based immunogen. A highly-sensitive icELISA was designed based on this mAb, which showed 50% inhibition concentration of PPQ at 1.66 ng/mL and a working range of 0.35 – 7.40 ng/mL. The mAb showed 10.2, 15.9 and 30.4% cross reactivity to hydroxychloroquine sulfate, chloroquine and amodiaquine, resp. No cross reactivity was observed to lumefantrine, mefloquine artemisinin and its derivatives Using our previous DHA dipstick design, a lateral flow dipstick for simultaneous anal. of PPQ and DHA was developed. The indicator ranges for PPQ and DHA were 2 – 5μg/mL and 250 – 500 ng/mL, resp. The dipstick was used to semi-quant. analyze PPQ and DHA content in com. ACT drugs, which produced agreeable results to those determined by high-performance liquid chromatog. This combination dipstick makes it a potential POC device for quality control of the two active ingredients in a commonly used ACT.

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Computed Properties of C13H14ClN3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis of hydroxypiperaquine, an antimalarial drug. Author is Thai, Hoang; Nguyen, Thac Kim; Nguyen, The Anh.

Piperaquine has been effectively used in combination with dihydroartemisinin for the treatment of the CQ-resistant malaria in Vietnam. At present, this compound is synthesized in our laboratory on multikilogram scale for making the drug artekin for the treatment of malaria. In this paper, we describe the synthesis of hydroxypiperaquine, a derivative of piperaquine. Hydroxypiperaquine is a known antimalarial drug. Hydroxypiperaquine was synthesized by two methods. In the first method, hydroxypiperaquine was synthesized in 50% yield by treatment of two equivalent of 7-chloro-4-(piperazin-1-yl)quinoline with one equivalent of epichlorohydrin. In the second method, hydroxpiperaquine was obtained in 70% yield by reaction of 7-chloro-4-(piperazin-1-yl)quinoline with 1-chloro-3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propan-2-ol. The structures of the intermediates and hydroxypiperaquine were reconfirmed by IR, MS and NMR spectra.

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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 New antiprotozoal agents: Synthesis and biological evaluation of different 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl)methanone derivatives.Formula: C13H14ClN3.

In an endeavor to develop efficacious antiprotozoal agents 4-(7-chloroquinolin-4-yl)(piperazin-1-yl)(pyrrolidin-2-yl)methanone derivatives were synthesized, characterized, and biol. evaluated for antiprotozoal activity. The compounds were screened in vitro against the HM1: IMSS strain of Entamoeba histolytica and NF54 chloroquine-sensitive strain of Plasmodium falciparum. Among the synthesized compounds, six exhibited promising antiamoebic activity with IC50 values (0.14-1.26 μM) lower than the standard drug metronidazole (IC50 1.80 μM). All nine compounds exhibited antimalarial activity (IC50 range: 1.42-19.62 μM), while maintaining a favorable safety profile to host red blood cells. All the compounds were less effective as an antimalarial and more toxic (IC50 range: 14.67-81.24 μM) than quinine (IC50: 275.6 ± 16.46 μM) against the human kidney epithelial cells. None of the compounds exhibited any inhibitory effect on the viability of Anopheles arabiensis mosquito larvae.

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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 Investigation of the mycobacterial enzyme HsaD as a potential novel target for anti-tubercular agents using a fragment-based drug design approach.Synthetic Route of C13H14ClN3.

With the emergence of extensively drug-resistant tuberculosis, there is a need for new anti-tubercular drugs that work through novel mechanisms of action. The meta cleavage product hydrolase, HsaD, has been demonstrated to be critical for the survival of Mycobacterium tuberculosis in macrophages and is encoded in an operon involved in cholesterol catabolism, which is identical in M. tuberculosis and M. bovis BCG. We generated a mutant strain of M. bovis BCG with a deletion of hsaD and tested its growth on cholesterol. Using a fragment based approach, >1000 compounds were screened by a combination of differential scanning fluorometry, NMR spectroscopy, and enzymic assay with pure recombinant HsaD to identify potential inhibitors. We used enzymol. and structural studies to investigate derivatives of the inhibitors identified and to test their effects on growth of M. bovis BCG and M. tuberculosis. The hsaD-deleted strain was unable to grow on cholesterol as sole carbon source but did grow on glucose. Of seven chem. distinct hits from the library, 2 chem. classes of fragments were found to bind in the vicinity of the active site of HsaD by X-ray crystallog. The compounds also inhibited growth of M. tuberculosis on cholesterol. The most potent inhibitor of HsaD was also found to be the best inhibitor of mycobacterial growth on cholesterol-supplemented minimal medium. We propose that HsaD is a novel therapeutic target, which should be fully exploited to design and discover new anti-tubercular drugs.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline(SMILESS: C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3,cas:837-52-5) is researched.Recommanded Product: (R)-2,2′,6,6′-Tetramethoxy-4,4′-bis(diphenylphosphino)-3,3′-bipyridine. The article 《Synthesis of totarol amino alcohol derivatives and their antiplasmodial activity and cytotoxicity》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:837-52-5).

The previously unknown antiplasmodial activity of the plant derived natural product totarol is reported. Novel β-amino alc. derivatives based on this natural product were designed, synthesized and evaluated for in vitro antiplasmodial activity and cytotoxicity. These derivatives showed antiplasmodial IC50 values in the range of 0.6-3.0 μM and were equally active against a chloroquine-sensitive and resistant strain of Plasmodium falciparum, while showing little cytotoxicity against a mammalian cell line (CHO). In terms of lead development, two of the compounds based on substituted phenylpiperazine warrant further investigation as potential antiplasmodial leads. In addition to their selective antiplasmodial activity and lack of chloroquine cross-resistance, these compounds are structurally different to any of the available antimalarial drugs.

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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.Synthetic Route of C13H14ClN3.Umar, Tarana; Shalini, Shruti; Raza, Kausar Md; Gusain, Siddharth; Kumar, Jitendra; Seth, Prerna; Tiwari, Manisha; Hoda, Nasimul published the article 《A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer’s disease》 about this compound( cas:837-52-5 ) in European Journal of Medicinal Chemistry. Keywords: piperazinyl pyrazolopyridinyl acetamide preparation docking cholinesterase inhibitor amyloid aggregation; AChE inhibitors; Amyloid β aggregation inhibitors; Docking; N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides; Selectivity. Let’s learn more about this compound (cas:837-52-5).

2-(Piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides I [R = piperidin-1-yl, 4-methylpiperazin-1-yl, Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, etc.] were described as a new class of selective and potent acetylcholinesterase (AChE) inhibitors and amyloid β aggregation inhibitors. Formation of synthesized compounds I was justified via 1H NMR, 13C NMR, mass spectra and single crystal X-Ray diffraction study. All compounds were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity, inhibition of self-mediated Aβ aggregation and Cu(II)-mediated Aβ aggregation. Also, docking study was carried out in concordance with in vitro results. The most potent mol. amongst the derivatives exhibited excellent anti-AChE activity (IC50 = 4.8 nM). Kinetic study of I [R = 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] suggested it to be a mixed type inhibitor. In vitro study revealed that all the compounds were capable of inhibiting self-induced β-amyloid (Aβ) aggregation with the highest inhibition percentage to be 81.65%. Potency of I [R = Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] to inhibit self-induced Aβ1-42 aggregation was ascertained by TEM anal. Compounds were also evaluated for their Aβ disaggregation, antioxidation, metal-chelation activity.

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Xu, Deyu; Chen, Xiong; Yin, Xiangsheng; Ning, Xiaomin 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 ).Recommanded Product: 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.

Tripiperaquine derivatives [I; Z, Z1 = (CH2)n where n = 2, 3, 4; CH2CHMe, CH2CHRCH2 where R = Cl, HO, PrCO2] were prepared and showed antimalarial activity at 3 mg/kg. Thus, 0.7 mol glycidyl chloride was added to a solution of 0.3 mol piperazine in EtOH at 40-50° and refluxed to give 87.0% II, which (0.01 mol) was refluxed with 0.021 mol III and 2.5 g Et3N in EtOH to give 79% I [Z = Z1 = CH2CH(OH)CH2].

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