Tag: M.W=200-300

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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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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Bromide – Wikipedia,
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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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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Twist-Bend Nematic Glasses: The Synthesis and Characterisation of Pyrene-based Nonsymmetric Dimers, published in 2021-03-01, which mentions a compound: 17696-11-6, mainly applied to pyrene liquid crystal dimer preparation twist bend nematic phase; glassy phase; liquid crystals; pyrene; spontaneous chirality; twist-bend nematic, Electric Literature of C8H15BrO2.

A selection of pyrene-based liquid crystal dimers I [n = 5, 6, 8, etc.] , II [n = 5, 6, 11, etc.] and III were prepared, containing either methylene-ether or diether linked spacers of varying length and parity. All the diether linked materials, II, exhibited conventional nematic and smectic A phases, with the exception of II [n = 11] which was exclusively nematic. The methylene-ether linked dimer, I with an even-membered spacer (n=5) was solely nematogenic, but odd-members (n=6, 8, 10) exhibited both nematic and twist-bend nematic phases. Replacement of the cyanobiphenyl fragment by cyanoterphenyl giving III, gave elevated melting and nematic-isotropic transition temperatures, and SmA and SmCA phases were observed on cooling the nematic phase. Intermol. face-to-face associations of the pyrene moieties drove glass formation, and all these materials had a glass transition temperature at or above room temperature The stability of the glassy twist-bend nematic phase allowed for its study using AFM, and the helical pitch length, PTB, was measured as 6.3 and 6.7 nm for I [n = 6, 8] , resp. These values were comparable to the shortest pitch of a twist-bend nematic phase measured to date.

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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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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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Bromide – Wikipedia,
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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Visible-light-induced metathesis reaction between diselenide and ditelluride, published in 2019, which mentions a compound: 17696-11-6, mainly applied to diselenide ditelluride metathesis reaction kinetics radical mechanism, Quality Control of 8-Bromooctanoic acid.

The Se-Te bond was prepared by a metathesis reaction between diselenides and ditellurides, which could be manipulated with the presence or absence of visible light. Addnl., the apparent activation energy of the exchange process was measured to be only 28.01 kJ mol-1, explaining the high reactivity and sensitivity to light.

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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: 6-Bromo-3-methyl-1H-indole, is researched, Molecular C9H8BrN, CAS is 1219741-50-0, about Construction of 9H-Pyrrolo[1,2-a]indoles by a Copper-Catalyzed Friedel-Crafts Alkylation/Annulation Cascade Reaction.Recommanded Product: 1219741-50-0.

An efficient and concise Cu(OTf)2-catalyzed Friedel-Crafts alkylation/annulation cascade reaction of substituted indoles with 1,2-dicarbonyl-3-enes has been established. This reaction uses readily available starting materials and is operationally simple, thus representing a practical method for the construction of diverse 9H-pyrrolo[1,2-a]indoles bearing a carbonyl group.

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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.Product Details of 837-52-5.Musonda, Chitalu C.; Little, Susan; Yardley, Vanessa; Chibale, Kelly published the article 《Application of multicomponent reactions to antimalarial drug discovery. Part 3: Discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro》 about this compound( cas:837-52-5 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: aminoquinoline aminoxazole preparation multicomponent reaction antimalarial activity; oxazole amino quinoline preparation multicomponent reaction antimalarial activity. Let’s learn more about this compound (cas:837-52-5).

The synthesis and antimalarial activity of a novel series of first generation 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles, e.g. I (R = H, Me; n = 1, 2, 3, 5), against two strains of the Plasmodium falciparum parasite in vitro is described. A number of compounds significantly more potent than the standard drug chloroquine were identified.

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Application of 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. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.

A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines (e.g. I and II) were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-aminoacridine analogs were also prepared and shown to have low nanomolar activity like their quinoline counterparts.

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Bromide – Wikipedia,
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