Category: 837-52-5

Application of 837-52-5. 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 Arylpiperazines displaying preferential potency against chloroquine-resistant strains of the malaria parasite Plasmodium falciparum. Author is Molyneaux, Carrie-Anne; Krugliak, Miriam; Ginsburg, Hagai; Chibale, Kelly.

Arylpiperazines in which the terminal secondary amino group is unsubstituted were found to display a mefloquine-type antimalarial behavior in being significantly more potent against the chloroquine-resistant (W2 and FCR3) strains of Plasmodium falciparum than against the chloroquine-sensitive (D10 and NF54) strains. Substitution of the aforementioned amino group led to a dramatic drop in activity across all strains as well as abolition of the preferential potency against resistant strains that was observed for the unsubstituted counterparts. The data suggest that unsubstituted arylpiperazines are not well-recognized by the chloroquine resistance mechanism and may imply that they act mechanistically differently from chloroquine. On the other hand, 4-aminoquinoline-based heteroarylpiperazines in which the terminal secondary amino group is also unsubstituted, were found to be equally active against the chloroquine-resistant and chloroquine-sensitive strains, suggesting that chloroquine cross-resistance is not observed with these two 4-aminoquinolines. In contrast, two 4-aminoquinoline-based heteroarylpiperazines are pos. recognized by the chloroquine resistance mechanism. These studies provide structural features that determine the antimalarial activity of arylpiperazines for further development, particularly against chloroquine-resistant strains.

《Arylpiperazines displaying preferential potency against chloroquine-resistant strains of the malaria parasite Plasmodium falciparum》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(7-Chloro-4-(piperazin-1-yl)quinoline)Application of 837-52-5.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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 Hybrid 4-Aminoquinoline-1,3,5-triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation, published in 2015, which mentions a compound: 837-52-5, mainly applied to aminoquinolinetriazine preparation antibacterial SAR, Electric Literature of C13H14ClN3.

A series of novel 4-aminoquinoline 1,3,5-triazine derivatives e.g., I were synthesized and their antibacterial activities were tested against three Gram-pos. bacteria, namely Bacillus subtilis (NCIM-2063), Bacillus cereus (NCIM-2156), and Staphylococcus aureus (NCIM-2079), and four Gram-neg. bacteria, namely Proteus vulgaris (NCIM-2027), Proteus mirabilis (NCIM-2241), Escherichia coli (NCIM-2065), and Pseudomonas aeruginosa (NCIM-2036), using ciprofloxacin as reference standard drug. Results showed compound with p-aminophenol substitution on 1,3,5-triazine nucleus is a more potent antibacterial agent than derivative with 1,3-diaminopropane group against all bacterial strains except Bacillus cereus (NCIM-2156).

Different reactions of this compound(7-Chloro-4-(piperazin-1-yl)quinoline)Electric Literature of C13H14ClN3 require different conditions, so the reaction conditions are very important.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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 Investigation on the synthesis of piperaquine, a component of the antimalarial drug artekin, the main research direction is piperaquine synthesis antimalarial.Category: bromides-buliding-blocks.

Plasmodium falciparum malaria remains a serious endemic disease in many parts of the world. It is estimated that 120 million cases occur worldwide each year, causing over one million deaths. The problem has been compounded by the emergence of strains of P. falciparum resistant to virtually all antimalarial agents. Resistance to chloroquine has now spread to almost all areas where malaria is endemic. Chloroquine-resistant strains are typically cross resistant to all drugs of relative chem. structure, and therefore the need for finding new mols. with novel modes of action is urgent. In an effort to discover active compounds against the chloroquine resistant malaria, several bis(quinolyl)piperazines such as piperaquine have been reported. Piperaquine has been effectively used in combination with dihydroartemisinin for treatment of the CQ-resistant malaria in Vietnam. However, Vietnam is still dependent upon the import of this compound In this article, the authors report the synthesis of piperaquine by reaction of 4,7-dichloroquinoline with N-formylpiperazine, followed by deprotection, and reaction with 1,3-dibromopropane.

Different reactions of this compound(7-Chloro-4-(piperazin-1-yl)quinoline)Category: bromides-buliding-blocks require different conditions, so the reaction conditions are very important.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline. 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 New piperazine-derived nnrtis as anti-HIV agent: synthesis, biological evaluation and molecular docking studies. Author is Kushwaha, Ram Najar; Debnath, Utsab; Singh, Pankaj; Saxena, Reshu; Gupta, Satish Kumar; Tripathi, Raj Kamal; Siddiqui, Hefazat Husain; Katti, Seturam Bandhacharya.

A new series of piperazine-derived compounds were synthesized and evaluated as HIV-1 reverse transcriptase (HIV-1 RT) inhibitors. Flexibility of the piperazine structure plays an importance role for its diverse pharmacol. properties and medicinal potentialities. Compounds having better inhibitory activities against HIV-1 RT were tested for their anti-HIV activity in TZM-bl cell line. Among tested compounds, 9k exhibited better anti-HIV activity with an IC50 value of 13.18 ± 1.62 μg/mL and a therapeutic index value of 2.26 in TZM-bl cell line. Furthermore, mol. docking anal. revealed the similar binding modes of 9k and delavirdine with HIV-1 RT in which carbonyl group of 9k established hydrogen bonding with Lys103 residue as delavirdine, and other hydrophobic groups were stabilized with hydrophobic area (TRP229, LEU100, TYR188, PHE227, VAL106, PRO236, TYR181, TYR188, TRP229, and TYR318 residues) of HIV-1 RT. Present study suggests that compound 9k may serve as a new lead template for further modification to obtain therapeutically useful mol. for the treatment of HIV infection.

The article 《New piperazine-derived nnrtis as anti-HIV agent: synthesis, biological evaluation and molecular docking studies》 also mentions many details about this compound(837-52-5)Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline, you can pay attention to it, because details determine success or failure

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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 Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group, published in 2012-08-15, which mentions a compound: 837-52-5, mainly applied to antidiabetic DPP4 inhibitor heteroarylpiperazine prolylthiazolidine preparation structure activity, Application of 837-52-5.

Hypoglycemic agents with a mechanism of dipeptidyl peptidase IV (DPP-4) inhibition are suitable for once daily oral dosing. It is difficult to strike a balance between inhibitory activity and duration of action in plasma for inhibitors bearing an electrophilic nitrile group. We explored fused bicyclic heteroarylpiperazine substituted at the γ-position of the proline structure in the investigation of L-prolylthiazolidines lacking the electrophilic nitrile. Among them, 2-trifluoroquinolyl compound 8g is the most potent, long-lasting DPP-4 inhibitor (IC50 = 0.37 nmol/L) with high selectivity against other related peptidases. X-ray crystal structure determination of 8g indicates that CH-π interactions generated between the quinolyl ring and the guanidinyl group of Arg358 enhances the DPP-4 inhibitory activity and selectivity.

The article 《Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group》 also mentions many details about this compound(837-52-5)Application of 837-52-5, you can pay attention to it, because details determine success or failure

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Application of 837-52-5. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. Author is Vennerstrom, Jonathan L.; Ager, Arba L. Jr.; Dorn, Arnulf; Andersen, Steven L.; Gerena, Lucia; Ridley, Robert G.; Milhous, Wilbur K..

N,N-Bis(7-chloroquinolin-4-yl)heteroalkanediamines I [R = HN(CH2)2O(CH2)2NH, HN(CH2)3O(CH2)4O(CH2)3NH, HN(CH2)6NH(CH2)6NH, etc.] were synthesized and screened against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. These bisquinolines had IC50 values from 1 to 100 nM against P. falciparum in vitro. Six of the 11 bisquinolines were significantly more potent against the chloroquine-resistant W2 clone compared to the chloroquine-sensitive D6 clone. For bisquinolines I, there was no relationship between the length of the bisquinoline heteroalkane bridge and antimalarial activity and no correlation between in vitro and in vivo antimalarial activities. Bisquinolines with alkyl ether and piperazine bridges were substantially more effective than bisquinolines with alkylamine bridges against P. berghei in vivo. Ten of the bisquinolines were potent inhibitors of hematin polymerization with IC50 values falling in the narrow range of 5-20 μM, and there was a correlation between potency of inhibition of hematin polymerization and inhibition of parasite growth. Compared to alkane-bridged bisquinolines (Vennerstrom et al., 1992), none of these heteroalkane-bridged bisquinolines had sufficient antimalarial activity to warrant further investigation of the series.

The article 《Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines》 also mentions many details about this compound(837-52-5)Application of 837-52-5, you can pay attention to it, because details determine success or failure

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation. Author is Singh, Amandeep; Rani, Anu; Gut, Jiri; Rosenthal, Philip J.; Kumar, Vipan.

A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38 μM against chloroquine-resistant and mefloquine-sensitive W2 strain of P. falciparum. The submicromolar activities of most of the synthesized conjugates suggest that such mol. frameworks can act as therapeutic templates for the design and synthesis of new antimalarials.

The article 《Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation》 also mentions many details about this compound(837-52-5)Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline, you can pay attention to it, because details determine success or failure

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Related Products 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 7-Chloroquinoline-isatin Conjugates: Antimalarial, Antitubercular, and Cytotoxic Evaluation.

A series of twenty piperazine-tethered 7-chloroquinoline-isatin hybrids have been synthesized via either direct nucleophilic substitution or Cu(Ι)Cl-mediated Mannich reaction. These new conjugates were evaluated for their antimalarial and antitubercular efficacy against a chloroquine-resistant strain of Plasmodium falciparum and Mycobacterium tuberculosis, resp., while the cytotoxic profiles were evaluated against 3T6 cell line, a permanent mouse embryonic fibroblast cell line. The most potent of the test compound with IC50 of 0.22 μm against W2 strain of P. falciparum and 31.62 μm against the embryonic fibroblast cell line (cytotoxicity) displayed a high selective index of 143.73.

The article 《7-Chloroquinoline-isatin Conjugates: Antimalarial, Antitubercular, and Cytotoxic Evaluation》 also mentions many details about this compound(837-52-5)Related Products of 837-52-5, you can pay attention to it, because details determine success or failure

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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: 1001-26-9. The article 《Synthesis and characterization of impurities present in an antimalarial drug piperaquine phosphate》 in relation to this compound, is published in Indian Journal of Heterocyclic Chemistry. Let’s take a look at the latest research on this compound (cas:837-52-5).

Six impurities formed during the process development of piperaquine phosphate, were identified as 7-chloro-4-(piperazine-1-yl)quinoline, 3-(4-(7-chloroquinolin-4-yl)piperazine-1-yl)propan-1-ol, 7-chloro-4-(4-(3-ethoxypropyl)piperazine-1-yl)quinoline, 1,4-bis(7-chloro-4-quinolinyl)piperazine, I [X = (CH2)3] and II by LC-MS. The structures of these impurities were further confirmed by synthesis. HPLC anal. of piperaquine phosphate API showed impurities ranging from 0.05 to 0.22%.

Different reactions of this compound(7-Chloro-4-(piperazin-1-yl)quinoline)Reference of 7-Chloro-4-(piperazin-1-yl)quinoline require different conditions, so the reaction conditions are very important.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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 The Ca2+-ATPase (SERCA1) Is Inhibited by 4-Aminoquinoline Derivatives through Interference with Catalytic Activation by Ca2+, Whereas the ATPase E2 State Remains Functional.COA of Formula: C13H14ClN3.

Several clotrimazole (CLT) and 4-aminoquinoline derivatives were synthesized and found to exhibit in vitro antiplasmodial activity with IC50 ranging from nM to μM values. We report here that some of these compounds produce inhibition of rabbit sarcoplasmic reticulum Ca2+-ATPase (SERCA1) with IC50 values in the μM range. The highest affinity for the Ca2+-ATPase was observed with NF1442 (N-((3-chlorophenyl)(4-((4-(7-chloroquinolin-4-yl)piperazin-1-yl)methyl)phenyl)methyl)-7-chloro-4-aminoquinoline) and NF1058 (N-((3-chlorophenyl)(4-(pyrrolidin-1-ylmethyl)phenyl)methyl)-7-chloro-4-aminoquinoline),yielding IC50 values of 1.3 and 8.0 μM as demonstrated by measurements of steady state ATPase activity as well as single cycle charge transfer. Characterization of sequential reactions comprising the ATPase catalytic and transport cycle then demonstrated that NF1058, and similarly CLT, interferes with the mechanism of Ca2+ binding and Ca2+-dependent enzyme activation (E2 to E1·Ca2 transition) required for formation of phosphorylated intermediate by ATP utilization. On the other hand, Ca2+ independent phosphoenzyme formation by utilization of Pi (i.e. reverse of the hydrolytic reaction in the absence of Ca2+) was not inhibited by NF1058 or CLT. Comparative experiments showed that the high affinity inhibitor thapsigargin interferes not only with Ca2+ binding and phosphoenzyme formation with ATP but also with phosphoenzyme formation by utilization of Pi even though this reaction does not require Ca2+. It is concluded that NF1058 and CLT inhibit SERCA by stabilization of an E2 state that, as opposed to that obtained with thapsigargin, retains the functional ability to form E2-P by reacting with Pi.

Different reactions of this compound(7-Chloro-4-(piperazin-1-yl)quinoline)COA of Formula: C13H14ClN3 require different conditions, so the reaction conditions are very important.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary