Month: April 2022

Application of 837-52-5. 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 Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents. Author is Thakur, Anuj; Khan, Shabana I.; Rawat, Diwan S..

A series of 4-aminoquinoline-pyrimidine hybrids linked through piperazine were synthesized and evaluated for their in vitro antimalarial activity against chloroquine (CQ)-sensitive and chloroquine (CQ)-resistant strains of Plasmodium falciparum and cytotoxicity against mammalian cell line (Vero). Nine compounds (5e, 5f, 5g, 5h, 5i, 5j, 5k, 7a, 7d) displayed good antimalarial activity against both the strains out of which compound 5j was the most potent with IC50 values in the range of 0.13-0.14 μM. The antimalarial activity of 5j was 2.5 fold stronger than chloroquine in the CQ-resistant strain of P. falciparum. None of the compounds were found to be cytotoxic against Vero cells. The X-ray crystal structure of one of the compounds was also determined

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Bromide – Wikipedia,
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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 and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents, the main research direction is aminoquinoline tetrazole preparation antimalarial malaria treatment Plasmodium falciparum; 4-Aminoquinoline; Antimalarial; Chloroquine; Cytotoxicity; Tetrazole.Safety of 7-Chloro-4-(piperazin-1-yl)quinoline.

A series of novel tetrazole derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities against both chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum as well as for cytotoxicity against VERO cell lines. Most of the synthesized compounds exhibited potent antimalarial activity as compared to chloroquine against K1-strain. Compounds with significant in vitro antimalarial activity were then evaluated for their in vivo efficacy in Swiss mice against Plasmodium yoelii following both i.p. (i.p.) and oral administration, wherein compounds I (R = Cl or Br) each showed in vivo suppression of 99.99% parasitemia on day 4.

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Urbina-Blanco, Cesar A.; Bantreil, Xavier; Clavier, Herve; Slawin, Alexandra M. Z.; Nolan, Steven P. published the article 《Backbone tuning in indenylidene-ruthenium complexes bearing an unsaturated N-heterocyclic carbene》. Keywords: imidazolylidene ruthenium indenylidene complex preparation catalyst olefin RCM; crystal mol structure mesityl imidazolylidene ruthenium complex; N-heterocyclic carbene; Tolman electronic parameter; olefin metathesis; percent buried volume; ruthenium–indenylidene.They researched the compound: 1,3-Dimesityl-1H-imidazol-3-ium tetrafluoroborate( cas:286014-53-7 ).Name: 1,3-Dimesityl-1H-imidazol-3-ium tetrafluoroborate. 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:286014-53-7) here.

The steric and electronic influence of backbone substitution in IMes-based (IMes = 1,3-bis(2,4,6-trimethylphenyl)imidazol-2-ylidene) N-heterocyclic carbenes (NHC) was probed by synthesizing the [RhCl(CO)2(NHC)] series of complexes to quantify exptl. the Tolman electronic parameter (electronic) and the percent buried volume (%Vbur, steric) parameters. The corresponding ruthenium-indenylidene complexes were also synthesized and tested in benchmark metathesis transformations to establish possible correlations between reactivity and NHC electronic and steric parameters.

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Bromide – Wikipedia,
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Application In Synthesis of 8-Bromooctanoic acid. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Streamlined One-Pot Synthesis of Nitro Fatty Acids. Author is Hassan, Mohamed; Krieg, Sara-Cathrin; Ndefo Nde, Cedric; Roos, Jessica; Maier, Thorsten J.; El Rady, Eman A.; Raslan, Mohamed A.; Sadek, Kamal U.; Manolikakes, Georg.

A novel method for the synthesis of nitro fatty acids (NFAs), an intriguing class of endogenously occurring lipid mediators, is reported. This one-pot procedure enables the controlled and stereoselective construction of nitro fatty acids from a simple set of common building blocks in a highly facile manner. Thereby, this methodol. offers a streamlined, highly modular access to naturally occurring nitro fatty acids as well as non-natural NFA derivatives

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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 Synthesis, cytotoxicity and antimalarial activity of ferrocenyl amides of 4-aminoquinolines, published in 2010, which mentions a compound: 837-52-5, mainly applied to ferrocenyl aminoquinoline amide preparation cytotoxicity antimalarial activity, Safety of 7-Chloro-4-(piperazin-1-yl)quinoline.

Series of 4-aminoquinolines bearing an amino side chain linked to the ferrocene moiety through an amide bond were synthesized and evaluated for their antimalarial activity against both chloroquine-sensitive (D10, CQ-S) and chloroquine-resistant (Dd2, CQ-R) strains of Plasmodium falciparum. They were also tested for cytotoxicity against Chinese Hamster Ovarian (CHO) cells. Amide featuring Pr side chain linked to the ferrocene ring was the most active of all tested compounds With an IC50 value of 0.08 μg/mL, this amide showed 1.5-fold higher activity than chloroquine diphosphate (IC50 = 0.12 μg/mL) against the resistant strain, with a selectivity index of 550 indicating its high selectivity towards the parasite. Derivatives which were equipotent against both strains also showed up to ten-fold increase in activity compared to primaquine.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Ethyl 3-Ethoxy-2-Propenoate(SMILESS: O=C(OCC)/C=C/OCC,cas:1001-26-9) is researched.Name: 8-Bromooctanoic acid. The article 《Practical preparation of esters and thioacetates from alkyl halides and carboxylates or thioacetate catalyzed by PEG400 without solvent》 in relation to this compound, is published in Synthetic Communications. Let’s take a look at the latest research on this compound (cas:1001-26-9).

Carboxylic esters and thioacetates were conveniently prepared in good to excellent yields under mild conditions by the reaction of alkyl halides with sodium carboxylates or sodium thioacetate catalyzed by PEG400 in the absence of solvents.

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Name: 8-Bromooctanoic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Alkyl Carbagermatrane Enabled Synthesis of Seven-Membered Carbocycle-Fused Aromatics through Catellani Strategy. Author is Xie, Xiu-Ying; Jiang, Wei-Tao; Xiao, Bin.

Synthesis of seven-membered carbocycle-fused aromatics was realized by Catellani reaction using terminally brominated alkyl carbagermatranes through intermol. cyclization manner. Various functional groups were well tolerated and this transformation was also expanded to the synthesis of carbocycles of other size. The utility of the above method was demonstrated by modification of natural product derivatives and synthesis of bioactive mols.

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Quality Control of 1,3-Dimesityl-1H-imidazol-3-ium tetrafluoroborate. 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: 1,3-Dimesityl-1H-imidazol-3-ium tetrafluoroborate, is researched, Molecular C21H25BF4N2, CAS is 286014-53-7, about Probing the Diastereoselectivity of Staudinger Reactions Catalyzed by N-Heterocyclic Carbenes.

The reaction of ethylphenylketene with 1,3-dimesitylimidazol-2-ylidene (IMes) or 1,3-dimesitylimidazolin-2-ylidene (SIMes) afforded the corresponding azolium enolates in high yields. The two zwitterions were fully characterized by various anal. techniques. Their thermal stabilities were monitored by thermogravimetric anal. and the mol. structure of SIMes·EtPhC=C=O was determined by means of X-ray crystallog. A mechanism was proposed to account for the trans-diastereoselectivity observed in the [2+2] cycloaddition of ketenes and N-protected imines catalyzed by N-heterocyclic carbenes and an extensive catalytic screening was performed to test its validity. The steric bulk of the NHC catalyst markedly affected the cis/trans ratio of the model β-lactam product. The nature of the solvent used to carry out the Staudinger reaction also significantly influenced its diastereoselectivity. Conversely, the nature of the substituent on the N-sulfonated imine reagent and the reaction temperature were less critical parameters.

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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: 1,3-Dimesityl-1H-imidazol-3-ium tetrafluoroborate( cas:286014-53-7 ) is researched.Related Products of 286014-53-7.Zhang, Liang; Wu, Jie published the article 《Rhodium/N-heterocyclic carbene-catalyzed cross-couplings of aryl arenesulfonates with arylboronic acids》 about this compound( cas:286014-53-7 ) in Advanced Synthesis & Catalysis. Keywords: coupling reaction rhodium imidazole carbene catalyst phenylboronic acid benzenesulfonate. Let’s learn more about this compound (cas:286014-53-7).

A method for the synthesis of biaryl compounds is reported here. A combination of rhodium(I) and N-heterocyclic carbenes (NHC) was found to be effective as a catalyst for cross-coupling reactions of aryl arenesulfonates with arylboronic acids, which gave rise to the desired biaryl compounds in good yields.

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Bromide – Wikipedia,
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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.Schaeker-Huebner, Linda; Warstat, Robin; Ahlert, Heinz; Mishra, Pankaj; Kraft, Fabian B.; Schliehe-Diecks, Julian; Schoeler, Andrea; Borkhardt, Arndt; Breit, Bernhard; Bhatia, Sanil; Huegle, Martin; Guenther, Stefan; Hansen, Finn K. researched the compound: 8-Bromooctanoic acid( cas:17696-11-6 ).COA of Formula: C8H15BrO2.They published the article 《4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads》 about this compound( cas:17696-11-6 ) in Journal of Medicinal Chemistry. Keywords: antileukemia drug HDAC BET dual inhibitors BRD4 apoptosis anticancer. We’ll tell you more about this compound (cas:17696-11-6).

Multitarget drugs are an emerging alternative to combination therapies. In three iterative cycles of design, synthesis, and biol. evaluation, we developed a novel type of potent hybrid inhibitors of bromodomain, and extra-terminal (BET) proteins and histone deacetylases (HDACs) based on the BET inhibitor XD14 and well-established HDAC inhibitors. The most promising new hybrids, 49 and 61, displayed submicromolar inhibitory activity against HDAC1-3 and 6, and BRD4(1), and possess potent antileukemia activity. 49 induced apoptosis more effectively than the combination of ricolinostat and birabresib (1:1). The most balanced dual inhibitor, 61, induced significantly more apoptosis than the related control compounds 62 (no BRD4(1) affinity) and 63 (no HDAC inhibition) as well as the 1:1 combination of both. Addnl., 61 (I) was well tolerated in an in vivo zebrafish toxicity model. Overall, our data suggest an advantage of dual HDAC/BET inhibitors over the combination of two single targeted compounds

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Bromide – Wikipedia,
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