Tag: M.W=200-300

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 Studies on aminoquinolines. Chemical, antiparasitic, antimicrobial and antifungal studies of 4-(4-mono-, di- and trichloroacetyl-1-piperazinyl)quinolines, the main research direction is chloroacetylpiperazinylquinoline preparation pharmacol; piperazinylquinoline preparation pharmacol; quinoline piperazinyl preparation pharmacol; parasiticide chloroacetylpiperazinylquinoline; fungicide chdloroacetylpiperazinylquinoline; bactericide chloroacetylpiperazinylquinoline; amebicide chloroacetylpiperazinylquinoline.COA of Formula: C13H14ClN3.

Piperazinylquinolines (I, R = H, Me; R1 = H, Cl, CF3, NO2; R2 = Cl, CF3, OMe; R3 = H, CH2ClCHCl2, CCl3 and II, R = H, Me; R1 = H, NO2; R2 = H, Cl, CF3, OMe) were prepared and their pharmacol. was studied. I were prepared either by the reaction of 1-nitrosopiperazines with chloroquinolines, hydrogenolysis of the chloro(nitrosopiperazinyl)quinolines, and chloroacetylation of the resultant II or by reaction of piperazine  [104667-94-9] with chloroquinolines followed by chloroacetylation. The parasiticidal, antibacterial and antifungal activities of I and II were studied in vitro. The amebicidal activity of the compounds was studied both in vitro and in vivo. The chloroacetyl derivatives showed weak bactericidal activity. The structure-activity relations of the compounds are discussed.

Compounds in my other articles are similar to this one(7-Chloro-4-(piperazin-1-yl)quinoline)COA of Formula: C13H14ClN3, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.

Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Name: 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 Mixed Fluorinated/Hydrogenated Self-Assembled Monolayer-Protected Gold Nanoparticles: In Silico and In Vitro Behavior. Author is Marson, Domenico; Guida, Filomena; Sologan, Maria; Boccardo, Silvia; Pengo, Paolo; Perissinotto, Fabio; Iacuzzi, Valentina; Pellizzoni, Elena; Polizzi, Stefano; Casalis, Loredana; Pasquato, Lucia; Pacor, Sabrina; Tossi, Alessandro; Posocco, Paola.

Gold nanoparticles (AuNPs) covered with mixtures of immiscible ligands present potentially anisotropic surfaces that can modulate their interactions at complex nano-bio interfaces. Mixed, self-assembled, monolayer (SAM)-protected AuNPs, prepared with incompatible hydrocarbon and fluorocarbon amphiphilic ligands, are used here to probe the mol. basis of surface phase separation and disclose the role of fluorinated ligands on the interaction with lipid model membranes and cells, by integrating in silico and exptl. approaches. These results indicate that the presence of fluorinated amphiphilic ligands enhances the membrane binding ability and cellular uptake of gold nanoparticles with respect to those coated only with hydrogenated amphiphilic ligands. For mixed monolayers, computational results suggest that ligand phase separation occurs on the gold surface, and the resulting anisotropy affects the number of contacts and adhesion energies with a membrane bilayer. This reflects in a diverse membrane interaction for NPs with different surface morphologies, as determined by surface plasmon resonance, as well as differential effects on cells, as observed by flow cytometry and confocal microscopy. Overall, limited changes in monolayer features can significantly affect NP surface interfacial properties, which, in turn, affect the interaction of SAM-AuNPs with cellular membranes and subsequent effects on cells.

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Bromide – Wikipedia,
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Application In Synthesis of 8-Bromooctanoic acid. 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: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about A Bioorthogonal Click Chemistry Toolbox for Targeted Synthesis of Branched and Well-Defined Protein-Protein Conjugates. Author is Baalmann, Mathis; Neises, Laura; Bitsch, Sebastian; Schneider, Hendrik; Deweid, Lukas; Werther, Philipp; Ilkenhans, Nadja; Wolfring, Martin; Ziegler, Michael J.; Wilhelm, Jonas; Kolmar, Harald; Wombacher, Richard.

Bioorthogonal chem. holds great potential to generate difficult-to-access protein-protein conjugate architectures. Current applications are hampered by challenging protein expression systems, slow conjugation chem., use of undesirable catalysts, or often do not result in quant. product formation. Here the authors present a highly efficient technol. for protein functionalization with commonly used bioorthogonal motifs for Diels-Alder cycloaddition with inverse electron demand (DAinv). With the aim of precisely generating branched protein chimeras, the authors systematically assessed the reactivity, stability and side product formation of various bioorthogonal chemistries directly at the protein level. The authors demonstrate the efficiency and versatility of the authors′ conjugation platform using different functional proteins and the therapeutic antibody trastuzumab. This technol. enables fast and routine access to tailored and hitherto inaccessible protein chimeras useful for a variety of scientific disciplines. The authors expect the authors′ work to substantially enhance antibody applications such as immunodetection and protein toxin-based targeted cancer therapies.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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.Hinklin, Ronald J.; Baer, Brian R.; Boyd, Steven A.; Chicarelli, Mark D.; Condroski, Kevin R.; DeWolf, Walter E. Jr.; Fischer, John; Frank, Michele; Hingorani, Gary P.; Lee, Patrice A.; Neitzel, Nickolas A.; Pratt, Scott A.; Singh, Ajay; Sullivan, Francis X.; Turner, Timothy; Voegtli, Walter C.; Wallace, Eli M.; Williams, Lance; Aicher, Thomas D. researched the compound: 4,4-Dipyridyl Disulfide( cas:2645-22-9 ).Application of 2645-22-9.They published the article 《Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator》 about this compound( cas:2645-22-9 ) in Bioorganic & Medicinal Chemistry. Keywords: hiadiazole heteroaryloxypyridine AR453588 synthesis antidiabetic SAR glucokinase activator diabetes; Diabetes; Glucokinase; Glucokinase activator; OGTT; S(0.5); Structure-aided design; Structure-based design; Type II diabetes; V(max); ob/ob mouse. We’ll tell you more about this compound (cas:2645-22-9).

Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an inadequacy or defect in one or both of these processes, identifying compounds that can activate GK could provide a therapeutic benefit. Herein we report the further structure activity studies of a novel series of glucokinase activators (GKA). These studies led to the identification of pyridine 72 as a potent GKA that lowered post-prandial glucose in normal C57BL/6J mice, and after 14d dosing in ob/ob mice. 3-(heteroaryloxy)pyridine.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Safety of 8-Bromooctanoic acid. 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: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Symmetrical-Tetramethyl-Cucurbit[6]uril-Driven Movement of Cucurbit[7]uril Gives Rise to Heterowheel [4]Pseudorotaxanes. Author is Lin, Rui-Lian; Li, Ran; Shi, Hao; Zhang, Kun; Meng, Di; Sun, Wen-Qi; Chen, Kai; Liu, Jing-Xin.

Two novel heterowheel [4]pseudorotaxanes consisting of cucurbit[7]uril (Q[7]) and sym.-tetramethyl-cucurbit[6]uril (TMeQ[6]) were constructed via the multirecognition mechanism, in which Q[7] can rotate freely around the horizontal axis, while TMeQ[6] cannot. In the construction process, due to strong repulsive forces between carbonyl portals of two neighboring wheels, the dethreading and movement of the wheels along the axle was observed The dissociation of the [4]pseudorotaxanes was also discussed.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Jeankumar, Variam Ullas; Reshma, Rudraraju Srilakshmi; Vats, Rahul; Janupally, Renuka; Saxena, Shalini; Yogeeswari, Perumal; Sriram, Dharmarajan published the article 《Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors》. Keywords: gyrase ATPase inhibitor tuberculosis screening structure; DNA gyrase; Differential scanning fluorimetry; Medium throughput virtual screening; Mycobacterium tuberculosis.They researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).Safety of 7-Chloro-4-(piperazin-1-yl)quinoline. 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.

A structure based medium throughput virtual screening campaign of BITS-Pilani in house chem. library to identify novel binders of Mycobacterium tuberculosis gyrase ATPase domain led to the discovery of a quinoline scaffold. Further medicinal chem. explorations on the right hand core of the early hit, engendered a potent lead demonstrating superior efficacy both in the enzyme and whole cell screening assay. The binding affinity shown at the enzyme level was further corroborated by biophys. characterization techniques. Early pharmacokinetic evaluation of the optimized analog was encouraging and provides interesting potential for further optimization.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Name: 6-Bromo-3-methyl-1H-indole. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 6-Bromo-3-methyl-1H-indole, is researched, Molecular C9H8BrN, CAS is 1219741-50-0, about A three-component iodine-catalyzed oxidative coupling reaction: a heterodifunctionalization of 3-methylindoles. Author is Zhang, Wei; Xiang, Shiqun; Fan, Weibin; Jin, Jiang; Li, Yinghua; Huang, Deguang.

A metal-free method for the synthesis of heterodifunctional indole derivatives was developed through TBHP/KI-mediated oxidative coupling. The reaction constructed C-O and C-C bonds in succession with the help of tert-Bu peroxy radicals generated by the TBHP/KI catalytic system, enabling the direct realization of the heterodifunctionalization of indole in one pot. The product of this reaction was a novel heterodifunctional compound This work might provided a new effective method for the synthesis of polycyclic indole compounds

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Electric Literature of C9H8BrN. 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: 6-Bromo-3-methyl-1H-indole, is researched, Molecular C9H8BrN, CAS is 1219741-50-0, about Chalcogen-Chalcogen Bonding Catalysis Enables Assembly of Discrete Molecules. Author is Wang, Wei; Zhu, Haofu; Liu, Shuya; Zhao, Zhiguo; Zhang, Liang; Hao, Jingcheng; Wang, Yao.

Despite the observation of noncovalent interactions between chalcogen atoms in X-ray crystal structures, catalysis that harnesses the power of such chalcogen-chalcogen bonding interactions to produce advanced mols. remains an unresolved problem. Here, we show that a class of extraordinary chalcogen-bonding catalysts enables assembly of discrete small mols. including three β-ketoaldehydes and one indole, leading to the construction of N-heterocycles in a highly efficient manner. The strong activation ability of these rationally designed catalysts provides a general solution to the intrinsic limitations of chalcogen bonding catalysis.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

Safety of 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 Synthesis of Novel G Factor or Chloroquine-Artemisinin Hybrids and Conjugates with Potent Antiplasmodial Activity. Author is Pepe, Dionissia A.; Toumpa, Dimitra; Andre-Barres, Christiane; Menendez, Christophe; Mouray, Elisabeth; Baltas, Michel; Grellier, Philippe; Papaioannou, Dionissios; Athanassopoulos, Constantinos M..

A series of novel hybrids of artemisinin (ART) with either a phytormone endoperoxide G factor analog (GMeP) or chloroquine (CQ) and conjugates of the same compounds with the polyamines (PAs), spermidine (Spd), and homospermidine (Hsd) were synthesized and their antiplasmodial activity was evaluated using the CQ-resistant P. falciparum FcB1/Colombia strain. The ART-GMeP hybrid I and compounds II [n = 1, 2] which are conjugates of Spd and Hsd with two mols. of ART and one mol. of GMeP, were the most potent with IC50 values of 2.6, 8.4, and 10.6 nM, resp. The same compounds also presented the highest selectivity indexes against the primary human fibroblast cell line AB943 ranging from 16,372 for the hybrid I to 983 for the conjugate II [n = 2] of Hsd.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary

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, Angewandte Chemie, International Edition called Nickel-Catalyzed Inter- and Intramolecular Aryl Thioether Metathesis by Reversible Arylation, Author is Delcaillau, Tristan; Bismuto, Alessandro; Lian, Zhong; Morandi, Bill, which mentions a compound: 17696-11-6, SMILESS is O=C(O)CCCCCCCBr, Molecular C8H15BrO2, Recommanded Product: 17696-11-6.

A nickel-catalyzed aryl thioether metathesis was developed to access high-value thioethers. 1,2-Bis(dicyclohexylphosphino)ethane (dcype) is essential to promote this highly functional-group-tolerant reaction. Furthermore, synthetically challenging macrocycles could be obtained in good yield in an unusual example of ring-closing metathesis that does not involve alkene bonds. In-depth organometallic studies support a reversible Ni0/NiII pathway to product formation. Overall, this work not only provides a more sustainable alternative to previous catalytic systems based on Pd, but also presents new applications and mechanistic information that are highly relevant to the further development and application of unusual single-bond metathesis reactions.

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Reference:
Bromide – Wikipedia,
bromide – Wiktionary