Tag: M.W=150-200

Meng, Genyi; Guo, Taijie; Ma, Tiancheng; Zhang, Jiong; Shen, Yucheng; Sharpless, Karl Barry; Dong, Jiajia published the artcile< Modular click chemistry libraries for functional screens using a diazotizing reagent>, Application In Synthesis of 387350-39-2, the main research area is alkyl aryl azide triazole chemoselective preparation; fluorosulfonyl azide generation chemoselective diazotization primary amine; combinatorial generation library alkyl aryl azide cycloaddition alkyne; functional screen click chem azide generated in situ.

Alkyl and aryl azides were prepared from the corresponding primary alkyl and aryl amines by reaction with fluorosulfonyl azide generated in situ from a fluorosulfonylimidazolium triflate and sodium azide, expanding access to azides and both to the 1,2,3-triazoles derived from them and to functional screens employing them. The method allowed the preparation of a library of >1000 azides from the corresponding amines; the azide library underwent copper-catalyzed azide-alkyne cycloaddition reactions to yield a library of >1000 1,2,3-triazoles.

Nature (London, United Kingdom) published new progress about Alkyl azides Role: CMB (Combinatorial Study), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 387350-39-2 belongs to class pyridine-derivatives, and the molecular formula is C7H7F3N2, Application In Synthesis of 387350-39-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Heinz-Kunert, Sherrie L.; Pandya, Ashma; Dang, Viet Thuc; Tran, Phuong Nguyen; Ghosh, Sabari; McElheny, Dan; Santarsiero, Bernard D.; Ren, Zhong; Nguyen, Andy I. published the artcile< Assembly of π-Stacking Helical Peptides into a Porous and Multivariable Proteomimetic Framework>, HPLC of Formula: 366-18-7, the main research area is .

The evolution of proteins from simpler, self-assembled peptides provides a powerful blueprint for the design of complex synthetic materials. Previously, peptide-metal frameworks using short sequences (≤3 residues) have shown great promise as proteomimetic materials that exhibit sophisticated capabilities. However, their development has been hindered due to few variable residues and restricted choice of side-chains that are compatible with metal ions. Herein, we developed a noncovalent strategy featuring π-stacking bipyridyl residues to assemble much longer peptides into crystalline frameworks that tolerate even previously incompatible acidic and basic functionalities and allow an unprecedented level of pore variations. Single-crystal X-ray structures are provided for all variants to guide and validate rational design. These materials exhibit hallmark proteomimetic behaviors such as guest-selective induced fit and assembly of multimetallic units. Significantly, we demonstrate facile optimization of the framework design to substantially increase affinity toward a complex organic mol.

Journal of the American Chemical Society published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, HPLC of Formula: 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Moreau, Robert J.; Skepper, Colin K.; Appleton, Brent A.; Blechschmidt, Anke; Balibar, Carl J.; Benton, Bret M.; Drumm, Joseph E.; Feng, Brian Y.; Geng, Mei; Li, Cindy; Lindvall, Mika K.; Lingel, Andreas; Lu, Yipin; Mamo, Mulugeta; Mergo, Wosenu; Polyakov, Valery; Smith, Thomas M.; Takeoka, Kenneth; Uehara, Kyoko; Wang, Lisha; Wei, Jun-Rong; Weiss, Andrew H.; Xie, Lili; Xu, Wenjian; Zhang, Qiong; de Vicente, Javier published the artcile< Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria>, Computed Properties of 19346-45-3, the main research area is triazolopyrimidinone preparation phosphopantetheine adenylyltransferase inhibitory activity; azabenzimidazole preparation phosphopantetheine adenylyltransferase inhibitory activity.

The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-neg. bacteria is a major challenge with fundamental importance to our global healthcare system. Part of our broad program at Novartis to address this urgent, unmet need includes the search for new agents that inhibit novel bacterial targets. Here we report the discovery and hit-to-lead optimization of new inhibitors of phosphopantetheine adenylyltransferase (PPAT) from Gram-neg. bacteria. Utilizing a fragment-based screening approach, we discovered a number of unique scaffolds capable of interacting with the pantetheine site of E. coli PPAT and inhibiting enzymic activity, including triazolopyrimidinone. Structure-based optimization resulted in the identification of two lead compounds as selective, small mol. inhibitors of bacterial PPAT: triazolopyrimidinone I and azabenzimidazole II efficiently inhibited E. coli and P. aeruginosa PPAT and displayed modest cellular potency against the efflux-deficient E. coli ΔtolC mutant strain.

Journal of Medicinal Chemistry published new progress about Antibiotics. 19346-45-3 belongs to class pyridine-derivatives, and the molecular formula is C6H5FN2O2, Computed Properties of 19346-45-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Malhotra, Rajesh; Rarhi, Chhanda; Diveshkumar, K. V.; Bommisetti, P.; Pany, Sushree Prangya P.; Roy, Subho; Pradeepkumar, P. I.; Kundu, Mrinalkanti published the artcile< Pyridopyrimidinone Derivatives as ΙDNAG-Quadruplex-Stabilizing Agents: Design, Synthesis and Biophysical Studies>, HPLC of Formula: 188577-68-6, the main research area is pyridopyrimidinone preparation quadruplex DNA stabilizer.

With an aim to engineer drug-like properties, pyridopyrimidinone based selective G4 DNA stabilizing agents, e.g., I were designed, synthesized and further they were evaluated for G4 DNA recognition properties. CD melting studies revealed the preferential stabilization of parallel topol. of promoter c-MYC and c-KIT G4 DNAs by the ligands, especially compound I and 4-[7-chloro-3-methyl-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl]-N-(2-dimethylamino-ethyl)-benzamide, over the different topologies of telomeric G4 DNA. UV melting experiments suggested that no significant stabilization was observed for duplex DNA. Further, the results from ITC experiments substantiated the preferential stabilization of parallel topol. of c-MYC G4 DNA over telomeric and duplex DNA by the ligands I. These data showed that ligand I has moderate binding affinity to the c-MYC G4 DNA and is ~49-fold and ~25-fold selective over the telomeric G4 DNA and the duplex DNA resp. The mol. modeling and dynamics studies of the ligand I in complex with c-MYC and c-KIT1 G4 DNAs showed that this ligand stacks on the 5′-quartet of c-MYC and 3′-quartet of c-KIT1 G4 DNA structures.

ChemistrySelect published new progress about Circular dichroism. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, HPLC of Formula: 188577-68-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gurgul, Ilona; Mazuryk, Olga; Stachyra, Kamila; Olszanecki, Rafal; Lekka, Malgorzata; Lomzik, Michal; Suzenet, Franck; Gros, Philippe C.; Brindell, Malgorzata published the artcile< Impact of Polypyridyl Ru Complexes on Angiogenesis-Contribution to Their Antimetastatic Activity>, HPLC of Formula: 366-18-7, the main research area is angiogenesis; cell adhesion properties; cell elasticity; cytotoxicity; endothelial cells; focal adhesions; migration; polypyridyl ruthenium (II) complexes; pseudovessel formation.

The use of polypyridyl Ru complexes to inhibit metastasis is a novel approach, and recent studies have shown promising results. We have reported recently that Ru (II) complexes gathering two 4,7-diphenyl-1,10-phenanthroline (dip) ligands and the one being 2,2′-bipyridine (bpy) or its derivative with a 4-[3-(2-nitro-1H-imidazol-1-yl)propyl (bpy-NitroIm) or 5-(4-{4′-methyl-[2,2′-bipyridine]-4-yl}but-1-yn-1-yl)pyridine-2-carbaldehyde semicarbazone (bpy-SC) moieties can alter the metastatic cascade, among others, by modulating cell adhesion properties. In this work, we show further studies of this group of complexes by evaluating their effect on HMEC-1 endothelial cells. While all the tested complexes significantly inhibited the endothelial cell migration, Ru-bpy addnl. interrupted the pseudovessels formation. Functional changes in endothelial cells might arise from the impact of the studied compounds on cell elasticity and expression of proteins (vinculin and paxillin) involved in focal adhesions. Furthermore, mol. studies showed that complexes modulate the expression of cell adhesion mols., which has been suggested to be one of the factors that mediate the activation of angiogenesis. Based on the performed studies, we can conclude that the investigated polypyridyl Ru (II) complexes can deregulate the functionality of endothelial cells which may lead to the inhibition of angiogenesis.

International Journal of Molecular Sciences published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, HPLC of Formula: 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pyrch, Mikaela M.; Williams, Jay M.; Kasperski, Maguire W.; Applegate, Lindsey C.; Forbes, Tori Z. published the artcile< Synthesis and spectroscopic characterization of actinyl(VI) tetrahalide coordination compounds containing 2, 2'-bipyridine>, Computed Properties of 366-18-7, the main research area is uranium neptunium oxo chloro bromo complex preparation crystal structure.

Three new actinide tetrahalide coordination compounds containing 2,2′-bipyridinium (H2bpy) were synthesized by room temperature evaporation and characterized via single crystal x-ray diffraction, Raman spectroscopy, and IR spectroscopy. The solid-state compounds (Np1, U1, and U2) contain the AnO2+2 cation coordinated to four halide (chloride or bromide) atoms to form the anionic tetrahalide mol. unit [AnO2X4]2- (X = Cl, Br) and are charge balanced by the 2,2′-bipyridinium cations that engage in electrostatic interactions with the actinyl complex. Np1 (N2C10H10)[NpO2Cl4] contains 2,2′-bipyridine in the cis conformation where both the nitrogen atoms are directed towards the [NpO2Cl4]2- monomer. Within U1 (N2C10H9)[UO2Cl4], the 2,2′-bipyridine is in a trans conformation, and found in the same orientation in the isomorphous structure U2 (N2C10H9)[UO2Br4]. The compounds were further characterized by vibrational spectroscopy with specific interest in the actinyl cation. Raman spectroscopy provided information on the actinyl sym. stretch (ν1) whereas IR spectroscopy was used to determine the location of the asym. stretch (ν3). Spectral similarities are observed between the two isomorphous structures, but slight variations across structures are associated with bipyridine bands in the various conformations. Addnl. anal. of these vibrational features in U1 and U2 provided information on the actinyl force constants, allowing insight into the relative uranyl bond strength that was compared to similar tetrahalide compounds

Inorganica Chimica Acta published new progress about Actinide complexes Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Computed Properties of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hooda, Anjli; Nehra, Kapeesha; Dalal, Anuj; Bhagwan, Shri; Gupta, Isha; Singh, Devender; Kumar, Sumit published the artcile< Luminescent Features of Ternary Europium Complexes: Photophysical and Optoelectronic Evaluation>, Name: 2,2′-Bipyridine, the main research area is ternary europium complex luminescence photophys optoelectronics; Cyclovoltammograms; Europium complexes; Fluorinated β-diketone; Thermal analysis.

Trivalent europium complexes exhibit good luminescent characteristics. A series of octacoordinated ternary europium complexes with fluorinated diketone and heteroaromatic auxiliary unit were synthesized. The synthesized europium complexes were characterized by elemental, thermal, electrochem. and spectroscopic analyses. Band gap values lie in range of semiconductors which confirm the conducting behavior of prepared complexes. Photoluminescence spectra were recorded in solid state and DMSO solvent. Emission spectral profiles have displayed most intense peak at ∼ 612 nm corresponding to hypersensitive 5D0 → 7F2 transition. Colorimetric parameters suggest red luminous nature of europium complexes. The luminescent heteroleptic europium complexes might be utilized as emissive materials for fabricating display.

Journal of Fluorescence published new progress about Absorption spectra. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Name: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Shichen; Feng, Lei; Ma, Chen published the artcile< Simple and green synthesis of benzimidazoles and pyrrolo[1,2-a]quinoxalines via Mamedov heterocycle rearrangement>, HPLC of Formula: 21901-29-1, the main research area is benzimidazole pyrroloquinoxaline preparation green chem Mamedov heterocycle rearrangement.

A method for the synthesis of coupling compounds of benzimidazoles and pyrrolo[1,2-a]quinoxalines via Mamedov Heterocycle Rearrangement is reported here. This method was conducted at room temperature and only solvent (HOAc) was required. A series of 4-(1H-benzo[d]imidazol-2-yl)pyrrolo[1,2-a]quinoxaline derivatives were obtained in moderate to good yields.

New Journal of Chemistry published new progress about Benzimidazoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, HPLC of Formula: 21901-29-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chand, Pooran; Kotian, Pravin L.; Morris, Philip E.; Bantia, Shanta; Walsh, David A.; Babu, Yarlagadda S. published the artcile< Synthesis and inhibitory activity of benzoic acid and pyridine derivatives on influenza neuraminidase>, Synthetic Route of 21901-29-1, the main research area is benzoate pyridine derivative preparation influenza neuraminidase inhibitor SAR.

Based upon the activity and X-ray crystallog. studies of tri-substituted benzene derivatives containing carboxylic acid, acetamido and guanidine groups, we investigated the effect of the fourth substituent to fulfill the fourth pocket of neuraminidase enzyme. The groups selected as fourth substituents were hydroxymethyl, hydroxyethyl, oxime and amino. These tetra-substituted benzene derivatives were synthesized and evaluated for neuraminidase inhibitory activity. All these compounds were found to have poorer IC50 values than the tri-substituted compounds Further, benzene ring was replaced by pyridine ring and di, tri and tetra-substituted pyridine derivatives were synthesized. The activity of the pyridine derivatives was comparable to benzene derivatives The fourth substituent seems to disturb the binding of the other three substituents, so the activity is reduced as compared to tri-substituted benzene and pyridine derivatives

Bioorganic & Medicinal Chemistry published new progress about Influenza virus. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Synthetic Route of 21901-29-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kondori, Tahere; Akbarzadeh-T, Niloufar; Ghaznavi, Habib; Karimi, Zeinab; Shahraki, Jafar; Sheervalilou, Roghayeh; Shahraki, Omolbanin published the artcile< A binuclear iron(III) complex of 5,5′-dimethyl-2,2′-bipyridine as cytotoxic agent>, Recommanded Product: 2,2′-Bipyridine, the main research area is binuclear iron complex dimethyl bipyridine cytotoxic agent; 5,5′-dimethyl-2,2′-bipyridine; Binuclear iron(III) complex; Cytotoxicity; Fish salmon DNA.

The binuclear iron(III) complex (1), namely, {[Fe(5,5′-dmbpy)2(OH2)]2(O)}(NO3)4 with a distorted octahedral coordination, formed by four nitrogen and two oxygen atoms, was previously reported by our team. In this study the DNA-binding and cytotoxicity evaluation for target complex were studied. The results indicated strong cytotoxicity activity against A549 cells comparable to cisplatin values. The binding interaction between complex 1 and FS-DNA was investigated by UV-Vis, fluorescence spectroscopy, and gel electrophoresis at physiol. pH (7.2). The DNA binding investigation has shown groove binding interactions with complex 1, therefore the hydrogen binding plays an important role in the interaction of DNA with complex 1. The calculated thermodn. parameters (ΔH°, ΔS° and ΔG°) show that hydrogen bonding and Vander-Waals forces have an important function in Fe(III) complex-DNA interaction. Moreover, DNA cleavage was studied using agarose gel electrophoresis. Viscosity measurements illustrated that relative viscosity of DNA was unchanged with the adding concentrations of Fe(III) complex. Mol. docking simulation results confirmed the spectroscopic and viscosity titration outcomes.

BioMetals published new progress about Bicyclic aromatic hydrocarbons Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Recommanded Product: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem