Month: November 2022

Ren, Rui published the artcileUltrafast 2,7-Naphthyridine-Based fluorescent probe for detection of thiophenol with a remarkable Stokes shift and its application In vitro and in vivo, Category: naphthyridine, the main research area is thiophenol naphthyridine fluorescent probe; 2,7-Naphthyridine; Bioimaging; Fluorescent probe; Theoretical calculation; Zebrafish.

2,7-Naphthyridine derivatives were developed as fluorophores for the first time to design two fluorescence probes, AND-DNP and ND-DNP, which can be applied for detecting thiophenol in aqueous media. Comparing with ND-DNP, AND-DNP showed more favorable properties such as lower background, larger Stokes shift, and higher fluorescence quantum yield for detecting thiophenol. Moreover, the exptl. results were verified by theor. calculations Hence, AND-DNP was selected as the superior fluorescence probe to detect thiophenol because of its high sensitivity and selectivity. Based on the exptl. results, AND-DNP showed a remarkably larger Stokes shift (225 nm), faster response speed (30 s) and higher fluorescence enhancement (240-fold) than most other fluorescent probes for thiophenol reported in the literature. For an extended application, AND-DNP was applied to detect thiophenol quant. in real water samples. Meanwhile, AND-DNP also detected thiophenol via red emission in living A549 cells and zebrafish. All these results proved AND-DNP’s potential value as an accurate probe for imaging thiophenol in different environments.

Talanta published new progress about Fluorescence microscopy. 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Category: naphthyridine.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Greiner, Robert published the artcilePreparation of Polyfunctional Naphthyridines by Cobalt-Catalyzed Cross-Couplings of Halogenated Naphthyridines with Magnesium and Zinc Organometallics, Safety of 2,7-Naphthyridin-1(2H)-one, the main research area is polyfunctional naphthyridine preparation fluorescent; halogenated naphthyridine alkyl magnesium halidearylmagnesium halide cross coupling; zinc organometallic.

CoCl2 (5%) catalyzes cross-couplings of various halogenated naphthyridines with alkyl- and arylmagnesium halides. Also, arylzinc halides undergo smooth cross-couplings with various naphthyridines in the presence of CoCl2·2LiCl (5%) and sodium formate (50%), leading to polyfunctional arylated naphthyridines. Two of these arylated naphthyridines, e. g., I, are highly fluorescent, with quantum efficiencies reaching 95% and long excited-state lifetimes of up to 12 ns.

Organic Letters published new progress about Cross-coupling reaction. 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Safety of 2,7-Naphthyridin-1(2H)-one.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Sakamoto, Takao published the artcileCondensed heteroaromatic ring systems. III. Synthesis of naphthyridine derivatives by cyclization of ethynylpyridinecarboxamides, Product Details of C8H6N2O, the main research area is cyclization ethynylpyridinecarboxamide; naphthyridinone; coupling palladium halopyridine acetylene.

Naphthyridinones I and II (R = H, R1R2, R2R1 = CONHCH:CH; R=Me, R1R2, R2R1 = CONHCPh:CH) were synthesized by the ring closure of pyridinecarboxamides I and II [R = H, R1(R2) = CONH2, R2(R1) = CH2CH(OMe)2; R = Me, R1(R2) = CONH2, R2(R1) = CCPh]. The starting pyridines I [R = H, R1(R2) = cyano, R2(R1)=CCSiMe3; R =Me, R2(R1) = CCPh] and II [R = H, R1(R2) = cyano, R2(R1) = CCSiMe3; R= Me, R1 = CONH2, R2 = CCPh; R = Me, R1 = CCPh, R2 = CO2Et] were easily synthesized by the Pd-catalyzed cross-coupling of halopyridines with PhCCH or Me3SiCCH.

Chemical & Pharmaceutical Bulletin published new progress about Cross-coupling reaction. 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Product Details of C8H6N2O.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zhang, Ao published the artcileConvenient Synthesis of 2,7-Naphthyridine Lophocladines A and B and their Analogues, Product Details of C8H6N2O, the main research area is lophocladine A B preparation analog; regioselective bromination iodination naphthyridine lophocladine A B preparation; Suzuki lophocladine A B preparation; Stille lophocladine A B preparation; Sonogashira lophocladine A B preparation.

The authors developed a convenient and flexible synthetic route to lophocladines A and B, I and II, resp., as well as their C-4 substituted analogs through a regioselective bromination/iodination of 2,7-naphthyridines followed by a Suzuki, Stille, or Sonogashira reaction. This method is useful for generating a 2,7-naphthyridine library (25 members) with a variant C-4 substituent, including differently substituted aryl, heteroaryl, as well as vinyl, alkyl, and substituted or nonsubstituted acetylenyl groups.

Journal of Combinatorial Chemistry published new progress about Halogenation, regioselective. 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Product Details of C8H6N2O.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Naik, Maruti published the artcile4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity, Recommanded Product: 4-Chloro-1,8-naphthyridin-2(1H)-one, the main research area is aminoquinolone piperidine amide derivative preparation DprE1 inhibitor tuberculostatic.

4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the min. inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-D-ribose 2′-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ∼100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacol. profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 < 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb. Journal of Medicinal Chemistry published new progress about Antimicrobial agent resistance. 59514-93-1 belongs to class naphthyridine, name is 4-Chloro-1,8-naphthyridin-2(1H)-one, and the molecular formula is C8H5ClN2O, Recommanded Product: 4-Chloro-1,8-naphthyridin-2(1H)-one.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Francis, Stuart published the artcileStructure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents, Quality Control of 67988-50-5, the main research area is isoquinolone preparation fascin inhibitor antimetastatic agent; pyrazolopyridine preparation fascin inhibitor antimetastatic agent; Cancer; Drug discovery; Fragments; Medicinal chemistry; Virtual screening.

Fascin is an actin binding and bundling protein that is not expressed in normal epithelial tissues but overexpressed in a variety of invasive epithelial tumors. It has a critical role in cancer cell metastasis by promoting cell migration and invasion. Here are reported the crystal structures of fascin in complex with a series of novel and potent inhibitors. Structure-based elaboration of these compounds enabled the development of a series with nanomolar affinities for fascin, good physicochem. properties and the ability to inhibit fascin-mediated bundling of filamentous actin. Compound I (BDP-13176) was found to be the best fascin binder (SPR Kd = 85±0.02 nM, LE=0.29, ITC Kd = 50 nM) and actin bundling inhibitor (IC50 = 240±0.01 nM). These compounds provide promising starting points for fascin-targeted anti-metastatic therapies.

Bioorganic & Medicinal Chemistry Letters published new progress about Actins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Quality Control of 67988-50-5.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Toure, Momar published the artcileExpeditious Synthesis of Isoquinolones and Isocoumarins with a Vinyl Borane as an Acetylene Equivalent, Formula: C8H6N2O, the main research area is isoquinolone isocoumarin preparation vinyl borane corydaldin doryanine total synthesis; Suzuki coupling; boronate; isocoumarin; isoquinolone; vinyl ether.

An innovative and simple expeditious synthesis of 3,4-unsubstituted isoquinolones and isocoumarins starting from a safe and easy-to-handle two-carbon acetylene equivalent was developed. The synthetic potential of this new method was further demonstrated in the facile total synthesis of two naturally occurring alkaloids, corydaldin and doryanine.

European Journal of Organic Chemistry published new progress about Aromatic carboxylic acids, esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (o-bromo). 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Formula: C8H6N2O.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem