5423-54-1

Usage

Uses

Used in Pharmaceutical Research:
4-Hydroxy-1,5-naphthyridine is used as a reagent for the synthesis of various pharmaceutical compounds. Its unique structure and functional groups make it a valuable building block in the development of new drugs and medicinal agents.
Used in Synthetic Chemistry:
In the field of synthetic chemistry, 4-Hydroxy-1,5-naphthyridine is employed as a starting material for the preparation of more complex molecules. Its versatility in participating in various chemical reactions allows for the creation of a wide range of chemical products.
Although 4-Hydroxy-1,5-naphthyridine has limited direct applications in industry or manufacturing, its role as a reagent and building block in the synthesis of other compounds is significant, particularly in the pharmaceutical sector where it contributes to the development of new therapeutic agents.

InChI:InChI=1/C8H6N2O/c11-7-3-5-9-6-2-1-4-10-8(6)7/h1-5H,(H,9,11)

Upstream product

• 6320-39-4 3-aminopyridin-4-ol 
• 7664-93-9 sulfuric acid 
• 56-81-5 glycerol 
• 1018812-89-9 1,5-naphthyridin-5-oxide 4-ol 
• 25063-68-7 2,2-dimethyl-5-[(pyridin-3-ylamino)methylidene]-1,3-dioxane-4,6-dione 
• 462-08-8 pyridin-3-ylamine 
• 4901-93-3 3-carboxy-4-hydroxy-1,5-naphthyridine 
• 14029-71-1 2-(pyridin-3-yl)aminomethylene-malonic acid diethyl ester 
• 13801-51-9 4-hydroxy-1,5-naphthyridine-3-carboxylic acid ethyl ester 
• 952059-56-2 2,2-dimethyl-5-[[(1-oxidopyridin-3-yl)amino]methylidene]-1,3-dioxane-4,6-dione 

Downstream Products

• 7689-63-6 4-chloro-1,5-naphthyridine 
• 90001-34-6 4-bromo-1,5-naphthyridine 
• 79425-89-1 4-mercapto-1,5-naphthyridine 
• 952059-67-5 2-[2-methoxy-4-(1,5-naphthyridin-4-yloxy)phenyl]acetic acid 
• 5423-93-8 N¹,N¹-diethyl-N⁴-1,5-naphthyridin-4-ylpentane-1,4-diamine 
• 792173-99-0 1-(2-methylbenzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea 
• 27392-68-3 4-amino-1,5-naphthyridine 

Relevant academic research and scientific papers

Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action

Ebola virus (EBOV) causes a deadly hemorrhagic fever in humans and non-human primates. There is currently no FDA-approved vaccine or medication to counter this disease. Here, we report on the design, synthesis and anti-viral activities of two classes of compounds which show high potency against EBOV in both in vitro cell culture assays and in vivo mouse models Ebola viral disease. These compounds incorporate the structural features of cationic amphiphilic drugs (CAD), i.e they possess both a hydrophobic domain and a hydrophilic domain consisting of an ionizable amine functional group. These structural features enable easily diffusion into cells but once inside an acidic compartment their amine groups became protonated, ionized and remain trapped inside the acidic compartments such as late endosomes and lysosomes. These compounds, by virtue of their lysomotrophic functions, blocked EBOV entry. However, unlike other drugs containing a CAD moiety including chloroquine and amodiaquine, compounds reported in this study display faster kinetics of accumulation in the lysosomes, robust expansion of late endosome/lysosomes, relatively more potent suppression of lysosome fusion with other vesicular compartments and inhibition of cathepsins activities, all of which play a vital role in anti-EBOV activity. Furthermore, the diazachrysene 2 (ZSML08) that showed most potent activity against EBOV in in vitro cell culture assays also showed significant survival benefit with 100% protection in mouse models of Ebola virus disease, at a low dose of 10 mg/kg/day. Lastly, toxicity studies in vivo using zebrafish models suggest no developmental defects or toxicity associated with these compounds. Overall, these studies describe two new pharmacophores that by virtue of being potent lysosomotrophs, display potent anti-EBOV activities both in vitro and in vivo animal models of EBOV disease.

TOLL-LIKE RECEPTOR 8 (TLR8)-SPECIFIC ANTAGONISTS AND METHODS OF MAKING AND USES THEREOF

Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.

A fluorescent material, preparation method and application

The invention discloses a kind of fluorescent material, preparation method and application, wherein the fluorescent material of the molecular structure of the general formula as follows: R1 - R6 are each independently selected from H atom, deuterium atoms, to the electronic group or pulling in the electronic group a; and R1 - R6 at least one electron-donating groups, at least one of the is dragging the electronic group. The present invention provides fluorescent material, with twisted of - A D (Donor) (Acceptor) structure, at the same time with a heat-activated delay fluorescent and aggregation induced characteristic, not only can realize 100% internal quantum efficiency, but also can reduce the aggregation caused by the luminescence quenching process. These material is used as the doping and-layer films of the organic electroluminescent device in the light-emitting layer of the light-emitting object, its efficiency can be comparable with the phosphorescence, and avoid the problems of the prior phosphorescent material usually to use heavy metal is the iridium, platinum and the problem of expensive heavy metal, the cost is reduced.

Fluorescent material as well as preparation method and application thereof

The invention discloses a fluorescent material as well as a preparation method and application thereof. The structural general formula of the fluorescent material is formula (shown in the description), wherein R1-R10 are respectively independently selecte

Discovery of an Inhibitor of the Proteasome Subunit Rpn11

The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ～2.5 μM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ～400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.

Platinum complexes of 4-hydoxy-1,5-naphthyridines as emitting dyes

4-Hydoxy-1,5-naphthyridines (HNt) are derivatives of 8-hydroxyquinolines, yet possess a wider HOMO and LUMO band gap than the latter. The cyclometalated complex of platinum(II) with Nt exists in a square planner geometry, and has a high tendency to aggregate in condensedmedia. Such a phenomenon was verified by examining its photo-luminescence spectra in different concentrations. In a dilute solution, it exhibits a yellow phosphorescence centered at 530∑555 nm, yet red-shifted to ∑660 nm in a concentrated solution or in the solid state. This series of compounds can be used as emitting dyes in light-emitting diodes (LED). The LED devices with a configuration ITO/NPB/dye (6%) in CBP/BCP/AlQ3 or TPBI/LiF/Al displayed a yellow to red color, where NPB, CBP, BCP, AlQ3 and TPBI denote 4,4′-bis[N-(1-naphthyl), Nphenylamino] biphenyl, 4,4′-bis(carbazol-9-yl)biphenyl, 2,9-dimethyl-4,7-diphenyl-1,10-phenanthroline, tris(8-hydoxyquinolinato) aluminium, and 2,2′,2′-(1,3,5-benzenetriyl)tris(1-phenyl-1H- benzimidazole), respectively. The maximal light intensity exceeds 2.6 × 104 cd/m2 with an external quantum efficiency up to 5.8%.

Hydroxynaphthyridine-derived group III metal chelates: Wide band gap and dee blue analogues of green Alq (tris(8-hydroxyquinolate)aluminum) and their versatile applications for organic light-emitting diodes

A series of group III metal chelates have been synthesized and characterized for the versatile application of organic light-emitting diodes (OLEDs). These metal chelates are based on 4-hydroxy-1,5naphthyridine derivates as chelating ligands, and they are

NAPHTHYRIDINE DERIVATIVES

The invention concerns naphthyridine derivatives of Formula (Ia) or (Ib) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.