53878-47-0

Usage

Uses

Used in Pharmaceutical Industry:
5-Hydroxy-4-oxo-4H-chromene-2-carboxylic acid is used as a potential anti-inflammatory agent for its ability to reduce inflammation, which can be beneficial in treating conditions characterized by excessive inflammation.
5-Hydroxy-4-oxo-4H-chromene-2-carboxylic acid is also used as a potential antioxidant agent for its ability to neutralize free radicals, which can help protect cells from oxidative damage and contribute to the prevention of various diseases.
Used in Drug Development:
5-Hydroxy-4-oxo-4H-chromene-2-carboxylic acid is used as a promising candidate for drug development due to its potential biological activity and the possibility of treating various diseases and conditions. Further research is needed to understand its full potential and optimize its use in pharmaceutical formulations.

Upstream product

• 699-83-2 2,6-dihydroxylacetophenone 
• 95-92-1 oxalic acid diethyl ester 
• 50521-64-7 5-hydroxy-4-oxo-4H-benzopyran-2-carboxylic acid ethyl ester 
• 703-23-1 2'-hydroxy-6'-methoxyacetophenone 
• 5527-76-4 ethyl 5-methoxy-4-oxo-4H-chromene-2-carboxylate 
• 5527-74-2 5-methoxy-4-oxo-4H-chromene-2-carboxylic acid 

Downstream Products

• 546093-05-4 MH-11 
• 546093-13-4 N-[(4-chlorophenyl)methyl]-5-hydroxy-4-oxochromene-2-carboxamide 
• 328058-17-9 5-hydroxy-N-methyl-N-[4-(4-morpholinylmethyl)phenyl]-4-oxo-4H-1-benzopyran-2-carboxamide hydrochloride 

Relevant academic research and scientific papers

Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- And BCRP-Mediated Multidrug Resistance

Overexpression of ATP binding cassette (ABC) transporters, including P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), is an important factor leading to multidrug resistance (MDR) in cancer treatments. Three subclasses of dual inhibitors of P-gp and BCRP were designed based on the active moieties of BCRP inhibitors, tyrosine kinase inhibitors, and P-gp inhibitors, of which compound 21 possessed low cytotoxicity, high reversal potency, and good lipid distribution coefficient. 21 also increased the accumulation of Adriamycin (ADM) and Mitoxantrone (MX), blocked Rh123 efflux, and made no change in the protein expression of P-gp and BCRP. Importantly, coadministration of 21 can significantly improve the oral bioavailability of paclitaxel (PTX). It was also demonstrated that 21 significantly inhibited the growth of K562/A02 xenograft tumors by increasing the sensitivity of ADM in vivo. In summary, 21 has the potential to overcome MDR caused by P-gp and BCRP and to improve the oral bioavailability of PTX.

ANTI-INFECTIVE AGENTS

The present invention relates to a novel class of chromene-2-carboxamide compounds inhibitors of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and their use as anti-infective agents in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF ASTHMA AND ALLERGY

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of fo

COMPOSITIONS AND METHODS FOR THE TREATMENT OF ASTHMA AND ALLERGY

The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of

NOVEL P-GLYCOPROTEIN INHIBITOR, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A p-glycoprotein inhibitor of Formula 1 is capable of effectively preventing the development of multi-drug resistance directed to an anticancer agent in cancer cells, and greatly enhances the bioavailability of the drug, such as paclitaxel, which is not readily absorbed when orally administered.

2-benzoylchromone derivatives

Hydroxy-substituted 2-benzoyl-chromone derivatives (I) are new. Benzoyl-chromone derivatives of formula (I) and their derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. R = OH, OA, phenoxy, Ar, OCOA, SO3H, SO3A, OSO3H

Modulation of P-glycoprotein-mediated multidrug resistance by flavonoid derivatives and analogues

Flavonoid derivatives were synthesized and tested for their ability to modulate P-glycoprotein (Pgp)-mediated multidrug resistance (MDR) in vitro. These compounds belong to various flavonoid subclasses, namely: chromones, azaisoflavones, and aurones. Among the investigated compounds, three showed potent reversing activity. 2-(4-Methylpiperazin-1-ylcarbonyl)-5-hydroxychromone (4a), 5,7-dimethoxy-3-phenyl-4-quinolone (5), and 4,6-dimethoxyaurone (6) potentiated daunorubicin cytotoxicity on resistant K562 cells. They were also able to increase the intracellular accumulation of rhodamine-123, a fluorescent molecule which acts as a probe of P-glycoprotein-mediated MDR. This suggests that these compounds act, at least in part, by inhibiting P-glycoprotein activity. The most active compound, 5-hydroxy-2-(4-methylpiperazin- 1-ylcarbonyl)chromone (4a) was found to be a powerful reversal agent, more potent than cyclosporin A, used as the reference molecule. No effect was observed on MRP transport nor on cell proliferation. Little apoptosis was induced on K562S cells with 4a compared to K562R, probably due to the extrusion of the compound by Pgp.