27440-42-2

Usage

Type of compound

Quinazolinone derivative
Used in medicinal chemistry as a building block for the synthesis of various pharmaceuticals and biologically active molecules

Potential pharmacological properties

anti-cancer, anti-inflammatory, and antimicrobial activities
Valuable tool for drug discovery and development

Upstream product

• 30507-15-4 3-(4-acetylamino-phenyl)-2-methyl-3H-quinazolin-4-one 
• 525-76-8 2-methyl-4-oxo-3,1-benzoxazine 
• 106-50-3 1,4-phenylenediamine 
• 1788-96-1 2-methyl-3-(4-nitrophenyl)-4-oxo-3,4-dihydroquinazoline 
• 122-80-5 N-acetyl-p-phenylenediamine 
• 118-92-3 anthranilic acid 
• 100-01-6 4-nitro-aniline 

Downstream Products

• 823801-51-0 2-chloro-N-(4-(2-methyl-4-oxoquinazolin-3(4H)-yl)phenyl)acetamide 
• 857759-23-0 3-chloro-propionic acid-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-anilide] 
• 138802-31-0 1-Ethyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 86716-41-8 N-(Imino-{N'-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-guanidino}-methyl)-4-methyl-benzenesulfonamide; hydrochloride 
• 86716-38-3 N-(Imino-{N'-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-guanidino}-methyl)-4-methoxy-benzenesulfonamide; hydrochloride 
• 86716-39-4 N-{4-[(Imino-{N'-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-guanidino}-methyl)-sulfamoyl]-phenyl}-acetamide; hydrochloride 
• 86716-40-7 N-(Imino-{N'-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-guanidino}-methyl)-benzenesulfonamide; hydrochloride 
• 138802-34-3 1-Benzyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 133764-70-2 1-(4-Chloro-phenyl)-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 138802-30-9 1-Methyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 138802-35-4 1-Benzoyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 133764-74-6 1-(2-Methoxy-phenyl)-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 138802-33-2 1-Cyclohexyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 
• 138802-32-1 1-Butyl-3-[4-(2-methyl-4-oxo-4H-quinazolin-3-yl)-phenyl]-thiourea 

Relevant academic research and scientific papers

Design, graph theoretical analysis, density functionality theories, Insilico modeling, synthesis, characterization and biological activities of novel thiazole fused quinazolinone derivatives

(Table presented.). A series of 2-(2-substituted benzylidenehydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolo din-3-yl]phenyl)quinazolin-4(3H)-one 7a-7l were synthesized and characterized by IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analyses. In this present study, the density functionality theory was performed to identify drug stability. Further we introduced graph theoretical analysis by utilised Kyoto Encyclopedia of Genes and Genomes (KEGG) database and Cytoscape software to identify drug target. Based on the observed drug target insilico modeling was executed to know effective drug. The antiepileptic effects of title compounds were evaluated by using MES and subcutaneous pentylenetetrazole (scPTZ) test. Acute neurological toxicity of title compounds was studied by using standardized rotorod test. After 0.5 hr of period many of the compounds showed anticonvulsant activity at MES or scPTZ test. Comparison of the biological activity of test compounds with its chemical structures indicates that, compounds possessing electron donating group exhibited superior activity than the analogs having electron withdrawing moieties. Among the electron donating group tested, amino derivative exhibited good activity than rest of derivatives. From the study it was concluded that, the compound 7j was established as very potent compared with rest of the compounds and standard drugs subjected to biological studies. Thus the compound 2-(2-[4-aminobenzylidene]hydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolidin-3-yl]phenyl) quinazolin-4(3H)-one (7j) came out as pilot derivative without any neurotoxicity with a wide spectrum of antiepileptic activity. Highlights: The performed work is having great significance in terms of Graph theoretical analysis used to identify drug target In silico modeling used to identify designed drug interaction with identify target Density functionality studies used to identify synthesized compound energy band gap which is correlate with enhancement of its biological activity Antiepileptic effects of entire synthesized quinazolinone scaffolds were evaluated by MES and scPTZ test 2-(2-[4-aminobenzylidene]hydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolidin-3-yl]phenyl) quinazolin-4(3H)-one (7j) was established as very potent compared to the rest of the compounds and standard drugs which were subjected to biological studies.

Synthesis, analgesic, anti-inflammatory, and in vitro antimicrobial activities of some novel quinazolin-4(3H)-one derivatives

With the aim of developing potent analgesic, anti-inflammatory, and antimicrobial agents a series of novel quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H-NMR, mass spectroscopy and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory, and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds were discussed. Compound 2-(2-(4-(trifluoromethyl)benzylidene)hydrazinyl)-N-(4-(2-methyl-4-oxoquinazolin- 3(4H)-yl) phenyl) acetamide 5e was determined to be the most active compound.

QUINAZOLINONE AND FUSED PYRIMIDINONE COMPOUNDS AND THEIR USE IN TREATING SODIUM CHANNEL-MEDIATED DISEASES OR CONDITIONS

This invention is directed to compounds of formula (I): wherein (A), n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Synthesis of Some New 2-Aryl-3-Hetaryl-4(3H) Quinazolones

2-Aryl (alkyl)-benzoxazin-4-ones (I, R = CH3, C6H5, C6H5CH2, p-NO2C6H4) are condensed with 2-amino hetaryls (pyridyl, pyrimidyl, thiazolyl), 1 and 2-amino anthraquinones, p-amino acetophenone and 1,2-diamines like ethylene diamine and o-phenylene diamine.The products are obtained in excellent yields and are characterised by infrared and elemental analysis.