10376-59-7

Upstream product

• 107-07-3 2-chloro-ethanol 
• 118-92-3 anthranilic acid 
• 141-43-5 ethanolamine 
• 78-39-7 Triethyl orthoacetate 
• 1885-29-6 anthranilic acid nitrile 
• 3416-93-1 2-(4,5-Dihydro-1,3-oxazol-2-yl)aniline 
• 879094-46-9 2-(2-methyl-4-oxo-3,4-dihydro-3-quinazolinyl)ethyl acetate 
• 89-52-1 o-acetylamino-benzoic acid 
• 525-76-8 2-methyl-4-oxo-3,1-benzoxazine 

Downstream Products

• 132808-61-8 3-{2-[3-(4-Chloro-phenylamino)-2-hydroxy-propoxy]-ethyl}-2-methyl-3H-quinazolin-4-one 
• 132808-49-2 2-phenyl-4(3H)-oxoquinazolin-3-ylethyl chloroacetate 
• 132808-52-7 o-Tolylamino-acetic acid 2-[4-oxo-2-((E)-styryl)-4H-quinazolin-3-yl]-ethyl ester 
• 111970-11-7 3-(2-benzoyloxyethyl)-2-(1,2-epoxy-2-phenylethyl)quinazolin-4(3H)-one 
• 111970-13-9 11H-5-acetoxy-1,2,4,5-tetrahydro-4-phenyl<1,4>oxazepino<5,4-b>quinazolin-11-one 
• 111970-10-6 2-(1,2-epoxy-2-phenylethyl)-3-(2-hydroxyethyl)quinazolin-4(3H)-one 
• 111970-12-8 11H-5-hydroxy-1,2,4,5-tetrahydro-4-phenyl<1,4>oxazepino<5,4-b>quinazolin-11-one 
• 111970-09-3 3-(2-benzoyloxyethyl)-2-(2-phenylethenyl)quinazolin-4(3H)-one 
• 68501-37-1 3-(2-hydroxyethyl)-2-(2-phenylethenyl)quinazolin-4(3H)-one 

Relevant academic research and scientific papers

Synthesis of quinazoin-4-ones through an acid ion exchange resin mediated cascade reaction

An interesting cascade reaction of N-(2-(4,5-dihydrooxazol-2-yl)phenyl)benzamide in the presence of an acid ion exchange resin is described. In this reaction, a range of substrates bearing various substituent groups are well compatible. This work provides a green and atom-economical alternative approach for the synthesis of quinazolin-4-ones in good yields.

Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases

A combinatorial series of novel quinazolin-4(3H)-ones were synthesised and their structures were established based on spectroscopic data (IR, NMR, EI-MS, and FAB-MS). The compounds were tested for inhibition of the zinc metalloproteinase thermolysin (TLN) utilizing a chemical array-based approach. Some of the compounds were found to inhibit TLN, with IC50 values ranging from 0.0115 μM (compound 3) to 122,637 μM (compound 29). Compound 3 [3-phenyl-2-(trifluoromethyl) quinazolin-4(3H)-one] (IC50 = 0.0115 μM) and compound 35 [3-(isopropylideneamino)-2,2-dimethyl-2,3-dihydroquinazolin-4 (1H)-one] (IC50 = 0.2477 μM) were found to be the most potent inhibitors.

Investigating biological activity spectrum for novel styrylquinazoline analogues

In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.

FIBRATE COMPOUNDS HAVING PPAR AGONIST ACTIVITY

There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH2-, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R1 and R2, which may be the same or different, are independently chosen from hydrogen and C1-C8 alkyl, or R1 and R2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R3 is chosen from hydrogen and C1-C8 alkyl; R4, R5, and R6, which may be the same or different, are independently chosen from hydrogen and C1-C8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARα agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARα agonist activity and a PPARα agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.

New Reaction of Deoxyvasicinone. Part 6

Several acylated derivatives of deoxyvasicinone 1 and its analogues were shown to exist as enols.The 3-hydroxymethyl derivative of 1 was shown to undergo rapid dehydration and products derived from an intermediate 3-methylene compound were obtained.Novel oxazepino analogues of 1 are reported.