2400-95-5

Upstream product

• 118-48-9 isatoic anhydride 
• 49802-15-5 diethyl (4-chlorophenyl)phosphoramidate 
• 19959-41-2 methyl 2-[3-(4-chlorophenyl)ureido]benzoate 
• 79860-14-3 N-(4-Chloro-phenyl)-2-(3,3-dimethyl-ureido)-benzamide 
• 81541-40-4 R,S-N-(<3-<4-Chlorphenyl>-3,4-dihydro-4-oxo-2-chinazolinyl>-hydroxymethyl)acetamid 
• 104-12-1 p-chlorphenylisocyanate 
• 87-25-2 2-ethoxycarbonylaniline 
• 91-56-5 indole-2,3-dione 
• 106-47-8 4-chloro-aniline 
• 28831-39-2 2-(ethoxycarbonylmethyl)thio-3-(4-chlorophenyl)-4-oxo-3H-quinazoline 
• 133764-45-1 [3-(4-Chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylsulfanyl]-acetic acid hydrazide 
• 1028-40-6 3-(4-chlorophenyl)-2-thioxo-2,3-dihydro-1H-quinazolin-4-one 
• 118-92-3 anthranilic acid 
• 140-38-5 N-(4-chlorophenyl)urea 

Downstream Products

• 925016-67-7 1-[2-(3,4-dimethoxyphenyl)-2-oxoethyl]-3-(4-chlorophenyl)quinazoline-2,4-dione 
• 1228963-55-0 3-(4-chlorophenyl)-1-(4-chlorophenylsulfonyl)quinazoline-2,4(1H,3H)-dione 
• 1228963-54-9 3-(4-chlorophenyl)-1-phenylsulfonylquinazoline-2,4(1H,3H)-dione 
• 1228963-56-1 3-(4-chlorophenyl)-1-(4-methylphenylsulfonyl)quinazoline-2,4(1H,3H)-dione 
• 115540-75-5 1-methyl-3-(4-chlorophenyl)quinazolin-2,4(1H,3H)-dione 
• 1028-40-6 3-(4-chlorophenyl)-2-thioxo-2,3-dihydro-1H-quinazolin-4-one 
• 16081-94-0 3-(4-chlorophenyl)quinazoline-2,4(1H,3H)-dithione 

Relevant academic research and scientific papers

Synthesis, 2D-QSAR studies and biological evaluation of quinazoline derivatives as potent anti-trypanosoma cruzi agents

Background: Chagas disease affects about 7 million people worldwide. Only two drugs are currently available for the treatment for this parasite disease, namely, benznidazol (Bzn) and nifurtimox (Nfx). Both drugs have limited curative power in the chronic phase of the disease. Therefore, continuous research is an urgent need so as to discover novel therapeutic alternatives. Objective: The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy. Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set of quinazolinone and quinazoline derivatives were studied as trypanocidal agents. All compounds were screened in vitro against Trypanosoma cruzi (Tulahuen strain, Tul 2 stock) epimastigotes and bloodstream trypomastigotes. Results: Out of 34 compounds synthesized and tested, six compounds (5a, 5b, 9b, 9h, 13f and 13p) displayed significant activity against both epimastigotes and tripomastigotes, without exerting toxicity on Vero cells. Conclusion: The antiprotozoal activity of these quinazolinone and quinazoline derivatives represents an interesting starting point for a medicinal chemistry program aiming at the development of novel chemotherapies for Chagas disease.

2-[3-(4-morpholinyl)propylamine]-3-aryl-4-quinolinone compounds and application thereof

The invention belongs to the technical field of medicines and relates to 2-[3-(4-morpholinyl)propylamine]-3-aryl-4-quinolinone compounds and an application thereof. 2-[3-(4-morpholinyl)propylamine]-3-aryl-4-quinolinone derivatives comprise stereisomers and pharmaceutically applicable salts of the compounds and have the general structural formula shown in the description, wherein R is described inthe claims and description. The 2-[3-(4-morpholinyl)propylamine]-3-aryl-4-quinolinone derivatives and pharmaceutically applicable acid-added salts of the compounds can be combined with existing medicines or used separately to serve as influenza virus inhibitors to treat influenza and have better curative effects on various type-A influenza in particular.

Oxidative Rearrangement of Isatins with Arylamines Using H2O2 as Oxidant: A Facile Synthesis of Quinazoline-2,4-diones and Evaluation of Their Antibacterial Activity

A green and highly efficient synthetic method for the synthesis of quinazoline-2,4-diones with hydrogen peroxide as the terminal oxidant has been developed. The reaction features the mild reaction conditions, broad substrate scope, metal-free catalysts, and sole byproduct water. A plausible mechanism for this process was proposed. Moreover, an antibacterial activity study was performed to evaluate the antimicrobial activities towards two Gram-negative bacterial strains (Escherichia coli, and Klebsiella pneumonia) and two Gram-positive bacterial strains (Staphylococcus epidermidis, and Staphylococcus aureus) using the Broth microdilution method.

Synthesis, molecular structure and spectroscopic studies of some new quinazolin-4(3H)-one derivatives; An account on the N- versus S-Alkylation

A new series of N- and S-alkylated products of 3-aryl-1H,3H-quinazolin-2,4-dione and 3-aryl-2-mercapto-3H-quinazolin-4-one, respectively, were prepared in good yields via efficient nucleophilic substitution reaction of the SH and NH substrates with methyl

Specific inhibitors of puromycin-sensitive aminopeptidase with a 3-(halogenated phenyl)-2,4(1H,3H)-quinazolinedione skeleton

Specific puromycin-sensitive aminopeptidase (PSA) inhibitors with a 3-(halogenated phenyl)-2,4(1H,3H)-quinazolinedione skeleton were prepared and their structure-activity relationships were investigated. The nature (F, Cl or Br), number and position(s) of the halogen atom(s) introduced into the 3-phenyl group were concluded to be critical determinants of the inhibitory activity.

Synthesis and antitumor evaluation of novel cyclic arylsulfonylureas: ADME-T and pharmacophore prediction

Novel derivatives of 5-(substituted)benzylidene-3-(4-substituted)phenylsulfonylimidazolidine-2,4-diones (3a-r), 1-(4-substituted)phenylsulfonyl-3-(4-substituted)phenylpyrimidine-2,4,6-(1H,3H,5H)-triones (6a-l), and 3-(4-substituted)phenyl-1-(4-substituted)phenylsulfonylquinazoline-2,4(1H,3H)- diones (8a-l) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from 9 different organs. The tested compounds have showed good inhibitory effect at the ovarian cancer (IGROV1) cell line. A significant inhibition for (RXF393) renal cancer cells was observed with series 3 compounds, while in the other two series 6 and 8, there was a significant inhibition of ovarian cancer cells (OVCAR-8) and melanoma cells (SK-MEL-2). Interestingly; beside the strong inhibition of compound 3q to IGROV1 and RXF393 cells, a great inhibition (199.62%) for (M14) Melanoma cells was observed at the tested concentration (10?μM). ADME-T and pharmacophore prediction methodology were used to study the antitumor activity of the most active compounds and to identify the structural features required for antitumor activity.

3-aryl(alkyl)quinazoline-2,4(1H,3H)-diones and their alkyl derivatives

Two-stage reaction of methyl anthranilate with aryl(alkyl) isocyanates in keeping with the quantumchemical calculations and XRD analysis resulted in 3-aryl(alkyl)quinazoline-2,4(1H,3H)-diones that by treatment with alkyl halides, phenacyl bromides, esters

One-pot synthesis of quinazoline-2,4(1H,3H)-diones and 2- thioxoquinazolinones with the aid of low-valent titanium reagent

(Chemical Equation Presented) An efficient, convenient, one-pot synthesis of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolinones was accomplished in good yields via the novel reductive cyclization of ethyl 2-nitrobenzoates with isocyanates or isothioc

An efficient one-pot procedure for preparation of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolinone derivatives under microwave irradiation

An efficient one-pot synthesis of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolinone derivatives are given by the condensation of isatoic anhydride, primary amine and urea or thiourea in the absence of organic or inorganic reagents under microwave irr

Rearrangement of 4-imino-(1H,4H)-3,1-benzoxazine-2-ones to 2,4- quinazolinediones via an isocyanate carboxamide intermediate

Reaction of 3-arylimino-2-indolinones 1 with m-chloroperbenzoic acid in CH2Cl2 or methanol at 0°C leads to the corresponding 3-aryl-2,4(1H,3H)- quinazolinediones 4 and (2-arylcarbamoyphenyl)carbamic acid methyl ester 5, respectively.