Montmorillonite K10 efficiently catalyzed a one pot-three component cyclocondensation of isatoic anhydride, NH4OAc and aromatic/heteroaromatic aldehydes under ambient conditions to produce the corresponding 2-substituted-2,3-dihydroquinazolin-4(1H)-ones in good yields. The 2-(2-chloroquinolin-3-yl)-2,3-dihydroquinazolin-4(1H)-ones 3a-d were screened for their antitumor activity against Ehrlich Ascites Carcinoma tumor cells © 2011 Springer Science+Business Media B.V.

Mohana Roopan S

Department of Chemistry

School of Advanced Sciences

Vellore Campus

Nawaz Khan F

Jin J.S

Senthil Kumar R.

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Research on Chemical Intermediates

A series of imidazo-pyrimido fused acridines were synthesized and identified using conventional spectroscopic techniques. All the synthesized title compounds were subjected to in vitro antibacterial and insecticidal screenings. For insecticidal activity, the synthesized fused compounds are testing against two pests namely, Sitophilus oryzae (S. oryzae) and Callosobruchus maculatus (C. maculatus). For antibacterial screening, the compounds are testing against four bacteria, Bacillus subtilis (B. subtilis), Proteus mirabilis (P. mirabilis), Staphylococcus aureus (S. aureus) and Vibrio parahaemolyticus (V. parahaemolyticus). Notably, compound 8-(4-isopropylphenyl)-16-phenyl-6,7-dihydrobenzo[4′,5′]imidazo[1′,2′:1,2]pyrimido[4,5-a]acridine and 8-(2,4-dimethoxyphenyl)-16-phenyl-6,7-dihydrobenzo[4′,5′]imidazo[1′,2′:1,2]pyrimido[4,5-a]acridine were identified as the most promising applicant for further studies. © 2017 Elsevier B.V.

Journal of Molecular Liquids

Conventional spectroscopic identification of biologically active imidazo-pyrimido fused acridines: In vitro anti-bacterial and anti-feedant activity

Dihydroquinazolinones is an important core structure reported with a wide variety of pharmacological activities. They are capable of undergoing various transformations because of its reactivity towards various reagents. The synthetic strategies for the functionalization and derivatization of the nucleus were explained. The diversified pharmacological actions of this moiety were illustrated through various biochemical pathways. The structural-activity relationship study of dihydroquinazolinones anticipated the relationship between the various substituents and its role in the pharmacological action. The main objective of this review is to summarize the importance of dihydroquinazolinones in the field of chemical biology.

European Journal of Medicinal Chemistry

Synthetic strategy with representation on mechanistic pathway for the therapeutic applications of dihydroquinazolinones

A new series of brominated derivatives of 2, 3-dihydroquinazolin-4(1H)-one were synthesized and their structures were confirmed using IR, NMR and mass spectra. The synthesized derivatives were screened for their in vitro anthelmintic activity. The investigations on interaction of the bioactive compound, 2i with bovine serum albumin (BSA) were evaluated. The quenching mechanism of the compound, 2i was deduced based on the results of Stern–Volmer equation. The number of binding site, prediction of binding site region and the changes in the secondary structure of protein were predicted using various spectroscopic studies.

Journal of Luminescence

Study of binding interaction between anthelmintic 2, 3-dihydroquinazolin-4-ones with bovine serum albumin by spectroscopic methods

A non-conventional methodology has been utilized for the synthesis of a series of 1,2,4-triazolo-quinazoline-thiones (2a-l). Here the reaction was carried out between 1,2,4-triazolo-quinazolinones (1a-l), in the presence of 1,4-dioxane. The mixture was irradiated under microwave (100W) for 7min to obtain targeted molecules (2a-l). All the synthesized molecules were confirmed by (1)H, (13)C NMR and HRMS. The solvatochromic property (absorption spectra) of compounds (2a-l) in solvents of different polarities was studied. The compounds (2a-l) were further subjected for their in vitro free radical screening using 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and also screened for their in vitro anti-fungal property against Aspergillus flavus (A. flavus) and Aspergillus niger (A. niger). The results from free radical scavenging assay showed promising activity for compounds 2a, e-i, whereas compound 2d showed significant antioxidant activity when compared to ascorbic acid. In vitro anti-fungal study showed that the 1,2,4-triazolo-quinazoline-thiones (2a-l) had significant activity against A. flavus and A. niger compared with widely used antifungal agent Fluconazole.

Journal of Photochemistry and Photobiology B: Biology

1,2,4-Triazolo-quinazoline-thiones: Non-conventional synthetic approach, study of solvatochromism and antioxidant assessment

A series of 6,7-dihydro-[1,2,4]triazolo[5,1-b]quinazolin-8(5H)-ones, 4a–o were synthesized via a one-pot, multicomponent reaction in the presence of water as a solvent under microwave irradiation using ceric ammonium nitrate as an oxidizing agent. This techno-chemical method provides a rapid construction of higher molecules in short duration with high yield. The adopted method was carried out in the presence of water without catalyst and yielded the compounds without any side products, and thus further purification of compounds by column chromatography was not required. All the synthesized compounds, 4a–o were screened for their 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity. All the compounds, 4a–o possessed moderate antioxidant activity when compared to their standard antioxidant (ascorbic acid). © 2015, Springer Science+Business Media Dordrecht.

Microwave assisted synthesis of ring junction heterocyclic antioxidants

An efficient and regioselective N-alkylation of 4(3H)-pyrimidone with various electrophiles in the presence of Fe nano particle is reported. The catalyst initiates N-alkylation of amides by alkyl chlorides. The reaction of equimolar 4(3H)-pyrimidone and 2-chloro-3-(chloromethyl)quinolines in the presence of KOH and Fe nano particle (5 mol %) in DMSO solution under reflux condition formed 3-[(2-chloroquinolin-3-yl]methyl)pyrimidin-4(3H)ones. © 2010 Elsevier Ltd. All rights reserved.

Tetrahedron Letters

Fe nano particles mediated C–N bond-forming reaction: Regioselective synthesis of 3-[(2-chloroquinolin-3-yl)methyl]pyrimidin-4(3H)ones

Solvent-free syntheses of quinazolin-4(3H)-ones were performed by reaction of anthranillic acid with different amides, such as nicotinamide, benzamide, formamide, etc., on montmorillonite K-10. Products were confirmed by FTIR, 1HNMR, and 13CNMR spectroscopic techniques. All synthesized compounds exhibited antioxidant properties and have been compared with standard antioxidant BHT.Key words: quinazolinone, montmorillonite K-10, solvent-free conditions, antioxidant properties.

Canadian Journal of Chemistry

Solvent-free syntheses of some quinazolin-4(3H)-ones derivatives

Novel 6,8-dibromo-4(3H)quinazolinone derivatives of anti-bacterial and anti-fungal activities

Bioorganic & Medicinal Chemistry

Quinazolinone linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates: Design, synthesis and biological evaluation as potential anticancer agents

Arkivoc

Synthesis, antioxidant, hemolytic and cytotoxic activity of AB ring cores of mappicine

An efficient one pot–three component cyclocondensation in the synthesis of 2-(2-chloroquinolin-3-yl)-2,3-dihydroquinazolin-4(1H)-ones: potential antitumor agents

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ISSN	0922-6168
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