We report an expeditious synthesis of selected indazolo-quinazolinone derivatives via an iodine-mediated multi-component reaction (MCR).

Mohana Roopan S

Department of Chemistry

School of Advanced Sciences

Vellore Campus

Palaniraja J

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

RSC Advances

A serious Mosquito borne yellow fever is one of the grave diseases which affect the major population. Since there is no specific treatment for yellow fever, there is a necessity to develop an effective agent. The series of acridinone analogues 3 to 5 were synthesized with help of non-conventional microwave heating and confirmed by respective spectral characterization. 5c and 3b showed highest activity to kill 90% of larvae against A. aegypti and C. quinquefasciatus, respectively. Also the active products were treated to check the mortality of non-target aquatic species. Through the reports of the larvicidal bioassay, compounds 3b against C. quinquefasciatus whereas 5c against A. aegypti were found to be more active. By keeping this as a platform, further extension of the work can be done to find out a valuable drug for controlling disease vectors. © The Author(s) 2017.

Fulltext

Scientific Reports

Synthesis and insecticidal activity of acridone derivatives to Aedes aegypti and Culex quinquefasciatus larvae and non-target aquatic species

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

This work describes the nitric acid catalysed synthesis of wollastonite (CaSiO3) nanoparticles (NP) from tetraethyl orthosilicate and calcium nitrate tetrahydrate. The formed calcium silicate nanoparticles were characterized by Fourier transform infrared spectroscopy (FTIR), Powder X-ray Diffraction (PXRD), and scanning electron microscopy (SEM) equipped with X-ray micro analysis. The CaSiO3 NPs showed an excellent yield (93%) towards the synthesis of quinolines via Friedlander reaction. The synthesized compound 3-dimethyl-7-nitro-9-phenyl-3,4-dihydroacridin-1(2H)-one was characterized by various spectroscopic techniques. © 2017 Taylor &amp; Francis Group, LLC.

Inorganic and Nano-Metal Chemistry

Synthesis of calcium silicate nanoparticles and its catalytic application in Friedlander reaction

A new and highly efficient microwave promoted N-alkylation of triazolo-quinazolinones was developed by treating various phenyl-substituted heterocyclic amines with benzyl chloride using K2CO3 as a base in the presence of DMF. Also the heterocyclic amines were synthesized by condensing the 3-amino-1,2,4-triazole substituted benzaldehydes and 1,3-cyclohexanedione in the presence of microwave irradiation under solvent free condition. The synthesized heterocycles 4a–o and 6a–o were further confirmed by using different spectroscopic techniques such as NMR and HRMS. The compounds 6a–o was studied for their solvatochromic property with increasing polarity of solvents. The determinations of 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging effect of the scaffolds 6a–o were carried out by UV–Vis spectrometer. In terms of IC50 all the compounds have shown remarkable antioxidant property compared with Ascorbic acid. © 2016 Elsevier B.V.

Conventional spectroscopic identification of N-alkylated triazolo-quinazolinones and its antioxidant, solvatochromism studies

This study deals with a new and efficient metal-free regioselective synthesis of pyrimido-fused indazoles with nitrogen ring junction motifs. We have developed a metal-free domino type reaction between 3-aminoindazole, aryl aldehydes and aceotophenones in the presence of KOH/DMF that leads to pyrimido[1,2-b]indazole analogues. Response Surface Methodology (RSM) coupled with a Box-Behnken design (BBD) were utilized for exploring the effect of base used (A), temperature of reaction (B) and (C), reaction time. This approach can allow access to a variety of pyrimidoindazole fluorophores and related compounds. The compound N,N-dimethyl-4-(2-phenylpyrimido[1,2-b]indazol-4-yl)aniline (4e) displays the maximum fluorescence intensity at 518 nm and shows a fluorescence quantum yield of 0.068. The synthesized pyramido-fused indazoles have been evaluated for their free radical scavenging activity and compound 4f showed good antioxidant activity. © 2016 by the authors; licensee MDPI.

Molecules

A Metal-Free Regioselective Multicomponent Approach for the Synthesis of Free Radical Scavenging Pyrimido-Fused Indazoles and Their Fluorescence Studies

Journal	Data powered by TypesetRSC Advances
Publisher	Data powered by TypesetRoyal Society of Chemistry (RSC)
ISSN	20462069
Open Access	0