- Synthesis and structure analysis of 2-(2′-propanonylthio)-3-(o-methyl phenyl) quinazol-4(3H)-one
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The three-dimensional molecular and crystal structure of 2-(2′-propanonylthio)3-(o-methyl phenyl)quinazol-4(3H)-one has been determined by X-ray crystallographic methods. This compound crystallizes in the orthorhombic space group Pbca with unit
- Rajnikant,Dinesh,Mousmi,Deshmukh,Patil,Sawhney, Anshu
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- Energy barriers to rotation in axially chiral quinazoline-4-ones
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Axially chiral 2-thioxo-3-(o-aryl)-quinazolin-4-ones and 2-(benzylthio)-3-(o-aryl)-quinazolin-4-ones were synthesized and their energy barriers to rotation about the N3-Caryl bond were determined by thermal racemization of the separa
- Hakgor, Ari,Erol Gunal, Sule
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- Enhancement of Different Biomedical Activities of Newly Synthesized Quinazoline Derivatives
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A series of newly synthesized compounds of quinazolinone by various substituents was screened for its pharmacological activities. These included their action as antibacterial agents against pathogenic bacteria (Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa) and as antifungal agents against Aspergillus niger and pathogenic yeast (Candida albicans). The presently investigated compounds were synthesized in higher yields, and the structure features were elucidated on the basis of IR, 1H-NMR, and mass and elemental analysis data. These compounds were also evaluated as antioxidant agent. The results revealed that six compounds (2a, 11b, 11a, 2b, 13a, and 3c) exhibited higher antimicrobial activity against the tested pathogenic strains. In addition, it was found that compound 6a exhibited a radical scavenging activity higher than other studied compounds.
- Zeid, Ibrahim F.,Kassem, Emad M.,Mohamed, Neama A.,Salman, Ahmed A.,Shalaby, Al Shimaa G.
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p. 1280 - 1290
(2018/06/20)
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- Antimicrobial activities of some synthesized 1-(3-(2-methylphenyl)-4-Oxo-3H-quinazolin-2-yl-4-(substituted)thiosemicarbazide derivatives
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The substituted thiosemicarbazide moiety was placed at the C-2 position and 2-methylphenyl group at N-3 position of quinazoline ring and obtained compounds were tested for their antitubercular activities and antibacterial activities against selected gram-positive and gram-negative bacteria. The target compounds 1-(3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl)-4-(substituted) thiosemicarbazides were obtained by the reaction of 2-hydrazino-3-(2-methylphenyl) quinazolin-4(3H)-one with different dithiocarbamic acid methyl ester derivatives. All synthesized compounds were also screened for their antimicrobial activity against selective gram-positive and gram-negative bacteria by agar dilution method. Among the series, 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-chlorophenyl]-thiosemicarbazide exhibited the most potent activity against S. typhi, E. coli, and B. subtilis, while 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-nitrophenyl]-thiosemicarbazide was the most potent against E. coli, B. subtilis, P. aeruginosa, S. typhi, and S. flexneri. These two compounds exhibited the antitubercular activity at the minimum concentration (3 μg/mL) that offered potential for further optimization and development of new antitubercular agents. The obtained results demonstrated promising antimicrobial and antitubercular activities of the synthesized quinazoline compounds which could be used as new scaffolds for improving their antimicrobial activity.
- Alagarsamy,Anjana,Sulthana,Parthiban,Solomon, V. Raja
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p. 332 - 339
(2016/07/06)
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- Nanomagnetically modified polyphosphoric acid (NiFe2O4@SiO2-PPA): An efficient, fast, and reusable catalyst for the synthesis of 2-thioxoquinazolinones under solvent-free conditions
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Polyphosphoric acid functionalized silica-coated magnetic nanoparticles with core-shell structure (NiFe2O4@SiO2-PPA) has been used as a magnetically recyclable green catalyst for the one-pot three-component synthesis of 2-thioxoquinazolinones by the reaction of isatoic anhydride, primary amines and thiourea under neat conditions. The catalyst is readily recovered by simple magnetic decantation and can be recycled five times with no significant loss of catalytic activity.
- Eshghi, Hossein,Khojastehnezhad, Amir,Moeinpour, Farid,Bakavoli, Mehdi,Zeinabi, Nafiseh,Allameh, Sadegh
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p. 7915 - 7924
(2015/04/16)
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- Synthesis and Anticonvulsant Activity Evaluation of 4-Phenyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one and Its Derivatives
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A series of 4-(substituted-phenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones (6a-x) with triazole and other heterocyclic substituents (7-14) were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity by maximal electroshock (MES) and rotarod neurotoxicity tests. Among the compounds studied, 6o and 6q showed wide margins of safety with protective indices (PIs) that were much higher than those of currently used drugs (PI6o > 25.5, PI6q > 26.0). Compounds 6o and 6q showed significant oral activity against MES-induced seizures in mice, with ED50 values of 88.02 and 94.6 mg/kg, respectively. The two compounds were also found to have potent activity against seizures that were induced by pentylenetetrazole and bicuculline. A series of 4-(substituted-phenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones with triazole and other heterocyclic substituents were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity using maximal electroshock and rotarod neurotoxicity tests.
- Zhang, Hong-Jian,Jin, Peng,Wang, Shi-Ben,Li, Fu-Nan,Guan, Li-Ping,Quan, Zhe-Shan
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p. 564 - 574
(2015/08/06)
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- Synthesis and characterization of new (E)-N'-(substituted benzylidene)-2-(3-(2-methyl)-4-oxo-3,4-dihydroquinazolin-2-ylthio) acetohydrazides
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A small library of new azomethine derivatives of 3-aryl-2-thioxo-2,3- dihydroquinazolin-4(1H)-ones was synthesized. The key intermediates 2-thioxo-quinazolinones (3a-e), obtained in 2 steps from the corresponding anilines, were treated with methyl chloroa
- Saeed, Aamer,Mahmood, Shams-Ul,Floerke, Ulrich
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p. 275 - 287
(2014/04/03)
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- Design and synthesis of novel 2-(3-substituted propyl)-3-(2-methyl phenyl) quinazolin-4-(3H)-ones as a new class of H1-antihistaminic agents
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A series of novel 2-(3-substituted propyl)-3-(2-methyl phenyl) quinazolin-4-(3H)-ones were synthesized by the reaction of 2-(3-bromopropyl thio)-3-(2-methyl phenyl) quinazolin-4-(3H)-one with various amines. The starting material, 2-(3-bromopropyl thio)-3
- Alagarsamy,Parthiban
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- Synthesis and antimicrobial evaluation of some new 1,3,4-oxadiazoles
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A series of 2-((4-acetyl-5-(aryl)-5-methyl-4,5-dihydro-1,3,4-oxadiazol-2- yl) methylthio)-3-o-tolylquinazolin-4(3H)-one 5 was synthesized by the cyclization of imines 4 using acetic anhydride. The Schiffs base 4 are obtained by the reaction of appropriate
- Godhani,Dobariya,Sanghani
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p. 259 - 262
(2013/09/24)
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- Synthesis and pharmacological investigation of novel 4-(2-methylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-o nes as new class of H1-antihistaminic agents
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A series of novel 1-substituted-4-(2-methylphenyl)-4H-[1,2,4]triazolo[4,3-a]quinazolin-5-o nes were synthesized by the cyclization of 2-hydrazino-3-(2-methylphenyl)-3H-quinazolin-4-one with various one carbon donors. The starting material 2-hydrazino-3-(2
- Alagarsamy,Rupeshkumar,Kavitha,Meena,Shankar,Siddiqui,Rajesh
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p. 2331 - 2337
(2008/12/23)
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- Synthesis and pharmacological evaluation of some 3-(2-methylphenyl)-2- substituted amino-quinazolin-4(3H)-ones as analgesic and anti-inflammatory agents
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A variety of novel 3-(2-methylphenyl)-2-substituted amino-quinazolin-4(3H)- ones were synthesized by reacting the amino group of 2-hydrazino-3-(2- methylphenyl)-quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material 2-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)-one was synthesized from 2-methyl aniline. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. Among these, the compound 2-(1-ethylpropylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)- one emerged as the most active compound for analgesic activity, while the compound 2-(1-methylbutylidene)-hydrazino-3-(2-methylphenyl)-quinazolin-4(3H)- one showed most potent anti-inflammatory activity of the series and was moderately more potent in its anti-inflammatory activity when compared to the reference standard diclofenac sodium (CAS 15307-86-5). Interestingly, the test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid (CAS No: 50-78-2). ECV - Editio Cantor Verlag.
- Alagarsamy, Veerachamy,Solomon, Viswas Raja,Murugesan, Sankaranarayanan
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p. 174 - 181
(2008/09/19)
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- Heterocycles as cholecystokinin (CCK) ligands
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Novel quinazolinone derivatives with good binding affinity for the CCK-A and CCK-B receptors, pharmaceutical compositions containing them and methods of using them are taught. The compounds are useful agents to suppress appetite, reduce gastric acid secre
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(2008/06/13)
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