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Novel Schiff Base-bridged quinazolinone Imidazoles:Synthesis, Antimicrobial Activity and Supramolecular Interaction with DNA

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Novel Schiff Base-bridged Quinazolinone Imidazoles:Synthesis...

全国第十八届大环化学暨第十届超分子化学学术讨论会

作者：方贤富 Hui Wang 周成合 Key Laboratory of Applied Chemistry of Chongqing Municipality Institute of Bioorganic ＆ Medicinal Chemistry School of Chemistry and Chemical Engineering Southwest University

＜正＞A series of novel Schiff base-bridged quinazolinone imidazoles were synthesized and confirmed by NMR and MS *** bioactive assay manifested that most target compounds exhibited good antimicrobial *** them,compoun... 详细信息

关键词： quinazolinone Schiff base Imidazoles Antimicrobial Supramolecular

Synthesis and Their Supramolecular Transportation and Activity of Antimicrobial quinazolinone Nitroimidazoles

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Synthesis and Their Supramolecular Transportation and Activi...

全国第十七届大环化学暨第九届超分子化学学术研讨会

作者：彭丽萍周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Quinolones are one of the most widely prescribed antimicrobial agents as they are generally well tolerated with excellent safety profile and favorable pharmacokinctic ***,with the increasing emergencies of micro... 详细信息

关键词： quinazolinone Nitroimidazole Antimicrobial Supramolecular Transportation

Design and synthesis of a series of quinazolinone derivatives as antibiotic against ***

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Design and synthesis of a series of quinazolinone derivative...

第十届全国化学生物学学术会议

作者： Jianbin Zhen Kewu Yang Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

Drug-resistant bacteria pose an urgent public-health crisis. Over the years, β-lactams were the antibiotics of choice for treatment of S. aureus infections1. However, the overuse of these antibiotics has resulted in a large number of bacteria with resistance to most current drugs. So, the present needs for new classes of antibacterial drugs are essential. quinazolinone represents a class of annulated six-membered nitrogen heterocycles2-3. These compounds show extensively biological and pharmacological activity, for instance, antitumor, anti-inflammatory, antihistamine, and antimicrobial et al. Based on the above information, we designed and synthesized quinazolinone derivatives as new antibiotics with potent activity against S. aureus. The synthesis route was showed in Scheme 1.

关键词： Drug-resistant bacteria Antibiotics quinazolinone

Synthesis and evaluation of some novel additives as antioxidants and corrosion inhibitors for petroleum fractions

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Petroleum Science 2014年第1期11卷 161-173页

作者： Ahmed El-Mekabaty Osman M. O. Habib Department of Chemistry Faculty of Science Mansoura University

Benzoxazinone 2 was prepared and reacted with formamide,acetamide,some primary aromatic amines and heterocyclic amines giving the corresponding quinazolone derivatives 3-15 *** reaction of benzoxazinone 2 with hydrazine hydrate and phenyl hydrazine was also *** compounds of the synthesized products were evaluated as antioxidants and corrosion inhibitors for gasoline engine lubricating *** highest antioxidant activities were obtained with compounds *** optimum concentration recommended for these new additives was found to be *** for 1L ofoil for compounds *** addition,some of the highly effective antioxidant additives,namely 10-15,were thermally analyzed by using thermogravimetric analysis （TGA） and differential thermal gravimetric analysis （DTGA） techniques and the results indicated that compounds are thermally stable and could be used under thermal ***,a comparison of the oxidation stability between the tested oil containing the prepared products and lubricating oil containing commercial additives was also studied.

关键词： Benzoxazinone quinazolinone thermal stability antioxidant additives anticorrosive additives

Clean heterocyclic synthesis in water:I_2/KI catalyzed one-pot synthesis of quinazolin-4(3H)-ones

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Chinese Chemical Letters 2008年第12期19卷 1403-1406页

作者： Mehdi Bakavoli Ali Shiri Zahra Ebrahimpour Mohammad Rahimizadeh Department of Chemistry School of SciencesFerdowsi UniversityMashhad 91775-1436Iran

Oxidative cyclocondensation of o-aminobenzamide with various aldehydes in water using I2/KI as catalyst and oxidizing agent is carded out giving the corresponding quinazolin-4（3H）-ones 3a-n in good to excellent yields.

关键词： Iodine quinazolinone Cyclocondensation

Identify Phthalazine[1,2-b]quinazolinones as p53 Activators in Bladder Cancer Cells

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Identify Phthalazine[1,2-b]quinazolinones as p53 Activators ...

中国化学会第十三届全国有机合成化学学术研讨会

作者： Jing-Mei Yuan Guo-Hai Zhang Gang Qian Guo-Xue He Qing-Qing Liu Cheng-Xue Pan Gui-Fa Su State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources School of Chemistry ＆ Pharmaceutical SciencesGuangxi Normal University

p53 inactivation is a new clinically defined characteristic for cancer *** is therefore highly desirable to develop anticancer agents by restoring p53 *** the synthesized phthalazine[1,2-b]quinazolinones were discovered as p53 activators in bladder cancer cells,especially for compound 5 d A,identified as a most promising candidate in view of both its anticancer activity and mechanisms of action.5 d A exhibited strong anticancer activity on a broad range of cancer cell lines and significantly reduced tumor growth in xenograft models at doses as low as 6 mg/***,5 d A caused cell cycle arrest at S/G2 phase,induced apoptosis,changed cell size and led to cell death by increasing the proportion of sub-G1 *** mechanism studies suggested that targeting accumulation of phospho-p53 in mitochondrial by 5 d A resulted in conformational activation of Bak,thereby evoking cell apoptosis,finally leading to irreversible cancer cell *** present studies furnish new insights into comprehension the molecular interactions and anticancer mechanisms of phospho-p53-dependent quinazolinone compound.

关键词： quinazolinone p53 conformational activation of Bak apoptosis

Synthesis and Crystal Structure of 2-(4-Oxo-3-o- tolyl-3,4-dihydroquinazolin-2-ylthio)acetohydrazide

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Chinese Journal of Structural Chemistry 2012年第9期31卷 1329-1333页

作者： Aamer Saeed Shams-ul-Mahmood Ulrich Flörke Department of Chemistry Quaid-I-Azam UniversityIslamabad 45320Pakistan Department Chemie Fakultät fur NaturwissenschaftenUniversität PaderbornWarburgerstrasse 100D-33098 PaderbornGermany

The title compound was synthesized from 3-（2-methylphenyl）-2-thioxo-2,3-dihy- droquinazolin-4（1H）-one （4） which was prepared from 2-methylaniline in two steps. The structure was supported by the spectroscopic data and unambiguously confirmed by single-crystal X-ray diffraction studies. It crystallizes in the orthorhombic space group Pbca with unit cell dimensions a = 6.687（4）, b = 24.788（16）, c = 30.453（19）  V = 5048（5） 3 and Z = 8.

关键词： quinazolinone acetohydrazide synthesis

Simplification of Rutaecarpine and Luotonin A to tricyclic fused ring and derivatization on ring A for antineoplastic activity

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Simplification of Rutaecarpine and Luotonin A to tricyclic f...