- 2-[3-(4-morpholinyl)propylamine]-3-aryl-4-quinolinone compounds and application thereof
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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.
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Paragraph 0051; 0063
(2018/04/21)
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- Oxidative Rearrangement of Isatins with Arylamines Using H2O2 as Oxidant: A Facile Synthesis of Quinazoline-2,4-diones and Evaluation of Their Antibacterial Activity
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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.
- Shi, Guanghao,He, Xinwei,Shang, Yongjia,Yang, Cheng,Xiang, Liwei
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p. 1835 - 1843
(2017/09/06)
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- Synthesis, molecular structure and spectroscopic studies of some new quinazolin-4(3H)-one derivatives; An account on the N- versus S-Alkylation
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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
- Hagar, Mohamed,Soliman, Saied M.,Ibid, Farahate,El Ashry, El Sayed H.
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p. 667 - 679
(2016/01/09)
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- Specific inhibitors of puromycin-sensitive aminopeptidase with a 3-(halogenated phenyl)-2,4(1H,3H)-quinazolinedione skeleton
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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.
- Matsumoto, Yotaro,Noguchi-Yachide, Tomomi,Nakamura, Masaharu,Mita, Yusuke,Numadate, Akiyoshi,Hashimoto, Yuichi
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p. 1449 - 1463
(2013/08/23)
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- An efficient synthesis of quinazoline-2,4-dione derivatives with the aid of a low-valent titanium reagent
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A facile synthetic method using low-valent titanium reagent (TiCl4/Zn system) to promote the novel reductive cyclization of 2-nitrobenzamides and triphosgene is described. Sequentially, a series of quinazoline-2,4-diones were synthesized in goo
- Shi, Da-Qing,Dou, Guo-Lan,Li, Zheng-Yi,Ni, Sai-Nan,Li, Xiao-Yue,Wang, Xiang-Shan,Wu, Hui,Ji, Shun-Jun
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p. 9764 - 9773
(2008/02/12)
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- An efficient one-pot procedure for preparation of 2,4(1H,3H)-quinazolinediones and 2-thioxoquinazolinone derivatives under microwave irradiation
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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
- Azizian, Javad,Mohammadi, Ali A.,Karimi, Ali R.
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p. 415 - 420
(2007/10/03)
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- Palladium-Catalyzed Cyclocarbonylation of o-Iodoanilines with Heterocumulenes: Regioselective Preparation of 4(3H)-Quinazolinone Derivatives
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A catalyst system comprising palladium acetate - bidentate phosphine is effective for the cyclocarbonylation of o-iodoanilines with heterocumulenes at 70-100°C for 12-24 h to give the corresponding 4(3H)-quinazolinone derivatives in good yields. Utilizing o-iodoaniline with isocyanates, carbodiimides, and ketenimines for the reaction, 2,4-(1H,3H)-quinazolinediones, 2-amino-4(3H)-quinazolinones and 2-alkyl-4(3H)-quinazolinones were obtained, respectively. The nature of the substrates including the electrophilicity of the carbon center of the carbodiimide, and the stability of the ketenimine, influence the product yields of this reaction. Urea-type intermediates are believed to be generated first in situ from the reaction of o-iodoanilines with heterocumulenes, followed by palladium-catalyzed carbonylation and cyclization to yield the products.
- Larksarp, Chitchamai,Alper, Howard
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p. 2773 - 2777
(2007/10/03)
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- Rearrangement of 4-imino-(1H,4H)-3,1-benzoxazine-2-ones to 2,4- quinazolinediones via an isocyanate carboxamide intermediate
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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.
- Azizian, Javad,Mehrdad, Morteza,Jadidi, Khosrow,Sarrafi, Yaghob
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p. 5265 - 5268
(2007/10/03)
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- Relationships between the chemical structure of substances and their antimycobacterial activity against atypical strains. Part 18. 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones and isosteric 3-phenylquinazoline-2,4(1H,3H)-diones
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A series of 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones 2 and 3-phenylquinazoline-2,4(1H,3H)-diones 5 substituted on the phenyl rings were synthesized. The target compounds as well as the intermediates were tested against Mycobacterium tuberculosis, M. kansasii, and M. avium. The replacement of the oxygen atom by nitrogen resulted in a decrease or loss of antimycobacterial activity. 2-[(Ethoxycarbonyl)amino]benzanilides 4 appeared to be inactive. Salicylanilides 1 and 3-phenyl-2H-1,3-benzoxazine-2,4(3H)-diones 2 exhibit significant activity against both M. tuberculosis and nontuberculous mycobacteria (the MICs within the range of 4-250 μmol/l for all compounds). The antimycobacterial activity of the compounds increases with increasing both electron-withdrawing properties and hydrophobicity of the substituent(s) on the phenyl moiety. The antimycobacterial profile of the compounds was analyzed according to the criteria based on vector algebra, such as cosine coefficients. Moreover, salicylanilides 1 exhibit activity against other microorganisms tested by the agar diffusion method.
- Waisser, Karel,Machacek, Milos,Dostal, Hynek,Gregor, Jiri,Kubicova, Lenka,Klimesova, Vera,Kunes, Jiri,Palat Jr., Karel,Hladuvkova, Jana,Kaustova, Jarmila,Moellmann, Ute
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p. 1902 - 1924
(2007/10/03)
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