- 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 0049; 0065
(2018/04/21)
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- Method for preparing a SUO draw non-Buddhist nun (by machine translation)
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This invention involves a kind of SUO draw non-Buddhist nun (structural formula as follows) and its toluene sulfonate preparation method, this method, in order to P-nitro-phenol as raw materials, by the benzyl protection, reduction, condensation, debenzylation, coupling and salt forming the several step to synthesize SUO draw non-Buddhist nun. The preparation method of fewer steps, high yield, low cost, environmental pollution is small, is suitable for industrial production. (by machine translation)
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Paragraph 0015; 0016
(2016/12/22)
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- 1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: Structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain
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1,3-Disubstituted ureas possessing a piperidyl moiety have been synthesized to investigate their structure-activity relationships as inhibitors of the human and murine soluble epoxide hydrolase (sEH). Oral administration of 13 1-aryl-3-(1-acylpiperidin-4-yl)urea inhibitors in mice revealed substantial improvements in pharmacokinetic parameters over previously reported 1-adamantylurea based inhibitors. For example, 1-(1-(cyclopropanecarbonyl) piperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (52) showed a 7-fold increase in potency, a 65-fold increase in Cmax, and a 3300-fold increase in AUC over its adamantane analogue 1-(1-adamantyl)-3-(1-propionylpiperidin-4-yl) urea (2). This novel sEH inhibitor showed a 1000-fold increase in potency when compared to morphine by reducing hyperalgesia as measured by mechanical withdrawal threshold using the in vivo carrageenan induced inflammatory pain model.
- Rose, Tristan E.,Morisseau, Christophe,Liu, Jun-Yan,Inceoglu, Bora,Jones, Paul D.,Sanborn, James R.,Hammock, Bruce D.
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supporting information; experimental part
p. 7067 - 7075
(2010/12/25)
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- New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)
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Two novel tyrosinase mediated drug delivery pathways have been investigated for the selective delivery of cytotoxic units to melanocytes from urea and thiourea prodrugs. The synthesis of these prodrugs is reported, as well as oximetry data that illustrate that the targets are substrates for tyrosinase. The stability of each of the prodrugs in (i) phosphate buffer and (ii) bovine serum is discussed, and the urea prodrugs are identified as lead candidates for further studies. Finally, HPLC studies and preliminary cytotoxicity studies in a melanotic and an amelanotic cell line, that illustrate the feasibility of the approach, are presented. The Royal Society of Chemistry 2005.
- Knaggs, Sarah,Malkin, Hugh,Osborn, Helen M.I.,Williams, Nana Aba O.,Yaqoob, Parveen
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p. 4002 - 4010
(2007/10/03)
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- 4'-Hydroxyphenylcarbamates of (3aS)eseroline and (3aS)-N(1)- noreseroline: Potential metabolites of the Alzheimer's anticholinesterase drug phenserine
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4'-Hydroxyphenylcarbamates of (3aS)-eseroline (3) and (3aS)-N(1)- noreseroline (4), as predicted metabolites of phenserine (1), were synthesized. Biological evaluation showed that 3 and 4 possessed potent activities for inhibition of acetylcholinesterase and butyrylcholinesterase in vitro. In contrast the intermediates, 4'-benzyloxyphenserine (8) and 4'- benzyloxy N(1)-benzylphenserine (12), demonstrated unusually potent and selective activities against butyrylcholinesterase.
- Yu, Qian-Sheng,Greig, Nigel H.,Holloway, Harold W.,Brossi, Arnold
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- Quantitative Structure-Activity Relationships of Insecticidal Pyrazolines
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Methyl 3-(4-chlorophenyl)-4-methyl-1--2-pyrazoline-4-carboxylates and related compounds were prepared. Their convulsant activity was determined as the minimum dose required to bring about the symptom within 1 h after injection against male adult American cockroaches, Periplaneta americana (L.). Insecticidal activity with metabolic inhibitors for oxidation and hydrolysis was measured 24 h after injection of the test compounds. Variations in each of the activities were analysed by using physicochemical substituent parameters and regression analysis. The findings indicated that the greater the hydrophobicity and the more the electron-withdrawing property of the substituents, the higher were the activities. Variations in each of the two activities were parabolically related to the STERIMOL width parameter with an optimum value of about zero.
- Hasan, Riaz,Nishimura, Keiichiro,Ueno, Tamio
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p. 291 - 298
(2007/10/03)
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