- Isatin-1,2,4-oxadiazole compound as well as preparation method and application thereof
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The invention discloses an isatin-1,2,4-diazole compound and a preparation method and application thereof. The structural general formula of the isatin-1,2,4-diazole compound is shown in the specification. According to the splicing principle of drugs and the structural drug molecular design concept, a five-membered heterocyclic structure is introduced to an isatin molecular skeleton of isatin, and the isatin-1,2,4-diazole derivative is obtained. A biological activity test result shows that the isatin-1,2,4-diazole compound disclosed by the invention has good inhibitory activity on mouse mononuclear macrophage leukemia cells.
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Paragraph 0024-0026
(2021/06/26)
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- Nonionic Isatin Surfactants: Synthesis, Quantum Chemical Calculations, ADMET and Their Antimicrobial Activities
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The most challenge task in the building up of surface-active molecules is maximizing their surface activity with good biological activity. A nonionic surfactant (N-isatin-EOm-Cn where m is 5, 7 and 9 ethylene glycol units and n is 8, 10 and 12) is achieved by first reacting isatin with chloroacetic acid and then with different types of ethoxylated (C8–C12) fatty alcohols that possess 5, 7 and 9 ethylene oxide units. The prepared surfactants were characterized by FTIR and 1H NMR to confirm the structure. The surface activity, biodegradability, antimicrobial, and antifungal activity of the surfactants were evaluated. In addition, quantum chemical calculations and computations of oral bioavailability were performed. The obtained data show that all the synthesized compounds had good surface activity, biodegradability and biological activity.
- Hussein, Ahmed M.,Khowdiary, Manal M.
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p. 489 - 501
(2020/02/11)
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- Multicomponent synthesis of novel class of isatin and 5-isatinyli-denerhodanine based diaminofuran derivatives
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A simple and efficient method has been developed for the synthesis of a new collection of isatin and 5-isatinylidenerhodanine derivatives carrying furan group, from N-(carboxymethyl)isatin through a multi-component reaction is explained. The reactive 1:1
- Baharfar, Robabeh,Rassi, Somayeh
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p. 393 - 399
(2016/10/18)
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- Polyfunctional 4-quinolinones. Synthesis of 2-substituted 3-hydroxy-4-oxo-1,4-dihydroquinolines
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We present here two new methods based on rearrangement reactions to obtain novel 2-substituted 3-hydroxy-4-oxo-1,4-dihydroquinolines, an important family of heterocycles with potential applications. Alkyl 3-hydroxy-4-oxo-1,4-dihydroquinoline-2-carboxylates were obtained by alkoxide promoted rearrangement of alkyl isatinacetates. A second synthetic route involves the alkoxide promoted reaction of both isatin and N-methylisatin, with alkylating agents having acidic methylenes. This reaction leads to the formation of spiroepoxyoxindoles via Darzens' condensation. When phenacyl bromides are used, the initially obtained benzoyl substituted spiroepoxyoxindoles were smoothly transformed into the corresponding 2-benzoyl-3-hydroxy-4-quinolinones with good to excellent yields.
- Shmidt, María S.,Perillo, Isabel A.,Camelli, Alicia,Fernández, María A.,Blanco, María M.
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p. 1022 - 1026
(2016/02/18)
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- Respiratory syncytial virus fusion inhibitors. Part 7: Structure-activity relationships associated with a series of isatin oximes that demonstrate antiviral activity in vivo
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A series of bezimidazole-isatin oximes were prepared and profiled as inhibitors of respiratory syncytial virus (RSV) replication in cell culture. Structure-activity relationship studies were directed toward optimization of antiviral activity, cell permeab
- Sin, Ny,Venables, Brian L.,Combrink, Keith D.,Gulgeze, H. Belgin,Yu, Kuo-Long,Civiello, Rita L.,Thuring, Jan,Wang, X. Alan,Yang, Zheng,Zadjura, Lisa,Marino, Anthony,Kadow, Kathleen F.,Cianci, Christopher W.,Clarke, Junius,Genovesi, Eugene V.,Medina, Ivette,Lamb, Lucinda,Krystal, Mark,Meanwell, Nicholas A.
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scheme or table
p. 4857 - 4862
(2010/04/29)
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- Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening
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A novel series of isatin-based inhibitors of β-secretase (BACE-1) have been identified using a virtual high-throughput screening approach. Structure-activity relationship studies revealed structural features important for inhibition. Docking studies suggest these inhibitors may bind within the BACE-1 active site through H-bonding interactions involving the catalytic aspartate residues.
- Yi Mok,Chadwick, James,Kellett, Katherine A.B.,Hooper, Nigel M.,Johnson, A. Peter,Fishwick, Colin W.G.
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scheme or table
p. 6770 - 6774
(2010/06/12)
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- The Mechanisms of Hydrolysis of the γ-Lactam Isatin and its Derivatives
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The pH dependences of the rates of hydrolysis of isatin, its N-carboxymethyl derivative and its 5-nitro substituted analogues exhibit a complex behaviour, showing a first- and second-order dependence upon hydroxide ion concentration, as well as a pH-independent pathway.The pH dependence is interpreted in terms of the formation of tetrahedral intermediates in different protonic states which may break down to products via hydroxide ion, hydronium ion and water catalysed pathways.These γ-lactams are as reactive, or more reactive, than benzylpenicillin.
- Casey, Lorraine A.,Galt, Ron,Page, Michael I.
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- Isatine derivatives, and their method of use
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A method of treatment of central nervous system disorders with compounds having the formula STR1 and isomers thereof wherein R 1, R 2, R 4, R 5, R 6, and R 7 and as defined in the specification; as well as pharmaceutical compositions thereof.
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- Isatine derivatives, their preparation and use
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A method of treatment with compounds having the formula STR1 R 1 is hydrogen, C 1-6 -alkyl which may be branched, C 3-7 -cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C 1-6 -alkoxy, CH 2 CO 2 R'' wherein R'' is hydrogen or C 1-6 -alkyl which may be branched, CH 2 CN, CH 2 CONR IV R V wherein R IV and R V independently are hydrogen or C 1-6 -alkyl, or CH 2 C( NOH)NH 2 ; R 2 is hydrogen, benzyl, C 1-6 -alkyl which may be branched, or C 3-7 -cycloalkyl; R 4, R 5, R 6, R 7 independently are hydrogen, C 1-6 -alkyl which may be branched, phenyl, halogen, C 1-6 -alkoxy, NO 2, CN, CF 3, OCF 3, or SO 2 NR""R''"" wherein R"" and R''"" independently are hydrogen, aralkoxy, aralkyl, or C 1-6 -alkyl; or R 6 and R 7 together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO 2, CF 3, CN, OCF 3, SO 2 NR"" R""'' wherein R"" and R""'' independently are hydrogen, aralkoxy, aralkyl, or C 1-6 -alkyl, and R 4 and R 5 have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel.The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.
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