- 3,4,5-TRISUBSTITUTED-1,2,4-TRIAZOLES AND 3,4,5-TRISUBSTITUTED-3-THIO-1,2,4-TRIAZOLES AND USES THEREOF
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The present disclosure describes novel compounds that are somatostatin receptor type 4 agonists.
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Paragraph 0158; 0168
(2018/12/02)
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- Sodium Iodide/Hydrogen Peroxide-Mediated Oxidation/Lactonization for the Construction of Spirocyclic Oxindole-Lactones
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The sodium iodide/hydrogen peroxide-mediated oxidation/lactonization of indolepropionic acids was achieved, affording the corresponding spirocyclic oxindole-lactones in moderate to high yields. This metal-free procedure features mild reaction conditions, non-toxicity and easy handling, with hydrogen peroxide (H2O2) as a clean oxidant. (Figure presented.).
- Li, Guofeng,Huang, Liwu,Xu, Jiecheng,Sun, Wangsheng,Xie, Junqiu,Hong, Liang,Wang, Rui
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supporting information
p. 2873 - 2877
(2016/09/16)
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- CuCl2/TBHP-mediated direct chlorooxidation of indoles
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CuCl2/TBHP-mediated direct chlorooxidation of indole derivatives under simple aerobic conditions was reported, leading to facile preparations of a range of 3,3-disubstituted 3-chlorooxindoles in good yields and selectivities.
- Wang, Huifei,Liu, Dong,Chen, Huiyu,Li, Jing,Wang, David Zhigang
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supporting information
p. 7073 - 7076
(2015/08/19)
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- Thee-component, one-pot synthesis of hexahydroazepino[3,4-b]indole and tetrahydro-1H-pyrido[3,4-b]indole derivatives and evaluation of their cytotoxicity
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A three-component, four-center Ugi reaction has been developed to produce a novel class of 2-aryl-3-oxo-hexahydroazepino[3,4-b]indole and 2-aryl-3-oxo-tetrahydro-1H-pyrido[3,4-b]indole derivatives in good to high yields. A few of them exhibit moderate cyt
- Reddy, B.V. Subba,Venkata Ganesh,Vani,Ramalinga Murthy,Kalivendi, Shasi V,Yadav
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supporting information
p. 4501 - 4503
(2015/02/06)
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- SMALL MOLECULE INHIBITORS OF HEPATITIS C VIRUS
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The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,.02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6.012,17] -heptadeca- 6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.
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Page/Page column 64-65
(2011/06/11)
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- New potent fluorescent analogues of strigolactones: Synthesis and biological activity in parasitic weed germination and fungal branching
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In this work we report the synthesis of new fluorescent analogues of strigolactones, their spectroscopic properties and the evaluation of their biological activity both on seeds of Orobanche aegyptiaca and on the AM fungus Gigaspora margarita. The synthes
- Prandi, Cristina,Occhiato, Ernesto G.,Tabasso, Silvia,Bonfante, Paola,Novero, Mara,Scarpi, Dina,Bova, Maria Elena,Miletto, Ivana
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experimental part
p. 3781 - 3793
(2011/09/16)
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- Efficient synthesis of tetrahydro-b-carbolin-1-one and dihydroisoquinolin- 1-one derivatives as versatile Intermediates
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An efficient one-pot procedure is described in which an isocyanate intermediate, generated from the corresponding carboxylic acid by a modified Curtius rearrangement, is captured by a tethered aromatic ring in the presence of BF3?OEt2 to generate various
- Judd, Katie E.,Mahon, Mary F.,Caggiano, Lorenzo
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experimental part
p. 2809 - 2817
(2010/01/21)
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- New small molecule inhibitors of hepatitis C virus
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New small molecule inhibitors of HCV were discovered by screening a small library of indoline alkaloid-type compounds. An automated assay format was employed which allowed identification of dimerization inhibitors of core, the capsid protein of the virus. These compounds were subsequently shown to block production of infectious virus in hepatoma cells.
- Wei, Wanguo,Cai, Cuifang,Kota, Smitha,Takahashi, Virginia,Ni, Feng,Strosberg, A. Donny,Snyder, John K.
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scheme or table
p. 6926 - 6930
(2010/06/16)
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- Addition of heterocycles to electron deficient olefins and alkynes catalyzed by gold(III)
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A gold(III)-catalyzed hydroarylation of different olefins is reported here. AuCl3 works as an excellent catalyst to mediate reactions between various heterocycles and electron deficient olefins and alkynes under mild conditions. This gold(III)-based method tolerates different functional groups such as aldehyde, carboxylic acid, nitrile, and is highly efficient. We have shown that some of these reactions complete in minutes at room temperature.
- Li, Zigang,Shi, Zhangjie,He, Chuan
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p. 5049 - 5054
(2007/10/03)
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- Synthesis of 3-alkyl-1,4-dihydrocyclopenta[b]indoles: Unexpected formation of dimeric compounds
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Acid-catalyzed dehydration of 3-alkyl(aryl)-4-methyl-1,2,3,4- tetrahydrocyclopenta[b]indol-3-ols gives dimeric derivatives of 3-alkyl(aryl)-4-methyl-1,4-dihydrocyclopenta[b]indole.
- Taidakov,Nifant'Ev,Talanova, M. Yu.,Lyssenko
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p. 897 - 900
(2007/10/03)
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- Intramolecular Ritter reactions of 2-(2-cyanoethyl)tetrahydrocyclopenta-[b] indole and -carbazole derivatives
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Intramolecular Ritter reactions of 2-(2-cyanoethyl)tetrahydrocyclopenta[b] indole and -carbazole derivatives, prepared by a sequence of two different α-substitutions and Grignard reactions of the indole-based ketones 4-methyl-1,4-dihydrocyclopenta[b]indol-3(2H)-one and 9-methyl-2,3,4,9- tetrahydro-1H-carbazol-1-one, were used as key steps in the construction of various tetracyclic lactam compounds. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Maertens, Faye,Van Den Bogaert, An,Compernolle, Frans,Hoornaert, Georges J.
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p. 4648 - 4656
(2007/10/03)
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- Synthesis and pharmacological evaluation of (indol-3-yl)alkylamides as potent analgesic agents
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A series of (indol-3-yl)alkylamides was synthesized and evaluated for analgesic activity. Two N-(pyridin-4-yl)acetamides, compounds 24 and 25, bearing benzyl or 4-fluorobenzyl moieties in 1-position of indole ring exhibited promising analgesic properties (ED50 = 8.1 and 11 mg/kg p.o., respectively), being as potent as the reference drugs flupirtine (CAS 56995-20-1), ibuprofen (CAS 15687-27-1) and diclofenac (CAS 15307-86-5). The two test compounds were tested for their anti-inflammatory activity by carrageenin-induced edema in rat paw test. 4-Fluorobenzyl derivative 25 whose ID50 was 0.085 ± 0.021 mmol/kg was selected as a lead compound for further pharmacomodulation.
- Fouchard,Marchand,Le Baut,Emig,Nickel
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p. 814 - 824
(2007/10/03)
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