50463-82-6Relevant academic research and scientific papers
FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Paragraph 00185, (2017/03/08)
Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
Isolation and total syntheses of two new alkaloids, dubiusamines-A, and -B, from Pandanus dubius
Tan, Mario A.,Kitajima, Mariko,Kogure, Noriyuki,Nonato, Maribel G.,Takayama, Hiromitsu
scheme or table, p. 3353 - 3359 (2010/06/17)
Chemical investigation of the crude base of Pandanus dubius led to the isolation of two new alkaloids, dubiusamine-A (1) and dubiusamine-B (2). The structures of the two alkaloids including their absolute configuration were unambiguously confirmed by 1D a
INDANOL DERIVATIVE
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Page/Page column 80, (2010/11/25)
The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: -CO-R4, -CO-O-R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).
New highly potent GABA uptake inhibitors selective for GAT-1 and GAT-3 derived from (R)- and (S)-proline and homologous pyrrolidine-2-alkanoic acids
Fuelep, Guenther H.,Hoesl, Cornelia E.,Hoefner, Georg,Wanner, Klaus T.
, p. 809 - 824 (2007/10/03)
We synthesized proline and pyrrolidine-2-alkanoic acid derivatives in their enantiomerically pure form and evaluated them for their affinity to the GABA transport proteins GAT-1 and GAT-3. Among the compounds presented herein, (R)-pyrrolidine-2-acetic aci
Synthesis and α4β2 nicotinic affinity of unichiral 5-(2-pyrrolidinyl)oxazolidinones and 2-(2-pyrrolidinyl)benzodioxanes
Pallavicini, Marco,Moroni, Barbara,Bolchi, Cristiano,Cilia, Antonio,Clementi, Francesco,Fumagalli, Laura,Gotti, Cecilia,Meneghetti, Fiorella,Riganti, Loredana,Vistoli, Giulio,Valoti, Ermanno
, p. 5610 - 5615 (2007/10/03)
The RS and SR enantiomers of 2-oxazolidinone and 1,4-benzodioxane bearing a 2-pyrrolidinyl substituent at the 5- and 2-position, respectively, were synthesized as candidate nicotinoids. One of the two benzodioxane stereoisomers reasonably fits the pharmac
Synthesis and cholinergic affinity of diastereomeric and enantiomeric isomers of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)- pyrrolidine, 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine and of Their iodomethylates
Dei, Silvia,Bellucci, Cristina,Buccioni, Michela,Ferraroni, Marta,Gualtieri, Fulvio,Guandalini, Luca,Manetti, Dina,Matucci, Rosanna,Romanelli, Maria Novella,Scapecchi, Serena,Teodori, Elisabetta
, p. 3153 - 3164 (2007/10/03)
Four out of the eight possible stereoisomers of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)pyrrolidine, 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine and the corresponding iodomethylates have been synthesised. They were formally derived from hybridisat
A mild and efficient dethioacetalization employing FeCl3·6H2O: Synthesis of DNA-binding pyrrolo[2,1-c][1,4]benzodiazepine ring system and its dimers
Kamal,Laxman,Reddy
, p. 1476 - 1478 (2007/10/03)
A simple and efficient dethioacetalization has been carried out by employing FeCl3·6H2O under mild conditions. This method has been investigated for the synthesis of DNA-interactive pyrrolo[2,1-c][1,4]benzodiazepine antitumour antibiotics via deprotective cyclization process.
Enantiospecific syntheses of (R)- and (S)-proline and some derivatives from D-glucono-1,5-lactone
Mazzini, Claudio,Sambri, Letitia,Regeling, Henk,Zwanenburg, Binne,Chittenden, Gordon J. F.
, p. 3351 - 3356 (2007/10/03)
Carbohydrate-based enantiospecific syntheses of (R)-proline 1 and (S)-proline 2 from the previously reported D-erythro-hexonate ester 9 are described. Azide-substitution reactions on appropriately activated intermediates derived from ester 9, followed by reductive cyclization (H2/Pd-C), gave the substituted pyrrolidines 14 and 22, which were converted into their corresponding N-Cbz derivatives 16 and 24 in conventional manner. Mild acidic hydrolysis of these, followed by oxidation (sodium metaperiodate), gave the protected prolinals 3 and 4, which on further oxidation (sodium chlorite), followed by catalytic hydrogenolysis, gave the prolines 1 and 2. The N-Cbz-prolinol derivatives 5 and 6 are also reported.
The synthesis of a conformationally restricted analog of the anti-migraine drug sumatriptan
Macor,Blank,Post,Ryan
, p. 8011 - 8014 (2007/10/02)
The synthesis of 5-N-Methylaminosulfonylmethyl-3-(N-methylpyrrolidin-2-ylmethyl)indole (1), a conformationally restricted analog of the anti-migraine drug, sumatriptan, is described. To incorporate our novel stereogenic replacement for the aminoethyl side
