58290-51-0Relevant academic research and scientific papers
Novel cryptands containing thiourea units as a part of the macrocyclic framework
Lukyanenko, Nikolay G.,Kirichenko, Tatiana I.,Scherbakov, Sergey V.
, p. 2347 - 2351 (2002)
Alkylation of diaza-18-crown-6 by N-substituted phthalimides having a terminal halogen in the substituent, and subsequent product interaction with hydrazine hydrate and acid hydrolysis gave corresponding N,N′-disubstituted diaza-18-crown-6 compounds with terminal primary amino groups in the side chains. The reaction of these compounds with carbon disulfide or with appropriate bis[oligo(ethyleneoxy)]isothiocyanates afforded a series of novel cryptands with one or two thiourea units in one of the bridges.
PROTEOLYSIS-TARGETING CHIMERIC MOLECULES (PROTACS) THAT INDUCE DEGRADATION OF INDOLEAMINE 2,3-DIOXYGENASE (IDO) PROTEIN
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Paragraph 0130; 0374; 0376-0379, (2022/02/05)
Disclosed are proteolysis-targeting chimeric molecules (PROTACs) that induce degradation of IDO protein. The disclosed PROTACs typically include a first targeting moiety that binds to IDO (MIDO). The first targeting moiety typically is linked v
Synthesis and in vitro antitumor activity of novel 2-alkyl-5- methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazol-2-ium and 2-alkylellipticin-2-ium chloride derivatives
Mori, Ryota,Kato, Asako,Komenoi, Kousuke,Kurasaki, Haruaki,Iijima, Touru,Kawagoshi, Masashi,Kiran,Takeda, Sho,Sakai, Norio,Konakahara, Takeo
, p. 16 - 35 (2014/06/09)
Twenty-one types of novel ellipticine derivatives and pyridocarbazoles (5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazoles) with a nitrosourea moiety, linked by an oxydiethylene unit at the 2 position, were synthesized, and their cytotoxicity against HeLa S-3 cells was evaluated. Some of these new compounds exhibited potent antitumor activity by comparison with that of ellipticine.
Synthesis of lariat diazacrown ethers with terminal amino groups in the side chains
Lukyanenko,Kirichenko,Shcherbakov
, p. 343 - 350 (2007/10/03)
Treatment of diazacrown ethers with N-(haloalkyl)- and N-(haloethoxy) phthalimides gives the corresponding N,N′- substituted diazacrown ether. Hydrazinolysis of the latter then gives diazacrown ethers with terminal primary amino groups in the side chain. Their reductive methylation using formaldehyde in formic acid gives the dimethylamino derivatives. The presence of a lariat effect was demonstrated by treating the compounds obtained with picrates of alkali and alkaline-earth metals.
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine
Young, Robert J.,Beams, Richard M.,Carter, Keith,Clark, Helen A.R.,Coe, Diane M.,Chambers, C. Lynn,Davies, P. Ifeyinwa,Dawson, John,Drysdale, Martin J.,Franzman, Karl W.,French, Colin,Hodgson, Simon T.,Hodson, Harold F.,Kleanthous, Savvas,Rider, Peter,Sanders, Daniela,Sawyer, David A.,Scott, Keith J.,Shearer, Barry G.,Stocker, Richard,Smith, Steven,Tackley, Miriam C.,Knowles, Richard G.
, p. 597 - 600 (2007/10/03)
The synthesis and in vitro evaluation of the acetamidine derivatives of hetero-substituted lysine and homolysine analogues have identified potent inhibitors of human nitric oxide synthase enzymes, including examples with marked selectivity for the inducible isoform. (C) 2000 Elsevier Science Ltd. All rights reserved.
Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives
Norman, Mark H.,Minick, Douglas J.,Rigdon, Greg C.
, p. 149 - 157 (2007/10/03)
A series of phthalimide and isoindolinone derivatives bridged to 4-(1,2- benzisothiazol-3-yl)-1-piperazinyl was prepared. The compounds were evaluated in vitro at dopamine D2 and serotonin 5-HT(1a) and 5-HT2 receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. The effects of bridge length and conformation on the biological activity of these potential antipsychotic agents are discussed. A four-carbon spacer provided optimal activity within the two homologous series. Conformational investigations of the lead compound, isoindolinone 2, were conducted in an attempt to account for the superior activity observed for the butyl derivatives. On the basis of NMR and molecular modeling studies, two types of folded structures were proposed and several conformationally restrained analogues were synthesized. In general, restrictions incorporated within the linking bridge were detrimental to activity.
Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation
Vidaluc,Calmel,Bigg,Carilla,Briley
, p. 2969 - 2973 (2007/10/02)
A series of flexible 1-(2-aminoethoxy)-3-ar(o)yl(thio)ureas was synthesized and assessed for antiacetylcholinesterase activity. This series was designed in order to optimize the spacer length linking the two pharmacophoric moieties, i.e., the basic nitrog
Novel 1-phenylcycloalkanecarboxylic acid derivatives as potential anticonvulsant agents
Calderon,Newman,Tortella
, p. 3159 - 3164 (2007/10/02)
A series of analogues based on the anticonvulsant carbetapentane (1, 2-[2- (diethylamino)ethoxy]ethyl 1-phenyl-1-cyclopentylcarboxylate) was prepared as potential novel anticonvulsant drugs. Structure-activity relationships of analogues in which the ester function and cyclopentane moieties were modified have been investigated by evaluating their ability to prevent seizures in the rat maximal electroshock test. These compounds (11, ED50 = 16 μmol/kg; 12, ED50 = 86 μmol/kg, and 23, ED50 = 173 μmol/kg) were effective anticonvulsants. Compound 11, an alkyl ether derivative of 1, was more potent than the parent compound (ED50 = 48 μmol/kg) and also showed a 2-fold increase in potency compared to that of the prototypic anticonvulsant drug diphenylhydantoin.
