4819-69-6Relevant academic research and scientific papers
Inhibition of bovine plasma amine oxidase by 1,4-diamino-2-butenes and -2-butynes
Jeon, Heung-Bae,Lee, Younghee,Qiao, Chunhua,Huang, He,Sayre, Lawrence M.
, p. 4631 - 4641 (2003)
Bovine plasma amine oxidase (BPAO) was previously shown to be irreversibly inhibited by propargylamine and 2-chloroallylamine. 1,4-Diamine versions of these two compounds are here shown to be highly potent inactivators, with IC50 values near 20 μM. Mono-N-alkylation or N,N-dialkylation greatly lowered the inactivation potency in every case, whereas the mono-N-acyl derivatives were also weaker inhibitors and enzyme activity was recoverable. The finding that the bis-primary amines 1,4-diamino-2-butyne (a known potent inhibitor of diamine oxidases) and Z-2-chloro-1,4-diamino-2-butene are potent inactivators of BPAO is suggestive of unexpected similarities between plasma amine oxidase and the diamine oxidases and implies that it may be unwise to attempt to develop selective inhibitors of diamine oxidase using a diamine construct.
MODULATORS OF CULLIN 3 ADAPTOR KBTBD4 AS ANTI-CANCER COMPOUNDS
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Paragraph 00162-00163, (2021/06/26)
It is provided the use of Pyrimido[4,5-B]indole derivatives as anti-cancer compounds, and more specifically the use of UM171 and its derivatives for treating cancer, by activating the CULLIN3-RING ubiquitin ligase complex which degrades RCOR1 which normal
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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Paragraph 0456, (2013/03/26)
The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position
Nguyen, Thuy,Sakasegawa, Yuji,Doh-Ura, Katsumi,Go, Mei-Lin
experimental part, p. 2917 - 2929 (2011/07/08)
In this paper, we report the synthesis and cell-based anti-prion activity of quinacrine analogs derived by replacing the basic alkyl side chain of quinacrine with 4-(4-methylpiperazin-I-yl)phenyl, (1-benzylpiperidin-4-yl) and their structural variants. Several promising analogs were found that have a more favorable anti-prion profile than quinacrine in terms of potency and activity across different prion-infected murine cell models. They also exhibited greater binding affinities for a human prion protein fragment (hPrP121-231) than quinacrine, and had permeabilities on the PAMPA-BBB assay that fall within the range of CNS permeant candidates. When evaluated on bidirectional assays on a Pgp overexpressing cell line, one analog was less susceptible to Pgp efflux activity compared to quinacrine. Taken together, the results point to an important role for the substituted 9-amino side chain attached to the acridine, tetrahydroacridine and quinoline scaffolds. The nature of this side chain influenced cell-based potency, PAMPA permeability and binding affinity to hPrP121-231.
N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl}arylcarboxamides as novel dopamine D3 receptor antagonists
Newman, Amy Hauck,Cao, Jianjing,Bennett, Christina J.,Robarge, Michael J.,Freeman, Rebekah A.,Luedtke, Robert R.
, p. 2179 - 2183 (2007/10/03)
The dopamine D3 receptor subtype has been targeted as a potential neurochemical modulator of the behavioral actions of psychomotor stimulants, such as cocaine. Previous synthetic studies provided structural requirements for high affinity bindin
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.
S-adenosyl methionine decarboxylase inhibitors
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, (2008/06/13)
The adenosine derivatives represented by the following formula: STR1 and the pharmaceutically acceptable salts thereof wherein R is H or C1 -C7 alkyl, Q is the moiety of the formula STR2 wherein V is H or --COOH X is H, F, Cl, Br, and Z is H, F, Cl, or Br. These compounds are inhibitors of S-adenosylmethione decarboxylase and are useful for treating parasitic infections.
S-Adenosylmethionine decarboxylase inhibitors
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, (2008/06/13)
This invention relates to novel chemical compounds useful as S-adenosylmethionine decarboxylase inhibitors, of the formula, , H2N-Q- wherein R1 is H or F, n is 1 or 2, V1 is H or CH3, V2 is H or COOH, and each of W, X, Y, and Z are H, F, Cl or Br. To the processes useful for their preperation and to their use in the treatment of a variety of condition and disease states associated with a rapid proliferation of cell growth.
