1255766-07-4Relevant academic research and scientific papers
The structure and use of the converted inhibitor prionoproteins
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Paragraph 0074-0075; 0082, (2016/10/09)
Provided is a novel compound which is capable of inhibiting the formation of an infectious prion protein via binding to a normal prion protein. Specifically provided is a compound represented by formula (1). In formula (1), X represents a carbon atom or a nitrogen atom; R1 and R2 may be either the same or different and represent a hydrogen atom, an oxygen atom, a halogen atom, a hydroxy group, a mercapto group, a cyano group, a carboxy group, a carbamoyl group, an alkoxycarbonyl group, an acyloxy group, an acyl group, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted amino group, etc.; and R3 to R6 may be either the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, etc., provided that at least one of R1 and R2 represents a group other than hydrogen atom.
Synthesis of GN8 derivatives and evaluation of their antiprion activity in TSE-infected cells
Kimura, Tsutomu,Hosokawa-Muto, Junji,Kamatari, Yuji O.,Kuwata, Kazuo
, p. 1502 - 1507 (2011/04/23)
A series of GN8 derivatives were synthesized from various diamines, carboxylic acid derivatives, and nitrogen nucleophiles, and their antiprion activity was tested in TSE-infected mouse neuronal cells. We found that two ethylenediamine units, hydrophobic substituents on the nitrogen atoms, and the diphenylmethane scaffold were essential structural features responsible for the activity. Seven derivatives bearing substituents at the benzylic position exhibited an improved antiprion activity with the IC50 values of 0.51-0.83 μM. Conformational analysis of model compounds suggested that the introduction of the substituent at the benzylic position restricted the conformational variability of the diphenylmethane unit.
