43077-90-3Relevant academic research and scientific papers
N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains
B?ck, Michael C.,H?fner, Georg,Wanner, Klaus T.
, (2020)
Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC50 value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.
Phenyl-imidazolyl-fatty acid derivatives
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, (2008/06/13)
Phenyl-imidazolyl-fatty acid derivatives of the formula EQU1 wherein R1, R2, and R3 are the same or different, and are hydrogen or lower alkyl; R4 is hydrogen, alkyl, lower alkoxy, alkylmercapto, or an electro negative moiety; R5 is benzene, benzene substituted by alkyl, lower alkoxy, alkylmercapto or an electro negative moiety, or R5 is an aliphatic moiety; X is a carboxyl moiety or a grouping of a functional carboxylic acid derivative; m is 0, 1, 2, 3, 4, 5 or 6; and n is 0, 1 or 2, And pharmaceutically acceptable non-toxic salts thereof. These phenyl-imidazolyl-fatty acid derivatives exhibit antimycotic activity.
