[EN] COMPOUND LIBRARIES<br/>[FR] BANQUES DE COMPOSES
申请人:BIOFOCUS PLC
公开号:WO2005023794A2
公开(公告)日:2005-03-17
The present invention provides a compound library targeted to receptors that recognise a central secondary amide moiety. The library is designed around an acetamide coupled to a piperidine moiety. A combination of specific motifs R1, R2, R3, and R4 are appended from the central scaffold and are designed to pick up different interactions at a receptor site. The library comprises or consists of a set of structurally related compounds of general formula (II).
Synthesis and gastric antisecretory activity of N-cyano-N'-(phenyl-pyridinylmethyl)guanidine derivatives.
N-Alkyl-N'-cyano-N"-(substituted phenyl-pyridinylmethyl) guanidine derivatives were synthesized and tested for inhibitory activity against gastric secretion in rats. Several of the compounds synthesized showed an inhibiting activity as potent as that of cimetidine against basal gastric secretion but showed less potent activity than cimetidine against histamine-stimulated gastric secretion. Some structure-activity relationships are discussed.