| 摘要 |
The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I)
wherein
y is any integer from 1 to 8;
z is any integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1;
X is -CO-(Y) k -(R 1 ) n or SO 2 -(Y) k -(R 1 ) n ;
k is 0 or 1
Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group);
or Y is a cycloalkenyl or polycycloalkenyl group;
each R 1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms;
or each R 1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and
n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or
alternatively R 1 may be selected from a peptido radical, for example having from 1 to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of 1 to 4 amino acid residues). |
