Development of subnanomolar-affinity serotonin 5-HT₄ receptor ligands based on quinoline structures.

ABSTRACT: Two small series of quinoline derivatives were designed starting from previously published quinoline derivatives 7a and b in order to obtain information about their interaction with the 5-HT₄R binding site. Initially, the structure of 7a and b was modified by replacing their basic moiety with that of partial agonist 4 (ML10302) or with that of reference ligand 6 (RS-67-333). Then, the aromatic moieties of 4-quinolinecarboxylates 7a, d-f, and h-k or 4-quinolinecarboxamides 7b, c, and g were modified into those of 2-quinolinecarboxamides 9a-e. Very interestingly, this structure-affinity relationship study led to the discovery of 7h-j as novel 5-HT₄R ligands showing K

SUBMITTER: Castriconi F 

PROVIDER: S-EPMC6148519 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature