Structure-Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands^†.

ABSTRACT: New classes of alkylated hetarylpropylguanidines with different functionality and variation in spacer length were synthesized to determine their behavior at the four histamine receptor (H₁R, H₂R, H₃R, H₄R) subtypes. Alkylated guanidines with different terminal functional groups and varied basicity, like amine, guanidine and urea were developed, based on the lead structure SK&F 91486 (2). Furthermore, heteroatomic exchange at the guanidine structure of 2 led to simple analogues of the lead compound. Radioassays at all histamine receptor subtypes were accomplished, as well as organ bath studies at the guinea pig (gp) ileum (gpH₁R) and right atrium (gpH₂R). Ligands with terminal functionalizat

SUBMITTER: Pockes S 

PROVIDER: S-EPMC6401531 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature